1. In-silico Validation of Pyrazolone Derivatives as the Potent Scaffold for Modulating Protein Abnormalities Associated with Parkinson’s Disease
Harsha Ashtekar, Prarambh S. R. Dwivedi, Natasha Aggarwal, Zeena Fernandes, Nimmy Varghese
Harsha Ashtekar, Prarambh S. R. Dwivedi, Natasha Aggarwal, Zeena Fernandes, Nimmy Varghese
Abstract
Aim: We explored pyrazolone derivatives for anti-Parkinson’s activity using in-silico tools to identify novel lead hits against Parkinson’s disease.
Background: Parkinson’s disease is the most predominant neuronal degenerative disorder, caused by protein aggregation and dopamine imbalance. The available therapeutic agents on prolonged exposure lead to severe adverse effects and provide only symptomatic relief. Therefore, it is a need for novel drug molecules that would modulate the disease condition.
Objectives: To identify novel hit molecule for a sequence of molecules designed using pyrazolone as a parent moiety by computer-aided drug design techniques.
Materials and Methods: Derivatives are generated by various substituted functional groups and further, pharmacokinetic profile, the biological spectrum, adverse drug effect, molecular docking, molecular dynamic, and MMPBSA evaluation was performed.
Results: Thirty-four compounds follow a pharmacokinetic profile. 15 compounds were predicted to possess a positive central nervous system activity score. The compounds C13, C12, C14, A1, C9, and C7 possessed the highest binding affinity of -7.81, -3.15, -8.49, -3.43, -6.09, and -2.77 kcal/mol with various targets involved in Parkinson’s disease. Compound C13 exhibited highest binding score of -9.78 kcal/mol for mono amino oxidase-B.
Conclusion: From our investigations, we hope that novel substituted pyrazolone derivatives can act as an assuring virtual hit molecule for developing anti-Parkinson’s agents. These predictions obtained via in-silico techniques could aid the development of pharmacological inhibitors for Parkinson’s disease.
Background: Parkinson’s disease is the most predominant neuronal degenerative disorder, caused by protein aggregation and dopamine imbalance. The available therapeutic agents on prolonged exposure lead to severe adverse effects and provide only symptomatic relief. Therefore, it is a need for novel drug molecules that would modulate the disease condition.
Objectives: To identify novel hit molecule for a sequence of molecules designed using pyrazolone as a parent moiety by computer-aided drug design techniques.
Materials and Methods: Derivatives are generated by various substituted functional groups and further, pharmacokinetic profile, the biological spectrum, adverse drug effect, molecular docking, molecular dynamic, and MMPBSA evaluation was performed.
Results: Thirty-four compounds follow a pharmacokinetic profile. 15 compounds were predicted to possess a positive central nervous system activity score. The compounds C13, C12, C14, A1, C9, and C7 possessed the highest binding affinity of -7.81, -3.15, -8.49, -3.43, -6.09, and -2.77 kcal/mol with various targets involved in Parkinson’s disease. Compound C13 exhibited highest binding score of -9.78 kcal/mol for mono amino oxidase-B.
Conclusion: From our investigations, we hope that novel substituted pyrazolone derivatives can act as an assuring virtual hit molecule for developing anti-Parkinson’s agents. These predictions obtained via in-silico techniques could aid the development of pharmacological inhibitors for Parkinson’s disease.
2. Development of Size Optimized Bromelain Loaded Nanocarriers by Box-Behnken Design
Anit J. George, Fels Saju, Bharat Mishra
Anit J. George, Fels Saju, Bharat Mishra
Abstract
Bromelain (BRN) is an extensive product of investigation, regarded as effective naturally produced anticancer agents. Heterogeneity of tumors amongst patients and within disease, generates a necessity of personalization of nanomedicine. The size of nanoparticle is found to be a significant target in enhancing precision therapeutics, by fondly accumulate it within the tumor microenvironment. The objective of the study is to achieve an optimum size of 50 to 100 nm BRN loaded nano carriers, to intensify the EPR effect and thereby overcome heterogeneity. Optimization of the nanoparticles commenced with the interrogation of effect by various formulation variables. The development of nanoparticles carried out by the nanoprecipitation method, where three independent variables, such as the amount of PLGA, Tween 80 and BRN are chosen after an overall screening and employed in Design Expert Software. The selected Box-Behnken design provides a total of 17 confirmatory runs at varied levels of independent variables and detected its influence on responses. The runs resulted in an optimized formula with the desired particle size of 78.64 ± 2.14 nm and a maximum entrapment efficiency of 89.14% at 24th hour. Then the selected formula characterized for polydispersity index, zeta potential, scanning electron microscopy, determination of drug content, study of in-vitro drug release etc.
3. Anti-Alzhimer Activity of Bay Leaves in Scopolamine-induced Rat Model
Sonali G. Banpure, Vitthal V. Chopade, Pravin D. Chaudhari, Pramod L. Ingale
Sonali G. Banpure, Vitthal V. Chopade, Pravin D. Chaudhari, Pramod L. Ingale
Abstract
Indian spices always play a great role in Ayurveda and Indian medicine. So, analyzing these plants for their unknown and specialized activity is great. Nearly all the spices have some activity on the brain and CNS. Bay leaves are one of the most common culinary spices from dayto day life of Indians. In this study, we have studied bay leaves for their anti-Alzheimer activity which depends on the inhibition of acetylcholine esterase and butyrylcholinesterase. For this study, firstly bay leaf oil was extracted by hydrodistillation. Further phytoconstituent like alpha-pinene, terpineol, 1,8-cineol, sabinene, and methyl eugenol were isolated and purified by using TLC, HPLC, and column chromatography followed by fractional distillation. These isolated phytoconstituents were evaluated for their acetylcholinesterase and butyrylcholinesterase inhibition activity in scopolamine-induced rats. This study used galanthamine as a reference and compared the anti-alzheimer activity of all isolated phytoconstituents.
4. Comparison between Ethylcellulose and Polymethacrylate Topical Nanosponges Loaded with Butenafine Hydrochloride
Hayder H. A. Hussein, Hanan J. Kassab
Hayder H. A. Hussein, Hanan J. Kassab
Abstract
In this study, nanosponges (NS) loaded with butenafine hydrochloride (a broad-spectrum benzylamine antifungal agent) were successfully prepared by emulsion solvent diffusion method using ethylcellulose or polymethacrylate as retarder polymers. PVA was used as a stabilizer. NS 18 formulations were formulated with various ratios of 1:1, 1:2, and 1:3 (%, w/w), using different PVA concentrations of 0.25, 0.5, and 0.75 (%, w/w). The prepared formulations were tested for particle size in terms of diameter, which ranged from (73.6 ± 15.4–991 ± 11.2 nm) for ethyl cellulose NS, and from (116 ± 0.96–1439.6 ± 237.4 nm) for polymethacrylate NS. The entrapment efficiency of the selected formulas (F1, F10) were (74.12 ± 2.60%) and (72.89 ± 1.41%). The selected formulas F1 and F10 were also evaluated for their polydispersity, yield, and in-vitro drug release. The release of BFNS powder in F10 (90.42 ± 1.81%) was higher than that of ECNS F1 powder (78.53 ± 3.24%) within 24 hours. Evaluation tests of the scanning electron microscope (SEM), Fourier transform infrared ray (FTIR), and powder X-ray diffraction (PXRD) confirmed the NS’ spherical and porous features, the absence of any drug polymer interaction, and the stability of the drug in the delivery system. The two formulas of F1 and F10 were found to exhibit prolonged drug release, which minimizes side effects and dosing frequency of BF drug application.
5. Using of Nano-poly Chitosan Cephalexin Drug to Inhibit Spread Cancer Cells
Aliaa H. Abbas, Mohammad N. Al-Baiati
Aliaa H. Abbas, Mohammad N. Al-Baiati
Abstract
In our work, a natural chitosan nano polymer was synthesized and characterized by fourier transform infrared (FTIR), proton nuclear magnetic resonance (1H-NMR), atomic force microscopy (AFM), transmission electron microscope (TEM) and X-ray diffraction (XRD) techniques. Then the nano-chitosan was linked with cephalexin drug, which FTIR characterized, and 1H-NMR techniques. The biological activity of the nano-chitosan cephalexin drug was studied by measured cell line breast cancer. Where it showed a high rate in preventing the spread of breast cancer.
6. Insights of In-silico Neurotoxicity Studies of Glucuronolactone, Taurine and Gluconolactone Correlating the Induced Neuronal Alteration in Rat Pups
Revathi Boyina, Sujatha Dodoala, Sumalatha Gindi, Pooja Reddy M, Prasanna K. Desu
Revathi Boyina, Sujatha Dodoala, Sumalatha Gindi, Pooja Reddy M, Prasanna K. Desu
Abstract
Background: Significant concentrations of food additives found in energy drinks have the potential to be neurotoxic and promote oxidative stress, among other negative consequences. Pregnant rats were split up into six groups for the current study. Group 1 received vehicle, CAF standard (25 mg/kg p.o.), groups 3-6 received GLUR (5 mg/kg p.o.), TAU (8 mg/kg p.o.), GLU (84 mg/kg p.o.), and combinations of the three chosen food additives (CF), respectively. From prenatal day 3 through postnatal day 15, certain food additives were administered to pregnant rats at significant doses. After parturition on PND 21, behavioral changes were assessed using the Rotarod, active avoidance, and elevated plus maze tests. On PND 30, 45, and 60, rat brain tissue had its acetylcholine and epinephrine levels evaluated. Further, on days 30 and 60, brain tissue was assessed for the presence of oxidative stress markers such as lipid peroxidation, catalase, superoxide dismutase, and glutathione peroxidase. Finally, histopathological studies were carried out in brain hippocampal region. Further in-silico studies were carried out on selected receptors.
Results: Rat pups fed with food additives showed a significant (p < 0.001) change in behavior, including memory, cognition, and motor activity. Increased lipid peroxidation and decreased antioxidant enzymes were significant in TAU and CF groups. Further in-silico studies were carried out, where GLUR showed high binding affinity to specific receptor targets, GABA A and NMDA1 receptors, and specific enzyme targets MAO A and MAO B neurotransmitter metabolic enzymes compared to caffeine hinted the decrease in neurotransmitters as in-vivo studies.
Conclusion: The current findings support the hypothesis that the chosen dose and mix of food additives altered rat pups’ neurobehavioral and neurotransmitter profiles.
Results: Rat pups fed with food additives showed a significant (p < 0.001) change in behavior, including memory, cognition, and motor activity. Increased lipid peroxidation and decreased antioxidant enzymes were significant in TAU and CF groups. Further in-silico studies were carried out, where GLUR showed high binding affinity to specific receptor targets, GABA A and NMDA1 receptors, and specific enzyme targets MAO A and MAO B neurotransmitter metabolic enzymes compared to caffeine hinted the decrease in neurotransmitters as in-vivo studies.
Conclusion: The current findings support the hypothesis that the chosen dose and mix of food additives altered rat pups’ neurobehavioral and neurotransmitter profiles.
7. Spectrophotometric Techniques for the Determination of Sitagliptin Phosphate Drugs in Bulk and few Pharmaceutical Products by using MBTH and Ferric Chloride
Dalil M. H. Alher, Saad I. Al-Abadi, Muneer A. Al-Da’amy
Dalil M. H. Alher, Saad I. Al-Abadi, Muneer A. Al-Da’amy
Abstract
The current study aimed to evolve a method for the detection of sitagliptin (STG) concentration. The method was built on the estimation of absorbance STG wave 612 nm concentration range was (1–18 ppm) and was reacted for oxidative coupling of pregabalin with 3-methyl-2-benzthiazolinone hydrazone (MBTH) to form green in color. The captured product was analyzed statistically by using (f and t-test). The current manners were profitably applied to the investigation of the pharmaceutical establishment. It is evicting that the modern manner is responsive and meticulous for terming of STG a different pharmaceutical formation.
8. Formulation and In-vitro Evaluation of Two Layers Tablet for Dual Release of a Model Drug
Mushtaq J. Mohammed, Wedad K. Ali
Mushtaq J. Mohammed, Wedad K. Ali
Abstract
Objective: Glimepiride is a third-generation sulfonylurea medication that has been used to treat type 2 diabetes (T2D) mellitus. It is class II drug according to the biopharmaceutical classification system (BCS) characterized with its low solubility and high permeability. Due to the drug’s weak water solubility, its bioavailability is restricted by its dissolving rate. This study aimed to develop a bilayer tablet of glimepiride with one layer for immediate release (IR), a dose of 2 mg, a second layer for sustained release (SR), and a 4 mg dose Immediate release layer included solid dispersion of glimepiride.
Methods: Glimepiride solid dispersions were prepared utilizing four water-soluble carriers (poloxamer 188, polyethylene glycol (PEG6000), Kollicoat IR and soluplus) by solvent evaporation and fusion techniques at 1:1, 1:2, and 1:4 ratios and evaluated in 0.1 N of HCL buffer pH 1.2 with 1% of sodium lauryl sulphate (SLS) for 2 hours. utilizing a USP-II paddle-type dissolution apparatus containing 900 mL dissolution medium kept at 37 ± 0.5℃ and 50 rpm. The sustained release layer of glimepiride bilayer tablet was prepared using various polymers, including HPMC K15, HPMC K4, xanthan gum, carbopol 934 and ethyl cellulose at 1:1, 1:2,1:3 ratios and combination of polymers in phosphate buffer pH 6.8 for 12 hours. The prepared solid dispersion of immediate release were evaluated by X-ray powder diffraction (PXRD), and fourier transform infrared spectroscopy for selected SD9. The FTIR spectroscopy analysis for selected formula (F24) of sustained layer, angle of repose, Hausner’s ratio and Carr’s Index were used to evaluate the flowability and compressibility of the formulation powders during the pre-compression investigations, while, thickness, hardness, weight variation, friability, drug content, for prepared tablets.
Results: The results revealed that SD9 at ratio (1:4 glimepiride: soluplus) was the optimal formula since 94% of drug released at 2 hours for immediate layer formula 24, which included ethyl cellulose polymer in a 1:1 ratio in the sustained layer of the tablet, was chosen as the optimal formula out of another formula (F1–F28), This formula demonstrated acceptable sustained properties of the glimepiride over the course of 12 hours and approximately 96% of the medication was released.
Conclusion: This study succussed in designing bilayer tablets containing glimepiride solid dispersion formulation in the first immediate release layer and untreated pure drug formulation in the second layer for sustaining the release of the drug for a specific period of time to be used as the effective treatment of type II diabetes mellitus.
Methods: Glimepiride solid dispersions were prepared utilizing four water-soluble carriers (poloxamer 188, polyethylene glycol (PEG6000), Kollicoat IR and soluplus) by solvent evaporation and fusion techniques at 1:1, 1:2, and 1:4 ratios and evaluated in 0.1 N of HCL buffer pH 1.2 with 1% of sodium lauryl sulphate (SLS) for 2 hours. utilizing a USP-II paddle-type dissolution apparatus containing 900 mL dissolution medium kept at 37 ± 0.5℃ and 50 rpm. The sustained release layer of glimepiride bilayer tablet was prepared using various polymers, including HPMC K15, HPMC K4, xanthan gum, carbopol 934 and ethyl cellulose at 1:1, 1:2,1:3 ratios and combination of polymers in phosphate buffer pH 6.8 for 12 hours. The prepared solid dispersion of immediate release were evaluated by X-ray powder diffraction (PXRD), and fourier transform infrared spectroscopy for selected SD9. The FTIR spectroscopy analysis for selected formula (F24) of sustained layer, angle of repose, Hausner’s ratio and Carr’s Index were used to evaluate the flowability and compressibility of the formulation powders during the pre-compression investigations, while, thickness, hardness, weight variation, friability, drug content, for prepared tablets.
Results: The results revealed that SD9 at ratio (1:4 glimepiride: soluplus) was the optimal formula since 94% of drug released at 2 hours for immediate layer formula 24, which included ethyl cellulose polymer in a 1:1 ratio in the sustained layer of the tablet, was chosen as the optimal formula out of another formula (F1–F28), This formula demonstrated acceptable sustained properties of the glimepiride over the course of 12 hours and approximately 96% of the medication was released.
Conclusion: This study succussed in designing bilayer tablets containing glimepiride solid dispersion formulation in the first immediate release layer and untreated pure drug formulation in the second layer for sustaining the release of the drug for a specific period of time to be used as the effective treatment of type II diabetes mellitus.
9. Nanoemulsion Formulation of Leflunomide for Transdermal Delivery: Preparation and Characterization
Bakr I. Nashat, Khalid K. Al-Kinani
Bakr I. Nashat, Khalid K. Al-Kinani
Abstract
Leflunomide (LEF) is an antirheumatic drug belonging to a class of drugs known as disease modifying antirheumatic drugs, indicated for moderate to severe psoriatic arthritis and rheumatoid arthritis. Orally administrated LEF causes many side effects that could result in treatment failure. Hence, in this study, leflunomide was formulated as a nanoemulsion to develop a transdermal dosage form that can circumvent such side effects and increase the rate of successful treatment by improving patient compliance with the medication. The nanoemulsion area was constructed by using pseudo-ternary phase diagrams. A total of 20 nanoemulsion formulas were prepared. These formulas’ mean particle size, zeta potential, and droplet morphology were studied. Thermodynamic stability studies were performed to test the stability of the prepared formulations. Also, the in-vitro release of the drug from the formulations was evaluated using phosphate buffer saline pH 7.4 as the release medium. According to the saturation solubility study results, capryol TM 90 was selected as oil, labrasol and Tween 20 as surfactants for formulation coded A1 and A2, respectively, and transcutol p as cosurfactant together with deionized water as the aqueous phase for the preparation of nanoemulsions. The LEF-nanoemulsion formulations were in the nanosize range (from 54.7–210.2 nm). Images for the chosen formulas revealed dark spherical nanoemulsion droplets against bright surroundings. All of the preparation showed a complete drug release by the end of 220 minutes and the release was highly dependent on the particle size. Based on the result of this study, the prepared LEF-nanoemulsion is successfully prepared and can be considered a promising approach to developing a transdermal preparation.
10. Synthesis of Thiolated Cashew Gum and Its Evaluation as an Improved Mucoadhesive Agent in Drug Delivery
Pranab K. Bandyopadhyay, Amit K. Nayak
Pranab K. Bandyopadhyay, Amit K. Nayak
Abstract
The objectives of present research work were to extract cashew exudate gum (CG), perform thiolation of extracted CG, and evaluate the synthesized thiolated cashew exudate gum (TCG) as a mucoadhesive agent in designing metronidazole mucoadhesive gels and metronidazole mucoadhesive buccal discs. The CG was thiolated or thiol-modified via esterification utilizing thioglycolic acid and hydrochloric acid. Metronidazole mucoadhesive gels and metronidazole mucoadhesive buccal discs made of unmodified CG and TCG (as mucoadhesive agent) were formulated and evaluated to reveal their bio-mucoadhesive potentials in drug delivery. The yield of thiolated product (TCG) was 56.24%, and the thiol-group content in TCG was found to be 9.06 mM of thiol group/g of CG. FTIR analysis indicated the thiolation of CG in the synthesized TCG. Both types of formulations (mucoadhesive gels and buccal discs) made of TCG exhibited excellent improved ex-vivo bio-mucoadhesion and consistent pattern of metronidazole releasing over a prolonged time. The synthesized TCG can be utilized as an improved mucoadhesive material in designing bio-mucoadhesive systems for drug delivery.
11. Biosynthesis and Characterization of CdO: Ag NPs using Moringa Leaves Extract for Use as Anti-microbial Activity
Suaad A. Muhammed, Nada K. Abass
Suaad A. Muhammed, Nada K. Abass
Abstract
The current research focuses on synthesizing cadmium oxide (CdO), CdO: Ag nanoparticle (NPs) by green method using the Moringa leaves Extract (MLE) and its anti-microbial activity. Using UV-vis spectroscopy to determine the formation of CdO: Ag NPs where the energy gap of the prepared samples was 2.79, 2.67, and 2.46 for CdO, CdO: Ag 3% and CdO: Ag 5%, respectively. The biological substances in responsibility of capping the produced NPs were identified using FTIR. The NPs were further characterized by X-ray diffractograms (XRD). The average grain size for CdO, CdO: Ag (3 and 5%) were 15.322, 15.5, and 36.84 nm, respectively, scanning electron microscope (SEM), energy dispersive X-ray (EDX) and atomic force microscope (AFM), were obtained the average diameter 18.88, 43.48, 99.15 nm for CdO, CdO: Ag 3% and CdO: Ag 5%, respectively. The anti-bacterial activity of green synthesized CdO: Ag(NPS) was investigated against (Staphylococcus aureus, Escherichia coli, and Klebsiella pneumonia) at diff erent concentrations, showing clear inhibition zones from 30 to 38 mm, thereby indicating its inhibitory activity.
12. Association of Inflammatory Bowel Disease and Tumor Necrosis Factor-863 C/A Polymorphism in Iraq
Sali E. Hussian, Wafaa S. Mahood
Sali E. Hussian, Wafaa S. Mahood
Abstract
Background: The underlying causes of inflammatory bowel disease (IBD) are unknown, but they are thought to be a combination of genetics, environmental factors, abnormal immune responses, and disruption of the gut microbiota. This study aims to investigate the effect of tumor necrosis factor-alpha (TNF-α) -863 C/A(rs 1800630) single nucleotide polymorphism (SNP) in inflammatory bowel patients and it is relation with the patient’s clinical characteristics.
Methods: The study was conducted on 74 blood samples from patients of IBD including 47 patients with ulcerative colitis (UC) and 27 patients with Crohn’s disease (CD) in addition to 20 blood samples apparently healthy individuals, TNF-α-863 C>A genotype was screened by PCR and Sanger sequencing techniques.
Results: The results showed that the homozygous CC genotype frequency was the higher genotype frequency in 45/60 (75%) for IBD patients with less than 50 years ages compared with 7/14 (50%) the IBD patients with more than 50 years, significantly high association OD (CI): 2.75 (1.38–4.08), The allelic C frequency in ulcerative colitis (UC) patients was (0.83) and significantly higher than the A allele frequency (0.17) and it may act as risk factor inflammatory disease. The homozygous CC genotype of the TNF-α-863 gene was 9/27 (70.37%) in CD patients compared with 6/20 (30%) in the control group with high significant differences (p ≤ 0.01, OR=1.00). Significant differences also applied for the heterozygous CA genotype in -863 SNP, it was 8/27 (29.62%) compared with the control group 14/20 (70%) the odds ratio (2.62), while the homozygous AA genotype frequency showed no significant association with CD (p -1.00).
Conclusion: The frequency of homozygous CC genotype of the TNF-α-863 gene was higher in CD patients than in the control group with significant differences. Significant differences also applied for the heterozygous CA genotype while the three genotypes (CC, CA and AA) of the TNF-α-863 gene showed non-significant differences in ulcerative patients in comparison with the control.
Methods: The study was conducted on 74 blood samples from patients of IBD including 47 patients with ulcerative colitis (UC) and 27 patients with Crohn’s disease (CD) in addition to 20 blood samples apparently healthy individuals, TNF-α-863 C>A genotype was screened by PCR and Sanger sequencing techniques.
Results: The results showed that the homozygous CC genotype frequency was the higher genotype frequency in 45/60 (75%) for IBD patients with less than 50 years ages compared with 7/14 (50%) the IBD patients with more than 50 years, significantly high association OD (CI): 2.75 (1.38–4.08), The allelic C frequency in ulcerative colitis (UC) patients was (0.83) and significantly higher than the A allele frequency (0.17) and it may act as risk factor inflammatory disease. The homozygous CC genotype of the TNF-α-863 gene was 9/27 (70.37%) in CD patients compared with 6/20 (30%) in the control group with high significant differences (p ≤ 0.01, OR=1.00). Significant differences also applied for the heterozygous CA genotype in -863 SNP, it was 8/27 (29.62%) compared with the control group 14/20 (70%) the odds ratio (2.62), while the homozygous AA genotype frequency showed no significant association with CD (p -1.00).
Conclusion: The frequency of homozygous CC genotype of the TNF-α-863 gene was higher in CD patients than in the control group with significant differences. Significant differences also applied for the heterozygous CA genotype while the three genotypes (CC, CA and AA) of the TNF-α-863 gene showed non-significant differences in ulcerative patients in comparison with the control.
13. Rheological and Thermal Behavior of Choline-based Deep Eutectic Ionic Liquid and its Impact on a Poorly Soluble Drug Model
Rafi f Raad, Nidhal K. Maraie, Ayad MR Raauf
Rafi f Raad, Nidhal K. Maraie, Ayad MR Raauf
Abstract
Objective: This study was conducted to prepare a deep eutectic ionic liquid based on choline chloride and malonic acid (Maline) in diff erent molar ratios and evaluate the maline properties to designate the best ratio for solubilizing risperidone, a poorly soluble drug model.
Method: Malines were prepared using choline chloride and malonic acid in 1:0.8, 1:0.9 and 1:1 molar ratios. The characterization of malines involved pH rating, rheological test and thermal behavior using DSC. In addition to estimating the interactions that occur between the choline chloride and malonic acid to form the malines theoretically using the computational prediction program Mercury and experimentally by 1H-NMR and FTIR.
Results: This study shows that all malines (M1-M3) represents an acidic pH and high viscosity with a non-newtonian behavior (shear thinning property ) at low temperature while a Newtonian behavior (shear rate-independent) at high temperatures. In malines (M1-M3) thermograms, the absence of pure compounds melting point peaks with a glass transition temperature at -14℃ that confi rms the DES property. FTIR and 1H-NMR results represent a hydrogen bond formation between choline chloride and malonic acid and further between maline and risperidone which is similar to the computational prediction. Maline (M1) with molar ratio of 1:1 had a preferable solubilizing eff ect on risperidone reaching 20.5 mg/mL, while in (M2) (1:0.9) reaches 13.6 mg/mL, and in (M3) reaches 11.9 mg/mL.
Conclusion: Maline (M1) was chosen as the optimum molar ratio to form a deep eutectic ionic liquid that successfully enhances risperidone solubility and boosts its bioavailability.
Method: Malines were prepared using choline chloride and malonic acid in 1:0.8, 1:0.9 and 1:1 molar ratios. The characterization of malines involved pH rating, rheological test and thermal behavior using DSC. In addition to estimating the interactions that occur between the choline chloride and malonic acid to form the malines theoretically using the computational prediction program Mercury and experimentally by 1H-NMR and FTIR.
Results: This study shows that all malines (M1-M3) represents an acidic pH and high viscosity with a non-newtonian behavior (shear thinning property ) at low temperature while a Newtonian behavior (shear rate-independent) at high temperatures. In malines (M1-M3) thermograms, the absence of pure compounds melting point peaks with a glass transition temperature at -14℃ that confi rms the DES property. FTIR and 1H-NMR results represent a hydrogen bond formation between choline chloride and malonic acid and further between maline and risperidone which is similar to the computational prediction. Maline (M1) with molar ratio of 1:1 had a preferable solubilizing eff ect on risperidone reaching 20.5 mg/mL, while in (M2) (1:0.9) reaches 13.6 mg/mL, and in (M3) reaches 11.9 mg/mL.
Conclusion: Maline (M1) was chosen as the optimum molar ratio to form a deep eutectic ionic liquid that successfully enhances risperidone solubility and boosts its bioavailability.
14. The Protective Potential effect of Metformin during Acetaminophen Hepatotoxicity through Nrf2 Activation
Safa H. Mohsin*, Inam S. Arif, Muthanna I. Hameed
Safa H. Mohsin*, Inam S. Arif, Muthanna I. Hameed
Abstract
Acetaminophen (N-acetyl-para-aminophenol [APAP]) is the most commonly used medication for the relief of pain and fever around the world. Although APAP is safe and effective at a therapeutic level, acute overdose causes hepatotoxicity and severe liver damage. The hepatotoxicity induced by APAP is a persistent global problem that results in hepatotoxicity cases; acute liver failure and even death worldwide. This toxicity is characterized by extensive oxidant stress which consequently causes hepatocyte cell death. On the other hand, scientific studies have proven that MET shows hepatoprotective eff ect against hepatotoxicity induced by APAP through numerous mechanisms, e.g., antioxidant activity that alleviate the hepatotoxicity by activating Nrf2 pathway. The activation of Nrf2 pathway is anticipated to protect cells from oxidative stress that forms during hepatotoxicity. The beneficial of using MET to protect against hepatotoxicity after APAP has been performed in an in-vitro experiment using Hep2G cell culture. However, up to our knowledge non, an in-vivo study (experimental animal) has been used to approve the benefit of MET.
Justification: Nrf2 pathway activation by MET is one of the most important issues that need to be explained and followed up in laboratory animals since it has been previously studied in-vitro. Our study focuses on studying Nrf2 pathway in-vivo, since the results of in-vivo study are more relevant and similar to that of human beings.
Aim of the study: To examine the possible stimulant effect of MET on Nrf2 pathway in experimental animals and its role in protecting the liver from oxidative stress that formed during APAP-induced hepatotoxicity.
Methodology: Twenty-four wistar rats were divided randomly into four groups (six rats/Grp). Grp1; normal saline orally, Grp2; toxic dose of APAP (1000 mg/kg) orally; Grp3; 200 mg/kg of MET ip after 1-hour of APAP (1000 mg/kg) orally, Grp 4; 200 mg/kg MET ip for 24 hours. Then sera from experimental animals were collected for subsequent assessments of aspartate aminotransferase (AST) and alanine aminotransferase (ALT) enzyme activities. Liver tissue was harvested to detect the expression of keap1 which is the negative regulator of Nrf2, and HO-1 and GST A1, which are related to Nrf2 pathway, by western blotting technique.
Results: The results were showed a significant elevation in ALT and AST activities in APAP treated group while MET normalized these biomarkers (AST and ALT). Western blotting assay showed that keap1 expression increased in APAP-treated animals while MET showed a significant decrement in keap1 expression. The expression of antioxidant proteins HO-1 and GST A1 are decreased significantly in APAP-treated animals while increased significantly by MET treatment.
Conclusion: The present results demonstrated that MET has a hepatoprotective effect in experimental animals against hepatotoxicity induced by APAP through activating Nrf2 pathway.
Justification: Nrf2 pathway activation by MET is one of the most important issues that need to be explained and followed up in laboratory animals since it has been previously studied in-vitro. Our study focuses on studying Nrf2 pathway in-vivo, since the results of in-vivo study are more relevant and similar to that of human beings.
Aim of the study: To examine the possible stimulant effect of MET on Nrf2 pathway in experimental animals and its role in protecting the liver from oxidative stress that formed during APAP-induced hepatotoxicity.
Methodology: Twenty-four wistar rats were divided randomly into four groups (six rats/Grp). Grp1; normal saline orally, Grp2; toxic dose of APAP (1000 mg/kg) orally; Grp3; 200 mg/kg of MET ip after 1-hour of APAP (1000 mg/kg) orally, Grp 4; 200 mg/kg MET ip for 24 hours. Then sera from experimental animals were collected for subsequent assessments of aspartate aminotransferase (AST) and alanine aminotransferase (ALT) enzyme activities. Liver tissue was harvested to detect the expression of keap1 which is the negative regulator of Nrf2, and HO-1 and GST A1, which are related to Nrf2 pathway, by western blotting technique.
Results: The results were showed a significant elevation in ALT and AST activities in APAP treated group while MET normalized these biomarkers (AST and ALT). Western blotting assay showed that keap1 expression increased in APAP-treated animals while MET showed a significant decrement in keap1 expression. The expression of antioxidant proteins HO-1 and GST A1 are decreased significantly in APAP-treated animals while increased significantly by MET treatment.
Conclusion: The present results demonstrated that MET has a hepatoprotective effect in experimental animals against hepatotoxicity induced by APAP through activating Nrf2 pathway.
15. Effectiveness of Combined Oral and Topical Ivermectin Compared to Topical Treatments in Patients with Scabies
Zubaidah A. Al-Asadi1*, Khalil I. Al-Hamdi, Jawad H. Ahmed
Zubaidah A. Al-Asadi1*, Khalil I. Al-Hamdi, Jawad H. Ahmed
Abstract
Background: Scabies is a common parasitic skin infestation transmitted mainly through direct skin contact. Permethrin was considered the standard treatment; however, due to increasing resistance against permethrin, recent research investigates the effect of other topical preparations like ivermectin as an alternative treatment.
Aim of the study: This study aim to evaluate the efficacy and safety of ivermectin whether its topical alone or combined with oral form of ivermectin in the same time on scabietic lesions compared to permethrin. Patient and Method: 236 patients with uncomplicated scabies participated in the study. The study population was selected and divided randomly into three groups. The first group received permethrin, the second group received topical ivermectin, and the third group received a combination of topical and oral ivermectin. Each patient received two doses one week apart. The patients were followed up for the first, second, and fourth week of treatment.
Results: At the first week, the group who received the combination of treatments has a significant decrease in both severity of itching and number of lesions, the reduction percentage is (77.6, 53.9%), respectively compared to (61.8, 55.2%) with topical ivermectin and (8.3, 19%) with permethrin. At the 4th week, 15.8% of patients in the combination treatment group reported severe itching, significantly lower than the corresponding values in the other groups.
Conclusion: The combination of topical and oral ivermectin is safe and more effective than topical ivermectin or permethrin alone. It achieves a remarkable effect in the first week.
Aim of the study: This study aim to evaluate the efficacy and safety of ivermectin whether its topical alone or combined with oral form of ivermectin in the same time on scabietic lesions compared to permethrin. Patient and Method: 236 patients with uncomplicated scabies participated in the study. The study population was selected and divided randomly into three groups. The first group received permethrin, the second group received topical ivermectin, and the third group received a combination of topical and oral ivermectin. Each patient received two doses one week apart. The patients were followed up for the first, second, and fourth week of treatment.
Results: At the first week, the group who received the combination of treatments has a significant decrease in both severity of itching and number of lesions, the reduction percentage is (77.6, 53.9%), respectively compared to (61.8, 55.2%) with topical ivermectin and (8.3, 19%) with permethrin. At the 4th week, 15.8% of patients in the combination treatment group reported severe itching, significantly lower than the corresponding values in the other groups.
Conclusion: The combination of topical and oral ivermectin is safe and more effective than topical ivermectin or permethrin alone. It achieves a remarkable effect in the first week.
16. Extraction, Characterization and Therapeutic Evaluation of Seeds of Phaseolus vulgaris L. for Inhibition of Carbohydrate Uptake
Yogesh S. Bhide, Jitendra Y. Nehete, Rajendra S. Bhambar
Yogesh S. Bhide, Jitendra Y. Nehete, Rajendra S. Bhambar
Abstract
Phaseolamin-rich beans, also known as -amylase inhibitor 1 (AI) bean. AI has shown promise in treating diabetes and obesity in human studies. Since enzymes speed up chemical reactions, thus they are needed for most biological processes. Humans have used catalysts for centuries. Chemical catalysis was a heavy, often-used method. The method lacks sensitivity, and catalysis requires high temperature and pressure. Enzymes may function under more benign settings than chemical catalysts. Enzymes speed up chemical processes more than chemical catalysts due to their specificity. Enzymes are used in practically every industry today. Enzymes have always been crucial. Enzymes have also been used to treat digestive diseases, coagulate milk for cheese, and process starch for drinks. Amylase is becoming increasingly popular because it may break down starch in multiple ways. Amylase reactions then cover amylases and other enzymatic reactions covered in this article as a catalyst. Amylases, a kind of hydrolase enzyme, are widely used. These enzymes randomly disrupt the glycosidic connections within starch molecules, releasing dextrin and oligosaccharides. Amylase is the most versatile type of amylase. Enzymes are replacing traditional chemical catalysts as consumers become more ecologically conscious.
17. Impact of Lipid Type and Ratio in Rizatriptan Benzoate Nanostructured Lipid Carrier
Nawal A. Rajab, Mohammad S. Jawad
Nawal A. Rajab, Mohammad S. Jawad
Abstract
Nanotechnology represents a magic wand to solve most problems related to improving drug efficiency, one of the most important of these problems is the drug’s permeability through biological membranes. Rizatriptan benzoate was used for the treatment of acute migraine, it has poor permeability and is difficult to administer through the nose. This study aims to design a nanostructured lipid carrier containing rizatriptan benzoate as a trial to enhance its biological permeability. A high shear homogenization technique was utilized as a method of preparation; glyceryl monostearate and beeswax are used as solid lipids while oleic acid and castor oil were used as liquid lipids in different ratios. Particle size analysis, polydispersity index, zeta potential, entrapment efficiency, and loading efficiency were considered the main criteria for the evaluation, meanwhile, the in-vitro release test was done for the formulas having smallest particle size. Moreover, the infrared spectroscopy and differential scanning calorimetry (DSC) are investigated for the selected formula. The obtained outcome revealed a significant effect on the particle size and entrapment efficiency upon enhancing the ratio of liquid lipid. Furthermore, changing the type of solid and liquid lipid leads to a dramatic alteration in the criteria of evaluation, also biphasic release pattern was seen. The infrared spectroscopy shows an intact rizatriptan benzoate, while DSC revealed a change of drug molecule to an amorphous state. In conclusion, a high shear homogenization can be used to formulate a successful nanostructured lipid carrier with good physical properties.
18. Preparation and Evaluation of Rizatriptan Benzoate Loaded Nanostructured Lipid Carrier Using Different Surfactant/Co-Surfactant Systems
Nawal A. Rajab, Mohammad S. Jawad
Nawal A. Rajab, Mohammad S. Jawad
Abstract
Migraine is the second most common neurological illness, affecting around one billion people each year; triptans are commonly used in the treatment; rizatriptan benzoate is a member of the triptan class, it’s available as a tablet dosage form. Unfortunately, it undergoes first-pass effect after oral intake. The intranasal route of administration represents a solve to such a problem. Because it has a limited permeability, an effort has been made to circumvent this hurdle. Nanotechnology’s innovation has offered a useful answer to several issues in the pharmaceutical field in which it could improve drug permeability. The aim of the present work involved loading rizatriptan benzoate on a nanostructured lipid carrier as an attempt to resolve adversity affiliated with the intended drug. The high-speed homogenization technique prepares six formulas. The formulations’ particle size, polydispersity index, zeta potential, entrapment efficiency, loading capacity, and in-vitro drug release were studied. Differential scanning calorimetry (DSC), Fourier transforms infrared spectroscopy (FTIR), and powder X-ray diffraction (PXRD) was investigated to exclude drug excipient incompatibility and to evaluate the crystallinity state of rizatriptan benzoate before and after formulation. Successful formulations were obtained with an acceptable nanostructured parameter in-vitro drug release profile illustrates a biphasic pattern in which an immediate followed by a persistent phase over a 6 hours. release period, with an estimated percent of the medication being released with an anomalous release mechanism. The compatibility and crystallinity investigation revealed that rizatriptan benzoate was compatible with the other excipients used in the research, and the drug molecule was found to be in an amorphous state within the lipid matrix. In conclusion, nanostructured lipid carriers might be a potential delivery approach for improving intranasal administration of rizatriptan benzoate.
19. The Effect of NSAIDS and Oral Hypoglycemic Agent on Leukemia and Lymphoma Cell Lines
Khaleed J. Khaleel, Abeer A. Ahmed, Maeda H. Mohammad, Alaa A. Fadhe
Khaleed J. Khaleel, Abeer A. Ahmed, Maeda H. Mohammad, Alaa A. Fadhe
Abstract
Cancer is regarded as global burden and a serious health challenge. Its occurrences increased due to population aging and the prevalence of risk factors. This study investigated the effect of metformin and aspirin on two cell lines SR (diffuse large B cell lymphoma) and NB4 (promyelocytic leukemia). The effect of metformin as monotherapy on SR was 28.43% viable, while on NB4, only 44.4% were viable. However, the effect of aspirin on SR and NB4 cell lines were decreased; the percentage of cell viability were 27.2 and 41.2%, respectively. In conclusion, there is significant effect of metformin and aspirin on SR cell line and only mild effect on NB4. These may be useful drugs in old diabetic patients with diffuse large B cell lymphoma that may reduce the chemotherapy dose.
20. The Probable Association between Type 2 Diabetes Mellitus and Toxoplasma gondii Infection
Omar D. Salman, Maysoon A. Z. Merdaw, Ahmed A. Almaliky
Omar D. Salman, Maysoon A. Z. Merdaw, Ahmed A. Almaliky
Abstract
Background: Type 2 diabetes mellitus (T2DM) is a chronic disorder that constitutes a major health problem worldwide. Toxoplasma gondii is an intracellular parasite that may infect any nucleated cell. Toxoplasmosis is becoming a worldwide health threat, infecting 30–50% of the world’s human population. The studies that have been undertaken to investigate the link between T. gondii infection and diabetes have shown contradictory findings. This research aimed to look at the possible link between T2DM and T. gondii infection.
Methods and Subjects: The enzyme-linked immunosorbent assay (ELISA) approach was used to screen for T. gondii IgM and IgG antibodies in 69 patients with T2DM and 92 seemingly healthy persons as controls.
Results: The results demonstrate that all participants were IgM negative, the percentage of T. gondii latent infection was (52.1%) among patients with T2DM and (31.5%) among non-diabetic individuals. The frequency of infection differs significantly between diabetic and non-diabetic people. T. gondii infection was not linked to the studied risk factors.
Conclusion: There is serological evidence of a link between T2D and T. gondii infection. Furthermore, Toxoplasmosis is a risk factor for type 2 diabetes.
Methods and Subjects: The enzyme-linked immunosorbent assay (ELISA) approach was used to screen for T. gondii IgM and IgG antibodies in 69 patients with T2DM and 92 seemingly healthy persons as controls.
Results: The results demonstrate that all participants were IgM negative, the percentage of T. gondii latent infection was (52.1%) among patients with T2DM and (31.5%) among non-diabetic individuals. The frequency of infection differs significantly between diabetic and non-diabetic people. T. gondii infection was not linked to the studied risk factors.
Conclusion: There is serological evidence of a link between T2D and T. gondii infection. Furthermore, Toxoplasmosis is a risk factor for type 2 diabetes.
21. Development of the Formulation and Evaluation of the Anti-arthritic Activity of Vitex negundo Gel and Latex
Jeevan R. Rajguru, Mrunal K. Shirsat, Sampat D. Navale
Jeevan R. Rajguru, Mrunal K. Shirsat, Sampat D. Navale
Abstract
The important oil is Vitex negundo Linn. It is used in the treatment of eye diseases, toothache, inflammation, leukoplakia, splenomegaly, skin ulcers, catarrh, rheumatoid arthritis, gonorrhea and bronchitis. It is also used as a tonic, insect repellent, galactagogue, menstrual agent, antibacterial, antipyretic and antihistamine. The plant component arrangements of V. negundo, are used commercially in a variety of Ayurvedic medicines and ointments for the treatment of a variety of ailments including rheumatism, arthritis, gout, cervical spondylitis, inflammatory musculoskeletal, hemorrhoids (hemorrhoids), painful wounds, painful wounds. wounds, painful sores, burns and fungal infections of the skin.
From the in-vitro diffusion of drugs, we concluded that Emulgel composed of HPMC polymers can control drug secretion for a long time, which helps to prevent more fluctuation and also reduces the cost of treatment. Due to the advantages of latex for improved spreadability, adhesion, viscosity, and extrudability, this new type of drug delivery is gaining popularity, besides systemic action, the local topical utility of hydrophobic dispensers is also of interest.
From the in-vitro diffusion of drugs, we concluded that Emulgel composed of HPMC polymers can control drug secretion for a long time, which helps to prevent more fluctuation and also reduces the cost of treatment. Due to the advantages of latex for improved spreadability, adhesion, viscosity, and extrudability, this new type of drug delivery is gaining popularity, besides systemic action, the local topical utility of hydrophobic dispensers is also of interest.
22. The Protective Effect of Cinnamic Acid against Ulcerative Colitis in Mice
Maysam A. Hussein, Munaf H. Abdulrazzaq
Maysam A. Hussein, Munaf H. Abdulrazzaq
Abstract
Objective: To study the protective effects of cinnamic acid on dextran sodium sulfate (DSS) induced ulcerative colitis (UC) in mice.
Materials and Methods: Forty adult male mice were randomly divided into five groups, control group, an induction group received 3% DSS in drinking water for 7 consecutive days. Two treatment groups received oral suspension of cinnamic acid 50 and 25 mg/kg, respectively and 3% DSS in drinking water, for 7 consecutive days. The final group received oral suspension of cinnamic acid 50 mg/kg for the latter 7 days without DSS in drinking water. All the animals were euthanized on day eight. The colon of animals was extracted and divided into two sections, the middle was homogenized and biochemically analyzed using the mean levels of total superoxide dismutase (SOD), and malondialdehyde, catalase, the distal for histopathological examination.
Results: Total SOD, malondialdehyde, and catalase show significant results in the model group when compared to the control group. DSS with cinnamic acid 50 mg/kg group and DSS with cinnamic acid 25 mg/kg revealed a significant (p < 0.05) increase in total SOD and MDA and significant reduction in catalase when compared to the model group. Histopathological examination showed a significant reduction of inflammatory signs in all cinnamic acid-treated groups compared to the DSS model group.
Conclusion: The treatment with cinnamic acid significantly decreased the levels of DSS-associated oxidative stress. This finding supports the idea that the use of this substance could be used as a potential therapy for patients with ulcerative colitis.
Materials and Methods: Forty adult male mice were randomly divided into five groups, control group, an induction group received 3% DSS in drinking water for 7 consecutive days. Two treatment groups received oral suspension of cinnamic acid 50 and 25 mg/kg, respectively and 3% DSS in drinking water, for 7 consecutive days. The final group received oral suspension of cinnamic acid 50 mg/kg for the latter 7 days without DSS in drinking water. All the animals were euthanized on day eight. The colon of animals was extracted and divided into two sections, the middle was homogenized and biochemically analyzed using the mean levels of total superoxide dismutase (SOD), and malondialdehyde, catalase, the distal for histopathological examination.
Results: Total SOD, malondialdehyde, and catalase show significant results in the model group when compared to the control group. DSS with cinnamic acid 50 mg/kg group and DSS with cinnamic acid 25 mg/kg revealed a significant (p < 0.05) increase in total SOD and MDA and significant reduction in catalase when compared to the model group. Histopathological examination showed a significant reduction of inflammatory signs in all cinnamic acid-treated groups compared to the DSS model group.
Conclusion: The treatment with cinnamic acid significantly decreased the levels of DSS-associated oxidative stress. This finding supports the idea that the use of this substance could be used as a potential therapy for patients with ulcerative colitis.
23. Study of Antibiotic-resistant Bacteria Isolated from Children with Urinary Tract Infection
Abbas H. S. Al-Wandawy, Luma A. Zwain, Murad R. Wali
Abbas H. S. Al-Wandawy, Luma A. Zwain, Murad R. Wali
Abstract
Urine samples 96 to 100 were collected from patients (children) with urinary tract infections (UTIs) from Azadi Hospital in Kirkuk province, Iraq, where included (76 males and 120 females) with ages ranging from (≥ one-15) years old, for period from 1/1/2022 to 26/4/2022. The study included isolation and identification depending on macroscopic, microscopic and definite with API 20e and API Staphylococcus. Moreover, all isolates were tested for resistance to 23 antibiotics. 55 bacterial isolations were obtained and E. coli had the highest rate of 27 (49.09%) followed by Klebsiella spp. with 14 (25.45%) and each of the bacteria, Staphylococcus aureus, Proteus spp., Citrobacter spp., Enterobacter spp., Pseudomonas spp. and Morganella morganii they reached 4(7.27%), 5(9.09%), 1(1.81%), 2 (3.63%), 1(1.81%) and 1(1.81%), respectively. Result showed Enterobacteriaceae higher resistance to amoxicillin-clavulanate (100%). E. coli had the highest rate and were resistance 100% to tobramycin, penicillin and amoicillin, followed by amoxicillin-clavulanate and ampicillin (96.29 and 91.66), respectively. At the same time (Doxycycline, Ceftazidime, Tetracycline, Cefepime, Trimethoprim, Cefotaxime) were (88.88, 88, 85.71, 84, 83.33, 81.81%), respectively. At the same time, Pseudomonas spp. were resistant to (Ampicillin, Cefotaxime, Morganella morgani, and Erythromycin) 100% and S. aureus were resistant to (Amoxicillin-clavulanate, Cefotetan, Cefepime, Erythromycin, Norfloxacin, Tetracycline, Cefotaxime, Morganella morgani, Amikacin) 100%.
24. Formulation and Characterization of Raloxifene loaded Biodegradable Polymeric Nanomicelles
Pooja Dave, Chetan Detroja
Pooja Dave, Chetan Detroja
Abstract
Raloxifene has been used to treat breast cancer; nevertheless, it has poor water solubility and a low bioavailability fraction because higher first-pass metabolism hinders its application raloxifene nano micelles by using PLGA50:50 to enhance solubility and bioavailability. The solvent evaporation technique was used to prepare polymeric nano-micelles. Ral-loaded polymeric micelles had a zeta potential of – 0.71 mV, implying a practically neutral surface charge. Blank micelles and RAL-loaded micelles had similar average sizes of 84.29 nm and 95.41 nm, respectively. The drug encapsulating and drug loading capacity was found to be 16.08 ± 0.34% and drug loading 5.04 ± 0.002% (w/w), respectively. An in-vitro study illustrates a 95.10% sustained release drug profile for 120 hours.
25. Retracted by Authors
26. Controlled Release Levetiracetam Loaded Eudragits Microspheres for Oral Drug Delivery: Preparation and Evaluation
Arshed A. Khalid, Wedad K. Ali
Arshed A. Khalid, Wedad K. Ali
Abstract
This work aims to prepare controlled release microspheres loaded with levetiracetam (LEV) for oral use that will have a targeted release site, thus reducing dose frequency and improving patient compliance. Levetiracetam is a 2nd generation anti-epileptic medication with a T/half-life of 7 hours that is administered twice daily, which makes it suitable for formulation that will reduce dosing intake. The microspheres were prepared by solvent evaporation method using Eudragit E100, L100, and S100 polymers as matrix core polymers at different ratios 1:1, 1:2 and 1:3 with levetiracetam. These polymers have different pH sensitivity profiles, which will aid the release of levetiracetam in a controlled manner along the gastrointestinal tract. The prepared microspheres were evaluated for yield percentage, entrapment efficiency (EE%), morphological characteristics and in-vitro release profile. The yield percentage and EE% for the formulation at different ratios ranged from 69–99%. The in-vitro release analysis showed favorable targeted release of the drug at specific pH ranges matching specific sites in the gastrointestinal tract.
27. A Comparative Study of Concentration of Growth Factors in Lyophilized PRP with Fresh PRP at Different Storage Conditions
Pooja U. Vyas, Deepak S. Khobragade, Dharmendra R. Mundhada, Sandeep P. Shrivastava, Ujwal B. Vyas, Anil M. Pethe
Pooja U. Vyas, Deepak S. Khobragade, Dharmendra R. Mundhada, Sandeep P. Shrivastava, Ujwal B. Vyas, Anil M. Pethe
Abstract
Background: There is ongoing debate regarding platelet-rich plasma’s (PRP) ability to effectively heal soft tissue injuries. Lyophilized platelet-rich plasma (L-PRP) was created and kept using the blood bank’s standard separation procedures. The objective of study was to evaluate effects of lyophilization on PRP and its properties such as level of growth factors. Also, the effect of storage conditions on growth factors.
Methods: The PRPs were created through a two-step centrifugation process and lyophilized. After freeze-thawing to allow platelet growth factors to be released, levels of hepatocyte growth factor (HGF), transforming growth factor (TGF), fibroblast growth factor (FGF)-basic, platelet-derived growth factor (PDGF)-AB, insulin-like growth factor (IGF)-1, and vascular endothelial growth factor (VEGF) were measured each day during storage.
Results: After L-PRP preparation, levels of FGF-basic, VEGF, PDGF-AB, EGF and TGF- beta1 significantly raised and levels of HGF and IGF-1 in L-PRPs had light rise.
Conclusions: In comparison to F-PRP, platelet counts and seven growth factors increased during preservation in L-PRP. PRPs that have been stored may be injected several times using our method. L-PRP was efficacious and stable for 90 days when stored at 8℃.
Methods: The PRPs were created through a two-step centrifugation process and lyophilized. After freeze-thawing to allow platelet growth factors to be released, levels of hepatocyte growth factor (HGF), transforming growth factor (TGF), fibroblast growth factor (FGF)-basic, platelet-derived growth factor (PDGF)-AB, insulin-like growth factor (IGF)-1, and vascular endothelial growth factor (VEGF) were measured each day during storage.
Results: After L-PRP preparation, levels of FGF-basic, VEGF, PDGF-AB, EGF and TGF- beta1 significantly raised and levels of HGF and IGF-1 in L-PRPs had light rise.
Conclusions: In comparison to F-PRP, platelet counts and seven growth factors increased during preservation in L-PRP. PRPs that have been stored may be injected several times using our method. L-PRP was efficacious and stable for 90 days when stored at 8℃.
28. Phytochemical Investigation and Pharmacological Activity of Solidago canadensis L. against H1N1 Virus, involving the Separation and Identification of Three New Compounds
Hayder T. Hasan, Enas J. Kadhim
Hayder T. Hasan, Enas J. Kadhim
Abstract
Solidago canadensis L. (S. canadensis) is a member of the Asteraceae family, which comprises over a 100 species. The aerial portion of S. canadensis was defatted by maceration in hexane for 24 hours; the defatted plant components were extracted for 24 hours using a soxhlet apparatus and aqueous ethanol 85%, and then fractionated by different solvents. The ethyl acetate, and chloroform fractions were examined using liquid chromatography-mass spectroscopy (LC-MS). The examination revealed the presence of several phenolics, coumarins, and flavonoid compounds. Preparative high-performance liquid chromatography (PHPLC) was utilized to isolate several compounds. Eugenol-o-glucoside, 2-hydroxy-4,5-dimethoxy-9,10-dihydrophenanthrene, and 2,5-dihydroxy-4-methoxy-9,10-dihydrophenanthrene (Hircinol) have been isolated and identified in the plant for the first time. High-throughput cytopathic effect (CPE) inhibitory tests for the H1N1 virus on vero cells were developed to investigate new potential antiviral agents. A crystal violet uptake assay was used to measure the cytotoxic and antiviral effects. The polyphenols in the ethyl acetate fraction showed high antiviral activities against H1N1 with a selective index (SI) = estimated CC50/estimated IC50 = 23.6. Consequently, the tested samples are good Candidates for further experiments as anti-influenza H1N1.
29. Preparation and Evaluation of Ophthalmic Ketorolac Tromethamine Minitablet
Nidhal K. Maraie, Wid F. Neamah
Nidhal K. Maraie, Wid F. Neamah
Abstract
Objective: The current research is for improving patient compliance by reducing dosing frequency of ocular ketorolac tromethamine used for allergic conjunctivitis through preparation of minitablet for ocular insertion.
Method: Ocular mini tablet was prepared by direct compression method using xanthan gum, chitosan and carbopol 943P as polymers to prepare the mini tablet for ocular insertion. The mini tablets were evaluated for drug content, weight variation, bioadhesion, water uptake and swelling behavior, in-vitro drug release and ocular irritation.
Results: The best formula (F1) containing 1% chitosan gave mini tablets with dimension (3 × 0.7 mm) with satisfactory physical properties and 100% release after 12 hours to be inserted anteriorly.
Conclusion: This work succeeded in preparing ocular mini tablet of ketorolac tromethamine to be inserted anteriorly for the treatment of allergic conjunctivitis. As promising sustained release drug delivery system to be a good alternative for the conventional treatment regimen to improve patient compliance by reducing frequent doses with no irritation.
Method: Ocular mini tablet was prepared by direct compression method using xanthan gum, chitosan and carbopol 943P as polymers to prepare the mini tablet for ocular insertion. The mini tablets were evaluated for drug content, weight variation, bioadhesion, water uptake and swelling behavior, in-vitro drug release and ocular irritation.
Results: The best formula (F1) containing 1% chitosan gave mini tablets with dimension (3 × 0.7 mm) with satisfactory physical properties and 100% release after 12 hours to be inserted anteriorly.
Conclusion: This work succeeded in preparing ocular mini tablet of ketorolac tromethamine to be inserted anteriorly for the treatment of allergic conjunctivitis. As promising sustained release drug delivery system to be a good alternative for the conventional treatment regimen to improve patient compliance by reducing frequent doses with no irritation.
30. Determination and Isolation of Valuable Bioactive Compound (lupeol) from Portulacaria afra Jacq.
Ali H. H. AL-temimi, Enas J. Kadhum
Ali H. H. AL-temimi, Enas J. Kadhum
Abstract
Portulacaria afra is a small succulent tree, previously belonging to the Portulacaceae family, but with further studies, the plant transferred to the Didieracea family. P. afra was used as an ornamental, vegetable, and ethnomedicinal plant. Uses of the plant by rural South Africans to treat chronic skin conditions and rashes, alleviate exhaustion, and aid in treating TB and diarrhea have been documented in folklore. According to pharmaceutical research, plant extracts offer a wide range of remedial outcomes, such as antidiabetic, antifungal, antibacterial, anticancer, antioxidant, and anti-inflammatory. The study aims to determine some bioactive constituents responsible for pharmacological activities and traditional usefulness. Thin-layer chromatography (TLC) is used for detecting lupeol by specific reagents; a p-anisaldehyde sulfuric acid reagent and 10% methanolic sulfuric acid. And high-performance liquid chromatography was used to detect pentacyclic triterpenoids (lupeol) in the n-hexane. The lupeol was isolated by preparative layer chromatography (PLC). Testing the efficacy of the separation method, the isolated compounds have been identified and characterized by different chromatographic and chemical analyses (TLC, ATR-FTIR, LC-CMS-APCI+, and 1H-NMR).
31. Synthesis, Characterization and Studying Biological Activity of Heterocyclic Compounds
Rana N. Atiya, Zahraa L. Razzaq, Widad I. Yahya, Helen M. Neamah
Rana N. Atiya, Zahraa L. Razzaq, Widad I. Yahya, Helen M. Neamah
Abstract
Heterocyclic moiety was mentioned to present diverse biological activities such as inhibitors of protein glycation, antibacterial, antifungal, anticancer, antidepressant, anti-inflammatory, antituberculosis, antioxidant, and as antiviral agents, in addition to other biological activities; therefore, many medicines containing heterocyclic moiety have been observed. Due to the pharmacological importance of heterocyclic derivatives, the present work comes as attempt to synthesis of heterocyclic compound involved (tetrazole and pyrazole rings) by series of steps starting from pyrimidin-2-amine, which reacted with 2-chloroacetyl chloride gave compound (1) [2-chloro-N-(pyrimidin-2-yl) acetamide], then the reflex reaction of the compound (1) with the hydrazine hydrate in ethanol led to compound (2) [2-hydrazinyl-N-(pyrimidin-2-yl)acetamide], the last one reacted with acetyl acetone to form pyrazole ring compound (3) [2-(3,5-dimethyl-1H-pyrazol-1-yl)-N-(pyrimidin-2-yl)acetamide]. In other line another pyrazole derivative was prepared by diazotization of pyrimidin-2-amine with NaNO2/HCl to azo derivative compound (4), which is reacted with acetyl acetone gave compound (5) [3-(2-(pyrimidin-2-yl) hydrazono) pentane-2,4-dione] to react with hydrazine gave pyrazole moiety compound (6) [(2-((1H-pyrazol-4-yl) diazenyl) pyrimidine]. Pyrimidin-2-amine was reacted with 4-hydroxybenzaldehyde in ethanol and glacial acetic acid gave Schiff base compound (7), which reacted with sodium azide in dioxane to form tetrazole ring compound (8) [4-(1-(pyrimidin-2-yl)-4,5-dihydro-1H-tetrazol-5-yl) phenol]. The spectroscopic techniques were used to confirmed the chemical structures are FTIR, 1H-NMR. The biological study of pyrazole and tetrazole derivative was evaluated as anti-bacterial against gram-negative (Klebsiella pneumoniae), gram-positive (Enterococcus faecalis) and as anti-fungal against the Candida trichomonas and Candida dubliniensis in concentration 25, 75, 50, and 100 mg/mL. It was found that pyrazole and tetrazole derivative have biological activity against the bacteria and fungi where the tetrazole ring has biological effect more than pyrazole ring.
32. Retracted by Authors
33. Spectrophotometric Method and Its Validation for Tolvaptan in Its Bulk and Marketed Formulation Including Stress Studies
Bhavya Sri, B. Aishwarya, Sowwjanya, Anushree Hari, Narmada Vallakeerthi, Sumakanth
Bhavya Sri, B. Aishwarya, Sowwjanya, Anushree Hari, Narmada Vallakeerthi, Sumakanth
Abstract
Tolvaptan in API and formulation may now be quantified using a technique. The solution was diluted with acetonitrile and scanned in the UV area between 200 and 400 nm. At 267 nm, tolvaptan exhibits maximum absorption. The accuracy investigations had been executed at3 levels, i.e., 80, 100, and 120%, and recuperation turned into discovered to be with inside the variety of 99.4% for the tolvaptan, which showed linearity over the range of 5 to 160 g/mL with correlation co-efficient (r2) of 0.9995. The quantification (LoQ) and detection (LoD) threshold were 0.471 and 1.435 g/mL, respectively. The suggested approach underwent forced deterioration, and each parameter’s degradation was discovered. The ICH rules were followed in the validation of each parameter.
34. Effect of Different Laser Irradiation Parameters on the Viability of Bacillus Species
Reem A. Naji, Huda K. Mohseen, Russell I. AL-Daher
Reem A. Naji, Huda K. Mohseen, Russell I. AL-Daher
Abstract
The genus Bacillus is present everywhere in the environment, it has environmental, industrial, and medical significance. This heterogeneous group of bacteria shares unique characteristics, one of these is the resistance to physical and chemical agents. Laser light is one of the most interesting physical agents with a wide range of applications in all scientific fields. It has the ability to alter bacterial growth by triggering inhibitory or stimulatory mechanisms. In this study, laser parameters were varied to evaluate the effect of each one on the viability of Bacillus species. CW or chopped (532 nm) laser light at different irradiation periods were examined. Results showed that tested bacterial species’ response to green laser light varied. Bacterial viability was dropped with increasing chopping frequency and exposure time. In conclusion, high repetition rate and prolonged exposure time increase the lethal effects of this type of laser.
35. The Effect of Metformin and Biological Therapy on Insulin Resistance in Iraqi Psoriatic Patients
Ghadah Ali Al-Oudah, Mohammed K. Al-Hattab, Ahmed S. Sahib, Shaimaa M. Mohammed
Ghadah Ali Al-Oudah, Mohammed K. Al-Hattab, Ahmed S. Sahib, Shaimaa M. Mohammed
Abstract
Psoriasis refers to a medical condition involving long-term inflammation, high insulin resistance, obesity and a likelihood of cardiovascular disease.
Objective: This paper attempts to find out if the addition of metformin to biological therapy has the beneficial effect of increasing insulin sensitivity in moderate to severe Iraqi psoriatic patients.
Subjects and Methods: The experimental group comprises 24 patients suffering from moderate to severe psoriasis. They were randomly selected into two groups: group A comprises 13 psoriatic patients treated with 40 mg of adalimumab twice monthly for 12 weeks. While group B contains 11 psoriatic patients treated with 40 mg of adalimumab twice monthly and a single daily dose of 850 mg of metformin for 12 weeks. The psoriasis area and severity index (PASI), glycosylated hemoglobin (HbA1c), body mass index (BMI), as well as insulin-resistance parameters, which include fasting blood glucose (FBG) and fasting serum insulin (FSI) are estimated for each patient before and after completion of therapy.
Results: The two groups showed a significant reduction in insulin resistance. Nonetheless, group B showed greater reduction. Furthermore, the PASI score of the two groups exhibited improvement, but group B exhibited a higher percentage improvement than group A, and the difference was significant (p < 0.05).
Conclusion: This study demonstrates that adding a single daily dose of 850 mg of metformin has a more beneficial effect on insulin resistance (IR) in psoriasis patients than using only biological therapy.
Objective: This paper attempts to find out if the addition of metformin to biological therapy has the beneficial effect of increasing insulin sensitivity in moderate to severe Iraqi psoriatic patients.
Subjects and Methods: The experimental group comprises 24 patients suffering from moderate to severe psoriasis. They were randomly selected into two groups: group A comprises 13 psoriatic patients treated with 40 mg of adalimumab twice monthly for 12 weeks. While group B contains 11 psoriatic patients treated with 40 mg of adalimumab twice monthly and a single daily dose of 850 mg of metformin for 12 weeks. The psoriasis area and severity index (PASI), glycosylated hemoglobin (HbA1c), body mass index (BMI), as well as insulin-resistance parameters, which include fasting blood glucose (FBG) and fasting serum insulin (FSI) are estimated for each patient before and after completion of therapy.
Results: The two groups showed a significant reduction in insulin resistance. Nonetheless, group B showed greater reduction. Furthermore, the PASI score of the two groups exhibited improvement, but group B exhibited a higher percentage improvement than group A, and the difference was significant (p < 0.05).
Conclusion: This study demonstrates that adding a single daily dose of 850 mg of metformin has a more beneficial effect on insulin resistance (IR) in psoriasis patients than using only biological therapy.
36. Pharmacological Evaluation of Alcoholic Extract of Clitoria ternatea Root for Anxiolytic and Anticonvulsant Activity
N V L S. Reddy V, M. G. Raju, M. Niharika, B. Pratyusha, Mahesh Thorat, Harshal Tare
N V L S. Reddy V, M. G. Raju, M. Niharika, B. Pratyusha, Mahesh Thorat, Harshal Tare
Abstract
Recent scientific studies have indicated that some of the same medicinal herbs used in traditional medicine to treat epilepsy may also have anticonvulsant qualities, suggesting that they may be a possible source of novel anticonvulsants. Anticonvulsant properties have been studied in animal models. Clitoria ternatea Linn’s ethanolic root extract was examined for antiepileptic, anxiolytic, and phytochemical properties. Phenytoin 25 mg/kg, as a reference medicine, the extract was tested against strychnine-induced convulsion in rats at oral doses of 200 and 400 mg/kg. The elevated plus maze and staircase test were used to examine mice’s anxiolytic activity with lorazepam (the gold standard) at 0.05 mg/kg. When using a strychnine-induced convulsion model, the ethanolic extract markedly accelerated the start of convulsions. In the elevated plus maze test, C. ternatea Linn ethanolic root extract at 200, 400, and standard doses significantly increased the time and number of the entry in open arms compared to the control group. In a staircase test, the ethanolic root extract of C. ternatea increased the number of steps climbed and lowered rearing compared to the control group. Docking scores in mcule software indicate that interactions with the glycine agonist (PDB: 5I57) and the GABA agonist (PDB: 4MS3) receptors for epilepsy and anxiety, respectively, are highly effective. Evidence for the biochemical evaluation of GABA, anticonvulsant, and anxiolytic action, as well as in-silico activities, of the ethanolic extract of Clitoria ternatea was reported in this work.
37. The Effectiveness of Salvadora persica Extracted Miswak and ZnO NPs on Pathogenic Bacteria
Muntaha R. Ibraheem
Muntaha R. Ibraheem
Abstract
Salvadora persica, (Miswak) deem oral hygiene essential biological and chemical activities. The current study aimed to study the biological activity of S. persica of extract using Fourier transform infrared spectroscopy (FTIR) show that contains analysis of the FTIR test results of miswak extract. While the analysis using UV-vis displays that the extract contains analysis of UV-vis test for miswak extract. The extract shows higher activity against bacteria than fungi. The inhibition zone of Escherichia coli, Staphylococcus aureus, and the ZnO nanoparticles show high biological activity against (bacteria and fungi). The chewing stick which is commonly known as the Miswak tree and its scientific name is S. persica L, occurs in most of the countries of Asia and Africa. The plant has long been prized in the Middle East for its vital biological and chemical properties and its usage in mouth hygiene, as mentioned in ethnobotanical records. This research aims to summarize this species’ biological effects (antibacterial and antifungal) by testing the effect of different concentrations of extracted Miswak (aqueous extracts) in E. coli as gram-negative in addition to use different measurement devices, FTIR, UV-vis spectroscopy, and gas chromatography (GC) to analyze the extracted Miswak. We found that S. persica has beneficial therapeutic effects and has the potential to be used as a useful adapt genic herbal treatment based on its chemical and pharmacological characteristics.
38. The Protective Effects Trimetazidine on Indomethacin Induced Gastric Ulcer in Rat Model
Redhaa Imad, Huda I. Al-Qadh
Redhaa Imad, Huda I. Al-Qadh
Abstract
Introduction: Gastric ulcer (GU) is the most common gastrointestinal tract disorder, representing about 20% of peptic ulcer due to an imbalance between gastric defense mechanisms and aggressive factors, mainly Helicobacter pylori and non-steroidal anti-inflammatory drugs (NSAIDs). The study aims to evaluate trimetazidine’s protective effect on histopathology, GU severity, inflammatory and oxidative stress markers (TNF- alpha, MPO and MDA) in rate model of indomethacin induced GU.
Method: Total 30 healthy male albino rats were divided into five groups each of ten (N=10). Group A: Given indomethacin vehicles (normal saline 0.9% and tween 80) orally via gavage tube and serve as control positive group. Group B: Induced ulcer by Indomethacin 60 mg/kg orally via oral gavage serve as control negative. Group C: Pretreated with trimetazidine 50 mg/kg orally by gavage tube 1-hour before administering indomethacin 60 mg/kg. At the end of study histological examination, anti-inflammatory and antioxidant markers were evaluated.
Results: TMZ 50 mg/kg pretreated groups show a significant (p < 0.01) reduction in GU severity score and histopathology damage score in comparison with the indomethacin ulcerated group. Moreover, pretreated groups TMZ 50 mg/kg showed a significant reduction in inflammatory markers (TNF-alpha and MPO) and oxidative stress marker (MDA) in comparison with the induction group, similar to the results of the reference drug.
Conclusion: TMZ dihydrochloride has similar efficacy as standard omeprazole drug by a decrease in oxidative stress status manifested by a reduction in lipid peroxidation indicator marker and a reduction in pro-inflammatory cytokine level and leukocyte recruitment indicator marker and finally, macroscopic and microscopic evaluation show a reduction GU severity.
Method: Total 30 healthy male albino rats were divided into five groups each of ten (N=10). Group A: Given indomethacin vehicles (normal saline 0.9% and tween 80) orally via gavage tube and serve as control positive group. Group B: Induced ulcer by Indomethacin 60 mg/kg orally via oral gavage serve as control negative. Group C: Pretreated with trimetazidine 50 mg/kg orally by gavage tube 1-hour before administering indomethacin 60 mg/kg. At the end of study histological examination, anti-inflammatory and antioxidant markers were evaluated.
Results: TMZ 50 mg/kg pretreated groups show a significant (p < 0.01) reduction in GU severity score and histopathology damage score in comparison with the indomethacin ulcerated group. Moreover, pretreated groups TMZ 50 mg/kg showed a significant reduction in inflammatory markers (TNF-alpha and MPO) and oxidative stress marker (MDA) in comparison with the induction group, similar to the results of the reference drug.
Conclusion: TMZ dihydrochloride has similar efficacy as standard omeprazole drug by a decrease in oxidative stress status manifested by a reduction in lipid peroxidation indicator marker and a reduction in pro-inflammatory cytokine level and leukocyte recruitment indicator marker and finally, macroscopic and microscopic evaluation show a reduction GU severity.
39. The Efficiency of Purified Pyocyanin from Pseudomonas aeruginosa in Disruption of Biofilm Formation by Candida albicans Causing Oral Candidiasis
Mohammad J. Al-Jassani, Noor A. Al-lamy, Ahmed A. Amir, Rouaida K. A. Al-hussein
Mohammad J. Al-Jassani, Noor A. Al-lamy, Ahmed A. Amir, Rouaida K. A. Al-hussein
Abstract
Candida albicans is the most usually isolated species in invasive oral candidiasis, which is a major health concern in underdeveloped nations. So pyocyanin was screened in Pseudomonas aeruginosa and found that the highest level of productivity in King A medium appeared compared with cetrimide agar, also, the productivity was increased in presence of sweet potato in comparison with soyabean. The pyocyanin was purified with silica gel chromatography as a single peak with high purity. C. albicans causing oral candidiasis is considered a stronger producer of biofilms. The effect of pyocyanin on Candida biofilm formation was inhibited with increasing incubation concentration and with increasing incubation period and the percentage of biofilm inhibition reached 73–87% after 72 hours.
40. Electrochemistry Study of Few Ru(II) and Zn(II)-Thione and Selone Complexes
Mohammed A. Abbas, Drew J. Reynolds, Julia L. Brumaghim
Mohammed A. Abbas, Drew J. Reynolds, Julia L. Brumaghim
Abstract
Hydrogen peroxide, as a byproduct of cellular respiration through incomplete reduction of oxygen yields deleterious free radicals through the Fenton reaction with iron (II/III) and Cu(I/II). Metals, such as ruthenium and zinc, are also capable of like- Fenton reaction and the production of the hydroxide radical responsible for oxidative DNA damage. This damage manifests itself through single-strand breaks in the DNA backbone corresponding to mutation and apoptosis of cells. Thus, recent research has focused on preventing this reaction through organometallic antioxidative methods. Sulfur and selenium antioxidant compounds like dmit, dmise, and methimazole coordinate to iron and other Fenton-like metal centers. Based on the electrochemistry study, the result of cyclic voltammetry can predict whether or not these metals compounds generate hydroxyl radicals when they meet hydrogen peroxide in body by figuring out their redox potentials. In this study, the electrochemical effects of these thione/selone ligands are determined through cyclic voltammetry with differing metal centers. Zinc complex redox activity was found to vary negligibly in changing solvent as well as scan speeds. In addition, ruthenium complexes from solvato complex precursors, their electrochemical peaks analyzed to prepare for reaction with hydrogen peroxide.
41. Evaluation of the Effectiveness of the Copper (II) Complex with a New Ligand derived from Benzothiazole and Anthranilic Acid as Anticancer and Antioxidant
Maysson H. Ali, Hayder O. Jamel
Maysson H. Ali, Hayder O. Jamel
Abstract
Four steps were used to convert 2-mercaptobenzothiazole into the new ligand (2-((2-((4-(1-((4’-(benzothiazol-2-ylamino)-[1,1’-biphenyl]-4-yl)imino) ethyl) phenyl)imino)-1,2diphenylethylidene) amino)benzoic acid (LH) type of schiff bases: The first step included preparing compound (A) N-(benzothiazol-2-yl)-[1, 1’-biphenyl]-4, 4’-diamine by the reaction 2-mercapto-benzothiazole with benzidine. The second step was prepared the compound(B) 2 OXO-1, 2-diphenylethylidene) amino) benzoic -((2- acid by the reacting anthranilic acid with benzil As for the third step, it included the reaction of the product of the firest step with 4-aminoacitophenon and the formation compound (C). The fourth step was the preparation ligand (LH) by reacting compound(B) with compound (C). Fourier-transform infrared spectroscopy (FTIR), proton nuclear magnetic resonance (1H-NMR), UV-vis, melting points, molar conductivity, CHN, atomic absorption, magnetic sensitivity, and other measurements were used to determine the structure of the ligand (LH) and its complex with copper (II). The MTT method was used to evaluate the activity of the ligand (LH) and its complex with copper (II) in-vitro as an anticancer (human breast cancer (MCF7). Nd (MTT) assay was used to evaluate the ligand schiff base in-vitro anticancer activity of a Cu(II) complex against human breast cancer MCF7.
42. Bioactive Secondary Metabolites Extracted from Some Species of Candida Isolated from Women Infected with Vulvovaginal Candidiasis
Khutam J. Hassan, Ali A. Kasim
Khutam J. Hassan, Ali A. Kasim
Abstract
Candida spp. are well known for their impact on our life as opportunistic pathogens and can produce secondary metabolites, which are an interesting source of high-value chemicals and are often difficult to synthesize chemically. Some of these metabolites are already being used as active antimicrobials or pharmaceuticals. GC-MS analysis of chemical compounds was conducted in ethyl acetate of five Candida species (C. parapsilosis, C. albicans, C. krusei, C. glabrata and C. kefyr). The results showed that about 249 chemical compounds were detected from all tested Candida species. Fifteen bioactive compounds identified in secondary metabolites of all tested species. Benzene, pentamethyl, n-hexadecanoic acid, 1-docosene and bis(2-ethylhexyl) produced by C. parapsilosis, C. albicans, C. krusei and C. glabrata. All tested Candida except C. krusei produced 3buten-1-ol and ethyl acetoacetate ethylene acetal. Benzen, 2-ethenyl-1,3-dimethyl- a compound found in four tested Candida except C. albicans, benezene, (1-ethyl-1-propenyl)- produced by all species except C. glabrata, acetic acid, cyclohexyl ester produced by C. parapsilosis, C. albicans and C. glabrata.
43. Factors Affecting Foam Stability of Clotrimazole Vaginal Foam
Jumana M. Falhi, Hanan J. Kassab
Jumana M. Falhi, Hanan J. Kassab
Abstract
Clotrimazole (CLT) is a broad-spectrum antifungal, synthetic imidazole derivative, used for Candida albicans the major cause of vaginitis. Vulvovaginal candidiasis (VVC) symptoms can cause discomfort and lower a women’s quality of life. Foams are used to apply formulation without the use of fingertips, the more stable the foam the better for coverage of larger surface area. CLT 2% vaginal foam were prepared as an O/W emulsion using Tween 20 and Span 20, lemon oil, PEG 400, SLS, cetyl alcohol, and the formulas were evaluated for foamability and foam stability, foam density, cycles of freezing and thawing, heating, and cooling, and the impact of the chosen formula on Candida culture are all taken into consideration.
The results showed that the CLT prepared successfully as vaginal foam, and the selected formula (F24) considered as the best formula which has good miscibility, texture and acceptable homogeneity, pH (4.8), drug content (97.5%), acceptable foamability and foam stability; foam expansion FE (70%), foam liquid stability (FLS) (40%), foam volume stability FVS (23.5%), gas fraction (GF) (35 mL), acceptable foam density (0.90), good stability at temperature changes, freeze–thaw cycle (pass), heating–cooling cycle (pass) with no phase separation, fast complete drug release (100% in about 40 min), no interaction between the solid components of the formula and acceptable inhibition zone against Candida strains.
Finally, we can conclude that formulation of CLT as vaginal foam is an optimum method to improve patients’ compliance and cure the disease with low recurrence possibility due to fast release and long contact time with the affected area.
The results showed that the CLT prepared successfully as vaginal foam, and the selected formula (F24) considered as the best formula which has good miscibility, texture and acceptable homogeneity, pH (4.8), drug content (97.5%), acceptable foamability and foam stability; foam expansion FE (70%), foam liquid stability (FLS) (40%), foam volume stability FVS (23.5%), gas fraction (GF) (35 mL), acceptable foam density (0.90), good stability at temperature changes, freeze–thaw cycle (pass), heating–cooling cycle (pass) with no phase separation, fast complete drug release (100% in about 40 min), no interaction between the solid components of the formula and acceptable inhibition zone against Candida strains.
Finally, we can conclude that formulation of CLT as vaginal foam is an optimum method to improve patients’ compliance and cure the disease with low recurrence possibility due to fast release and long contact time with the affected area.
44. Preparation and Evaluation of PVA, Chitosan Polymeric Matrixes and In-vitro Study for their Controlled Release of Enzalutamide
Oraas A. Hatem, Zainab A. H. Alebady
Oraas A. Hatem, Zainab A. H. Alebady
Abstract
Enzalutamide is an effective androgen signaling receptor inhibitor that affects the androgen pathway in various ways. Enzalutamide can reduce the competitive binding of testosterone to the androgen receptor. It also inhibits the translocation of the activated androgen receptor for the cytoplasm to the nucleus, and its binding to DNA and cofactors recruitment to the binding site.
This study evaluated polyvinyl alcohol/chitosan hydrogels as a pH-sensitive matrix drug delivery system for enzalutamide.
The release of enzalutamide from PVA/CS hydrogel were determined at the simulated gastric and intestinal fluid (SGF and SIF, respectively). Various kinetic models were employed to evaluate the drug release’s kinetic mechanism. The drug release was influenced by the concentration of polymers, the pH of the release medium, and the amount of cross-linking agent. Hydrogels containing (60:40) PVA to chitosan showed a higher release percentage of about 98% at SIF. The kinetic models showed that the release process follows the Higuchi model in SGF with a regression coefficient of 0.925. In contrast, SIF follows the first-order model with a regression coefficient value of 0.994. The results confirmed that the new formed PVA/CS hydrogels are potential systems for enzalutamide-controlled drug delivery.
This study evaluated polyvinyl alcohol/chitosan hydrogels as a pH-sensitive matrix drug delivery system for enzalutamide.
The release of enzalutamide from PVA/CS hydrogel were determined at the simulated gastric and intestinal fluid (SGF and SIF, respectively). Various kinetic models were employed to evaluate the drug release’s kinetic mechanism. The drug release was influenced by the concentration of polymers, the pH of the release medium, and the amount of cross-linking agent. Hydrogels containing (60:40) PVA to chitosan showed a higher release percentage of about 98% at SIF. The kinetic models showed that the release process follows the Higuchi model in SGF with a regression coefficient of 0.925. In contrast, SIF follows the first-order model with a regression coefficient value of 0.994. The results confirmed that the new formed PVA/CS hydrogels are potential systems for enzalutamide-controlled drug delivery.
45. Pharmacobotanical Application of Ricinus communis Seed Oil in Formulation and Evaluation of Herbal Emulgel for the Treatment of Psoriasis
Sujit Pathare, Snehal Babar, Manoj Tare, Dwarkadas Baheti, Harshal Tare, Nitin Deshmukh, Vijay Sable
Sujit Pathare, Snehal Babar, Manoj Tare, Dwarkadas Baheti, Harshal Tare, Nitin Deshmukh, Vijay Sable
Abstract
Inflammatory and immune-mediated skin disease, psoriasis. It’s common for psoriasis to be seen in people all over the globe. Drugs are most effectively delivered through the topical route for treating skin conditions. An attempt was made to increase the effectiveness of topical treatment for psoriasis by using emulgel compositions containing Ricinus communis seed oil. In order to create the gel, the extract was mixed with liquid paraffin, olive and coconut oils, and Carbopol 936 and 940 gelling agents. The viscosity and glossiness of the emulgel were achieved using herbal extracts. When tested for physicochemical criteria, the developed formulations were found to be acceptable in every way. These findings imply that topical gel therapy for psoriasis is becoming more effective. Due to the emulgel improved penetration, the herbal gel has more effectiveness.
46. The Effect of Testosterone Gel for Patients with Poor Ovarian Response Prior to IVF Cycles: Is It really Effective?
Eaman M. Muhammed, Zainab H. Al khafajy, Huda A. Rasool
Eaman M. Muhammed, Zainab H. Al khafajy, Huda A. Rasool
Abstract
Background: Classically, poor women respond with old maternal age and little ovarian standby. Though, some females unpredictably have little reply to measured ovarian stimulation.
Aim of the Study: To evaluate the effectiveness of transdermal testosterone gel (TTG) before controlled ovarian stimulation (COS) in poor responders undergoing intracytoplasmic sperm injection (ICSI).
Methods: An interventional prospective randomized control trial that included 60 females who were definite as unfortunate responders undergoing an intracytoplasmic sperm injection (ICSI) procedure. The population was divided into two groups. Approximately 30 patients received 10 mg TTG that was applied daily for 21 days in the cycle preceding COS for ICSI Transdermal testosterone gel (TTG) pretreatment group, while the other 30 patients are the control group. All patients were assessed for their AFC again and to begin in-vitro futilization (IVF) treatment with the beginning of the menstrual cycle. Serum testosterone was measured again in the study group. The primary outcome is the number of retrieved oocytes while the secondary outcome is the number and quality of embryos transferred, chemical gestation rate.
Results: No important differences in sociodemographic features between both groups compared. Also, there was an increase in total number of oocytes in the study group but again, this difference was statically non-significant. Although the total dose of gonadotrophin (GT) and the duration of stimulation days were less in study group, but this was statically non-significant. No differences experiential regarding number and grading of embryos, chemical pregnancy rate nor clinical pregnancy rate.
Conclusion: Pretreatment of transdermal testosterone at a dose of 10 mg/day for 21 days not upsurge the number of oocyte retrieved nor the number of embryos or pregnancy rate to a significant level in poor responders undergoing ICSI.
Aim of the Study: To evaluate the effectiveness of transdermal testosterone gel (TTG) before controlled ovarian stimulation (COS) in poor responders undergoing intracytoplasmic sperm injection (ICSI).
Methods: An interventional prospective randomized control trial that included 60 females who were definite as unfortunate responders undergoing an intracytoplasmic sperm injection (ICSI) procedure. The population was divided into two groups. Approximately 30 patients received 10 mg TTG that was applied daily for 21 days in the cycle preceding COS for ICSI Transdermal testosterone gel (TTG) pretreatment group, while the other 30 patients are the control group. All patients were assessed for their AFC again and to begin in-vitro futilization (IVF) treatment with the beginning of the menstrual cycle. Serum testosterone was measured again in the study group. The primary outcome is the number of retrieved oocytes while the secondary outcome is the number and quality of embryos transferred, chemical gestation rate.
Results: No important differences in sociodemographic features between both groups compared. Also, there was an increase in total number of oocytes in the study group but again, this difference was statically non-significant. Although the total dose of gonadotrophin (GT) and the duration of stimulation days were less in study group, but this was statically non-significant. No differences experiential regarding number and grading of embryos, chemical pregnancy rate nor clinical pregnancy rate.
Conclusion: Pretreatment of transdermal testosterone at a dose of 10 mg/day for 21 days not upsurge the number of oocyte retrieved nor the number of embryos or pregnancy rate to a significant level in poor responders undergoing ICSI.
47. Preparation, Characterization, Antioxidant and Antibacterial Studies of New Metal (II) Complexes with Schiff Base for 3-amino-1-phenyl-2-pyrazoline-5-one
Nazar M. Abdalsahib, Lekaa K.A. Karem
Nazar M. Abdalsahib, Lekaa K.A. Karem
Abstract
A new ligand complexes have been synthesis from reaction of metal ions of Mn(II), Co(II), Ni(II), Cu(II), Zn(II), Cd(II), Hg(II), Pd(II) and Pt(II) with schiff base LH. 5-[(2-Hydroxy-naphthalen-1-ylmethylene)-amino]-2-phenyl-2,4-dihydro-pyrazol-3-one, this ligand was characterized by Fourier transform infrared (FTIR), UV-vis, 1H, 13CNMR, and mass spectra. All complexes were characterized by techniques micro analysis C.H.N, UV-vis and FTIR spectral studies, atomic absorption, chloride content, molar conductivity measurements and magnetic susceptibility. The ligand acts as bidentate, coordination through nitrogen atom from azomethin group and deprotonated phenolic oxygen atom. The spectroscopic and analytical measurements showed that the geometric shape of the prepared complexes is octahedral, while the square planar of the palladium and platinum complexes. The ligand and its complexes were having been screened for their antimicrobial activities and antioxidant.
48. The Study Around Effects Cell Wall of Streptococcus pyogenes on the Immune System Response
Mytham J. A. Hussain, Fadaa A. Mahmoud, Mervet A. Mshachal
Mytham J. A. Hussain, Fadaa A. Mahmoud, Mervet A. Mshachal
Abstract
Many of the most common diseases affecting humans are caused by Streptococcus. The study of the cell wall of these bacteria is directly related to the immune response. In our study, about 20 throat swabs were collected for children aged 5 to 15 years, according to the procedures and protocol of the World Health Organization (WHO), to search for Streptococcus pyogenes. We cultured bacteria on blood agar media and then used HA and HAI to obtain the main component of the bacteria wall, peptidoglycan, to determine its immune response. Whereas the study we carried out proved that the injection of Ags S/C after one month and collecting serum from these labs gives titers in group 1 1:1280 and in group 2 1:640, indicating that antigens are highly virulence (complex antigens), composed of peptides and carbohydrates.
All samples we tested gave positive results and generated an immune response to the bacteria’s cell wall peptidoglycan material.
All samples we tested gave positive results and generated an immune response to the bacteria’s cell wall peptidoglycan material.
49. Effect of Tea Extract on Few Bacterial Species Isolated from Tonsillitis by Adding Some Concentrations of NaCl
Afrah A. Jasim, Noor S. Ahmed, Marwan A. Hussein
Afrah A. Jasim, Noor S. Ahmed, Marwan A. Hussein
Abstract
Several bacterial species associated with tonsillitis were isolated from the samarra general hospital, including Staphylococcus aureus, Escherichia coli, and Klebsiella pneumoniae. The extract of alcohol and water tea was used to observe its effect in inhibiting the growth of bacteria with the addition of 3 concentrations of NaCl (5, 7.5, 10 g/L ) to the medium used (Muller hinton agar, Nutrient agar), the results showed that the effect of S. aureus on the alcohol and water extracts and all the concentrations used in addition to the use of the muller hinton agar and the use of nutrient agar the result showed that the bacteria were affected by alcohol extract and all the concentrations used however when adding the water extract the effect of bacteria was observed when adding the third concentration of NaCl , The effect of E. coli was observed by alcoholic and water extract of tea with the addition of the third concentration of NaCl using the muller hinton agar and the use of the nutrient agar the growth of E. coli was observed by alcoholic extract only and by the addition of the third concentration of NaCl, The effect of the bacteria was observed with alcohol extract only for the tea and all the concentrations using the muller hinton agar and using the nutrient agar the effect of bacterial growth was observed by the extract when adding the third concentration of NaCl to the medium, we conclude are differences in the effect of extract on isolated bacterial species
50. Osmotic Release Oral Tablet Formulation, Development, and Evaluation of an Anti-epileptic Drug
Sufiyan Ahmad, Tanvirahmad J. Shaikh, Jayesh Patil, Abhishek Meher, Deshraj Chumbhale, Harshal Tare
Sufiyan Ahmad, Tanvirahmad J. Shaikh, Jayesh Patil, Abhishek Meher, Deshraj Chumbhale, Harshal Tare
Abstract
Efforts were attempted to create a bioequivalent Osmatic release tablet formulation of carbamazepine, with a drug release profile comparable to that of the innovator product. Tablets were formulated using the wet granulation technique based on literature data and the innovative product’s characterization. It was discovered that the pioneer tablet had a film coating. After reviewing the existing literature and patents, it was determined to use a non-infringing approach and create a film-coated tablet with an equivalent bioavailability and dissolution profile. Based of justification, the optimized formulation has an F9 value of 90, which is excellent. The intention was to keep the same composition and only increase the size. Trial formulation 9’s formula and procedure fulfilled the specified physicochemical properties and dissolution profile, which is equivalent to the reference product in various media, based on the results of several laboratory trials and evaluations. The extended-release was achieved by combining the rate-controlling polymer Natrosol 250L/Natrosol 250 H, a pH-dependent polymer, and Hypromellose. Compared to the innovator sample, the extended-release tablets were found to comply with the USP specification. Stability tests on the optimised batch showed no major deviations, which is a positive result.
51. Eco-friendly Analytical Method for Estimation for Benzodiazepine Drug in Pure and Pharmaceuticals Formulations by Oxidative Coupling Reaction with Phenylephrine Hydrochloride
Aseel M. Aljeboree, Shaimaa M. Essa, Farah A. Dawood, Mohammed S. Ali, Ayad F. Alkaim
Aseel M. Aljeboree, Shaimaa M. Essa, Farah A. Dawood, Mohammed S. Ali, Ayad F. Alkaim
Abstract
A simple, fast, sensitive and selective spectrophotometric method has been developed based on the oxidative coupling reaction process, which depends on the determination of clonazepam (CZP) drug using an oxidizing agent sodium periodate (NaIO4) in the presence of a reagent, phenylephrine hydrochloride (PH-HCL), that uses the pink color of CZP at a wavelength of 495 nm. Where several factors affecting the color intensity and absorbance were studied, including the effect of color stability time, effect of the volume of the reagent, the effect of the volume of the oxidizing agent, order of addition and temperature. The calibration curve found to obey Lambert beer at range concentration (2–20 mg/L), while the limit of detection (LoD) (8. 9*10-2), limit of quantitation (LoQ) (2.6*10-2) and molar absorbance is 1.4 × 102 liters mol-1cm-1. The method was applied to pharmaceutical preparations (Tablet) and was found to characterize the best precision and accuracy. The standard methods not need any control of temperature and also not affected by interferences and henceforth successfully utilized to determine CZP in pharmaceutical preparations.
52. The Potential Protective Effects of Pirfenidone on Diclofenac Sodium Induced Gastric Ulcer in a Rat Model
Russul Abdelfatah, Huda I. Al-Qadh
Russul Abdelfatah, Huda I. Al-Qadh
Abstract
Introduction: Non-steroidal anti-inflammatory drugs (NSAIDs), are widely prescribed in clinical practice because of their ability to reduce pain, fever, and inflammation. However, NSAID-induced gastric mucosal damage is the major side effect of these medications. This study aims to reduce gastric mucosal lesions caused by NSAIDs by using pirfenidone by investigating their effect on histological, gastric gross mucosal damage.
Method: 30 healthy male albino rats were divided into 3 groups each of ten (N=10). A single oral dose of diclofenac sodium (150 mg/kg body weight) was used to induce ulceration for all groups except first. The vehicle (tween 80+NS) was given to the first group, while diclofenac sodium was given to the second group and to all pre-treated groups. The third group were pre-treated with pirfenidone (300 mg/kg). At the end of the experiment, histological examination, and antioxidant and anti-inflammatory parameters by immunohistochemistry method were evaluated.
Results: Diclofenac sodium at a dose (150 mg/kg) produces a significant increment (p > 0.01) in gastric damage score, the expression of tumor necrosis factor-alpha (TNF-α), myeloperoxidase, malonaldehyde, and the ulcer formation percent, compared to the healthy rat’s group. Pirfenidone at a dose of (300 mg/kg) pretreatment in diclofenac induced-ulcer in rats produces a significant reduction (p > 0.01) in gastric damage score, the expression of TNF-alpha, myeloperoxidase, the expression of TNF-alpha, myeloperoxidase, malonaldehyde, and in the ulcer formation percent, yet, less effectively than omeprazole and pirfenidone.
Conclusion: Diclofenac can be reduced or prevented by the pretreatment of pirfenidone. Pirfenidone showed similar results to the standard treatment (Omeprazole), the protective effect of pirfenidone was mainly through their antioxidant and anti-inflammatory activity by reducing oxidation markers like MPO and MDA, and also reducing inflammatory cytokines like TNF-alpha.
Method: 30 healthy male albino rats were divided into 3 groups each of ten (N=10). A single oral dose of diclofenac sodium (150 mg/kg body weight) was used to induce ulceration for all groups except first. The vehicle (tween 80+NS) was given to the first group, while diclofenac sodium was given to the second group and to all pre-treated groups. The third group were pre-treated with pirfenidone (300 mg/kg). At the end of the experiment, histological examination, and antioxidant and anti-inflammatory parameters by immunohistochemistry method were evaluated.
Results: Diclofenac sodium at a dose (150 mg/kg) produces a significant increment (p > 0.01) in gastric damage score, the expression of tumor necrosis factor-alpha (TNF-α), myeloperoxidase, malonaldehyde, and the ulcer formation percent, compared to the healthy rat’s group. Pirfenidone at a dose of (300 mg/kg) pretreatment in diclofenac induced-ulcer in rats produces a significant reduction (p > 0.01) in gastric damage score, the expression of TNF-alpha, myeloperoxidase, the expression of TNF-alpha, myeloperoxidase, malonaldehyde, and in the ulcer formation percent, yet, less effectively than omeprazole and pirfenidone.
Conclusion: Diclofenac can be reduced or prevented by the pretreatment of pirfenidone. Pirfenidone showed similar results to the standard treatment (Omeprazole), the protective effect of pirfenidone was mainly through their antioxidant and anti-inflammatory activity by reducing oxidation markers like MPO and MDA, and also reducing inflammatory cytokines like TNF-alpha.
53. Design, Development and Optimization of Solid Lipid Nanoparticles for Ocular Delivery of an Antifungal Agent
Raffah K. Mahal, Fatima Al-Gawhari
Raffah K. Mahal, Fatima Al-Gawhari
Abstract
Oral and intravenous dosing of the second-generation antifungal drug voriconazole (VCZ), with its wide range of antifungal action, is commercially accessible. Visual and hepatic problems might occur when VCZ is used in large doses. Voriconazole SLNs were prepared in this study with the goal of increasing corneal penetration and drug release. The thin film hydration approach was used to make VCZ SLNs. The central composite experimental design was used to maximize the impacts of independent processing factors on vesicle size (R1), drug entrapment efficiency (%EE) and zeta potential (ZP; R3) responses on lipid concentration (X1), surfactant concentration (X2), and sonication duration (X3). An evaluation of the drug release profile, corneal penetration, antifungal susceptibility, and cytotoxicity of the improved formula was conducted. The improved recipe achieved the best results with a ZP of -39.6 ± 0.28 mV, an average particle size of 156 ± 3.84 nm, and an EE% of 89.2 ± 2.01. When compared to the unformulated drug solution, the VCZ-SLNs had a prolonged 10 hours drug release profile with improved corneal penetration, with Papp and Jss measuring 14.35×10-2 cm h-1 and 4.61 mol h-1, respectively, instead of 7.28×10-2 cm h-1 and 2.48 mol h-1. Non-irritating VCZ-SLNs were determined to be corneal tissue, according to the study. Improved corneal penetration and higher antifungal activity without harmful effects on ocular tissues were achieved by VCZ-SLNs.
54. Bacterial Inhibition by Nanoparticles Treated Eucalyptus Extract
Rana S. Hasan, Maha E. Irzoqy, Jalal M. Z. Jalal, Safaa M. Sultan
Rana S. Hasan, Maha E. Irzoqy, Jalal M. Z. Jalal, Safaa M. Sultan
Abstract
This study aimed to test the efficiency of eucalyptus extracts (aqueous and alcoholic) supplemented with zinc nanoparticles in inhibiting gram-negative and gram-positive bacteria isolated in patients and their identification. The results showed the identification of two gram-negative bacteria: Salmonella and Entamoeba coli.
Three types of gram-positive bacteria are Staphylococcus aureus, Staphylococcus albus, Staphylococcus epidermidis. The effect of the aqueous extract of eucalyptus on the aforementioned species was tested, as it proved highly effective in influencing the growth of gram-positive bacteria than it is with gram-negative bacteria. While the effect of the alcoholic extract on the growth of negative bacteria was greater than its effect on the gram-positive bacteria and it proved highly effective on E. coli compared to Salmonella.
The results of the synergistic action of the above-mentioned extracts when mixed with nano-zinc, showed a significant increase in the inhibition of the growth of bacterial species. Whereas the turbulent effect of the alcoholic extract with nano-zinc showed a significant effect on the growth of dye-negative bacteria compared to the effect of the aqueous extract supplemented with nano-zinc, which gave the highest effect in inhibiting the growth of gram-positive bacteria.
Three types of gram-positive bacteria are Staphylococcus aureus, Staphylococcus albus, Staphylococcus epidermidis. The effect of the aqueous extract of eucalyptus on the aforementioned species was tested, as it proved highly effective in influencing the growth of gram-positive bacteria than it is with gram-negative bacteria. While the effect of the alcoholic extract on the growth of negative bacteria was greater than its effect on the gram-positive bacteria and it proved highly effective on E. coli compared to Salmonella.
The results of the synergistic action of the above-mentioned extracts when mixed with nano-zinc, showed a significant increase in the inhibition of the growth of bacterial species. Whereas the turbulent effect of the alcoholic extract with nano-zinc showed a significant effect on the growth of dye-negative bacteria compared to the effect of the aqueous extract supplemented with nano-zinc, which gave the highest effect in inhibiting the growth of gram-positive bacteria.
55. Improvement of Entrapment and Ocular Permeability of Ganciclovir Nanostructured Lipid Carriers Using Various Conditions of Preparations
Zainab T. Salih, Fatima Al-Gawhari
Zainab T. Salih, Fatima Al-Gawhari
Abstract
Ganciclovir (GCV) is a drug included in BCS-Class III, having high solubility and low permeability. It is a synthetic acyclic nucleoside analog of 2′-deoxyguanosine, considered a potent inhibitor of herpes viruses and cytomegalovirus (CMV) infection. Herpes simplex virus (HSV) infections are very common and are also considered a major cause of corneal blindness.
This study intended to advance a pioneering nanostructured lipid carriers (NLCs) system for improving the ocular permeability of GCV. Several procedures were used for the preparation. Cold homogenization, solvent injection, and emulsification-ultrasonication methods. A mixture of palmitic acid (PA) and oleic acid (OA) as a lipid matrix, cremophore EL, and transcutol HP were used as emulsifiers. To evaluate the optimum method, the particle size (PS), polydispersity index (PDI), zeta potential (ZP), entrapment efficiency (EE), and drug loading (DL%) were determined for the prepared NLCs. Due to the decreased particle size value, the polydispersity index, and the high value of EE%, emulsification/ultrasonication outcomes were more practical than cold homogenization and solvent injection procedures.
The findings demonstrated that the preparation procedure had a substantial impact on the EE%. The emulsification method can prepare the NLCs of GCV successfully.
This study intended to advance a pioneering nanostructured lipid carriers (NLCs) system for improving the ocular permeability of GCV. Several procedures were used for the preparation. Cold homogenization, solvent injection, and emulsification-ultrasonication methods. A mixture of palmitic acid (PA) and oleic acid (OA) as a lipid matrix, cremophore EL, and transcutol HP were used as emulsifiers. To evaluate the optimum method, the particle size (PS), polydispersity index (PDI), zeta potential (ZP), entrapment efficiency (EE), and drug loading (DL%) were determined for the prepared NLCs. Due to the decreased particle size value, the polydispersity index, and the high value of EE%, emulsification/ultrasonication outcomes were more practical than cold homogenization and solvent injection procedures.
The findings demonstrated that the preparation procedure had a substantial impact on the EE%. The emulsification method can prepare the NLCs of GCV successfully.
56. Causes and Treatment of Hematuria in Newborns
Ghanim A. Abbas, Meraim A. Kazaal
Ghanim A. Abbas, Meraim A. Kazaal
Abstract
Background: Hematuria is one of the cases that has started to increase in newborns, but studies on the causes and treatment of this condition are very limited, especially in Iraq. Therefore, the current study aims to determine the prevalence of this condition and monitor its causes and appropriate treatment.
Methods: The current study includes the collection of questionnaires and medical examinations from 35 newborns (ages between 2 hours to 2.5 months) suffering from hematuria for various reasons. Samples were collected during the period from 2/1/2021 to 28/3/2021, and information and examinations for each diseased case were collected.
Results: The results of the study showed that most of the newborns had gross hematuria (91%) compared to microhematuria (9%), especially males and that the main causes of hematuria in newborns were due to bacterial septicemia (37%) and urinary tract infections (32%), congenital malformations (14%), and renal artery thrombosis (11%). The results also showed that most of the children who suffer from hematuria whose mothers suffer from health problems during pregnancy, the most important of which are anemia (31.4%), urinary tract infection (UTI) (14.2%) and gestational diabetes (14.2%). The results of this study also showed that the treatment of hematuria depends on the diagnosis of the pathogen, and the CT scan was a basic examination for all cases, in addition to that, the microscopic examination and the culture of urine were also used. Antibiotics and surgeries were the appropriate treatment in most cases of hematuria. In conclusion, blood in urine is a pathological condition that needs diagnosis and treatment as soon as possible to avoid complications or disorders that may threaten the newborn’s life.
Methods: The current study includes the collection of questionnaires and medical examinations from 35 newborns (ages between 2 hours to 2.5 months) suffering from hematuria for various reasons. Samples were collected during the period from 2/1/2021 to 28/3/2021, and information and examinations for each diseased case were collected.
Results: The results of the study showed that most of the newborns had gross hematuria (91%) compared to microhematuria (9%), especially males and that the main causes of hematuria in newborns were due to bacterial septicemia (37%) and urinary tract infections (32%), congenital malformations (14%), and renal artery thrombosis (11%). The results also showed that most of the children who suffer from hematuria whose mothers suffer from health problems during pregnancy, the most important of which are anemia (31.4%), urinary tract infection (UTI) (14.2%) and gestational diabetes (14.2%). The results of this study also showed that the treatment of hematuria depends on the diagnosis of the pathogen, and the CT scan was a basic examination for all cases, in addition to that, the microscopic examination and the culture of urine were also used. Antibiotics and surgeries were the appropriate treatment in most cases of hematuria. In conclusion, blood in urine is a pathological condition that needs diagnosis and treatment as soon as possible to avoid complications or disorders that may threaten the newborn’s life.
57. Preliminary Phytochemical Investigation and Effect of Cucurbita maxima Seeds Oil on Burn Wound Healing in Iraq
Estabraq H. Naser, Haifaa R. Alansari, Abbas M. Kashmer
Estabraq H. Naser, Haifaa R. Alansari, Abbas M. Kashmer
Abstract
Cucurbita maxima seeds oil were extracted by hot and cold method, identified their phytochemical components as it contains alkaloids, flavonoids, saponins and tannins and analyzed to explain its ability to heal burn wound. Male albino 32 Sprague-Dawley rats were divided into four rats in each cage which included a positive control group (Mebo ointment): two rats for first-degree burn and two for the second one, negative control group: two rats for first-degree burn and two for the second one, cold method: 100% concentration with two rats for first-degree burn and two for the second one and hot method: 100, 75, 50, 25 and 10% concentration with two rats for first-degree burn and two for the second one for each concentration. The results showed that the extracts of C. maxima seeds oil at first and second-degree burn by the cold method were not efficient so it could neglect where it compared to the hot procedure at the same time the concentrations 100, 75, 50, 25, and 10% were significant as LSD5% were more than 0.01 when compared with the negative standard, while when compared with the positive standard 100 and 75% were significant while 25, 10% were insignificant and 50% had the same activity as the positive standard. Also, there is a significant difference between concentration at fifth week; 100 and 75% has the largest significant differences which is 0.01 among the other concentrations. At second-degree burn we notice that all the concentrations 100, 75, 50, 25, and 10% were significant as LSD5% were more than 0.01 when compared with the negative control, while when compared with the positive control 100 and 75% were significant while 25, 10% were insignificant and 50% had the same activity as the positive standard. Also, there is a significant difference between concentrations at fifth week, 75% has the largest significant difference among the other concentrations. As a final result the concentration 100 and 75% were the best concentration in the treatment of burn wound as the 100% contained a large amount of extract and 75% contained a sufficient quantity of extract in addition to the ointment base vaseline which aid in keeping the skin wet enough to avoid shrinkage of it and help in the rehabilitation of skin epithelial cells. This study of C. maxima seeds oil is the first study in the healing of burn wound on rats in Iraq.
58. Preparation and Characterization of Instantly-soluble Solid Eye Drop for Glaucomatous Patients
Ahed R. Hameed, D. H. Athmar, Habeeb Al-Shohani
Ahed R. Hameed, D. H. Athmar, Habeeb Al-Shohani
Abstract
For the treatment of glaucoma eye drops are chronically used. However, chronic use of preservatives in eye drops cause irritation problem and affects ocular tissues. The aim is to formulate an instant soluble solid eye drop to avoid using preservatives since solid dosage forms do not require preservation.
Ocular mini-tablets of dorzolamide hydrochloride (DZ) and timolol maleate (TM) were prepared by direct compression using different polymers and were evaluated for their physical properties. The release DZ and TM was compared to COSOPT eye drops.
Formulation F2 mini-tablets (which contain DZ, TM, mannitol and microcrystalline cellulose MCC) were chosen as the optimum formula because they had uniform shape and minimum variation in weight 9.69 ± 0.55 mg. Thickness and diameter were 1.38 ± 1.28 and 3.01 ± 0.03 mm, respectively, within the acceptable limits. Hardness and friability were also within the permissable range which were 4.14 ± 0.22 kg/cm2 for hardness and 0.73% ± 0.05 for friability. The drug content for both DZ and TM were within the acceptable limits and the release had no significant difference (p > 0.05) compared to commercial eye drop and the mini-tablets dissolved completely with less than one minute. The FTIR and DSC revealed no interaction between the drugs and excipients used.
Sterilization using gamma radiation was performed to test the animal’s mini-tablets. The radiation did not significantly (p>0.05) alter any properties of F2 and no signs of irritation on the animal eye appeared.
In conclusion, instant soluble solid eye drop in the form of mini-tablet was successfully prepared by direct compression method and caused no irritation when tested on animals.
Ocular mini-tablets of dorzolamide hydrochloride (DZ) and timolol maleate (TM) were prepared by direct compression using different polymers and were evaluated for their physical properties. The release DZ and TM was compared to COSOPT eye drops.
Formulation F2 mini-tablets (which contain DZ, TM, mannitol and microcrystalline cellulose MCC) were chosen as the optimum formula because they had uniform shape and minimum variation in weight 9.69 ± 0.55 mg. Thickness and diameter were 1.38 ± 1.28 and 3.01 ± 0.03 mm, respectively, within the acceptable limits. Hardness and friability were also within the permissable range which were 4.14 ± 0.22 kg/cm2 for hardness and 0.73% ± 0.05 for friability. The drug content for both DZ and TM were within the acceptable limits and the release had no significant difference (p > 0.05) compared to commercial eye drop and the mini-tablets dissolved completely with less than one minute. The FTIR and DSC revealed no interaction between the drugs and excipients used.
Sterilization using gamma radiation was performed to test the animal’s mini-tablets. The radiation did not significantly (p>0.05) alter any properties of F2 and no signs of irritation on the animal eye appeared.
In conclusion, instant soluble solid eye drop in the form of mini-tablet was successfully prepared by direct compression method and caused no irritation when tested on animals.
59. High-Performance Thin Layer Chromatography Method Development to Estimate Phytoconstituents in Hedychium species
Samiksha Karde, Srishti Jha, Bhushan Pimple, Mohini Kuchekar, Padmaja Kore, Gauri Ghangale, Harshal Tare
Samiksha Karde, Srishti Jha, Bhushan Pimple, Mohini Kuchekar, Padmaja Kore, Gauri Ghangale, Harshal Tare
Abstract
Objective: The Hedychium coronarium (Zingiberaceae) is a perennial herbaceous plant. Chinese immigrants introduced the H. coronarium species as an ornamental plant in 1888. Its attractive flowers make it a desirable ornamental plant. The present study aims to evaluate the physiochemical characteristics and development of the (HPTLC) Fingerprint sequence profile of H. coronarium leaves.
Method: Pharmacognostic characteristics and physiochemical parameters were performed according to the method prescribed. The mobile phase confirmation was completed using by performing (TLC). The development of the HPTLC fingerprint was performed with some modifications to get exact separation of phytochemicals using mobile phases such as Toluene: chloroform: ethanol (4:4:1).
Result: Pharmacognostic study reported the presence of unicellular trichomes, vessels, epidermal cells, oil globules, and vascular bundles. Pharmacognostic and physiochemical parameters like color, nature, odor, taste, foreign organic matter, loss on drying, ash value, extractive value, and the foaming index were found to be satisfied as documented in the results. The HPTLC fingerprinting reveals the presence of various chemical compounds expressed as Rf value.
Conclusion: From current scientific research work, H. coronarium can be useful in modern medicine as various bioactive secondary metabolites were detected.
Method: Pharmacognostic characteristics and physiochemical parameters were performed according to the method prescribed. The mobile phase confirmation was completed using by performing (TLC). The development of the HPTLC fingerprint was performed with some modifications to get exact separation of phytochemicals using mobile phases such as Toluene: chloroform: ethanol (4:4:1).
Result: Pharmacognostic study reported the presence of unicellular trichomes, vessels, epidermal cells, oil globules, and vascular bundles. Pharmacognostic and physiochemical parameters like color, nature, odor, taste, foreign organic matter, loss on drying, ash value, extractive value, and the foaming index were found to be satisfied as documented in the results. The HPTLC fingerprinting reveals the presence of various chemical compounds expressed as Rf value.
Conclusion: From current scientific research work, H. coronarium can be useful in modern medicine as various bioactive secondary metabolites were detected.
60. Knowledge of The HILIC Retention Behaviors of Two Quinolone Antibiotics on Sulfobetaine-Type Zwitterionic Stationary Phases
Bashaer A. Al-Aphalahy, Ameen W. Qassim, Raad R. Karabat
Bashaer A. Al-Aphalahy, Ameen W. Qassim, Raad R. Karabat
Abstract
Fluoroquinolones treat infections of the urinary, respiratory, gastrointestinal, skin, bone, and joint systems. This article describes the development of the hydrophilic interaction liquid chromatography (ZIC-HILIC) method to determine norfloxacin and ofloxacin retention characteristics. Separation of all analytes was accomplished using ZIC-HILIC1 and ZIC-HILIC4 columns. The mobile phase was 40 mM sodium acetate water solution in acetonitrile pumped at a 0.7 mL/min flow rate. The influence of acetonitrile concentration, the presence of salt in the mobile phase, and pH on the retention of norfloxacin and ofloxacin in the HILIC mode were investigated in this study. When using ZIC-HILIC columns, it was discovered that the retention factors of the analytes were inversely proportional to the amount of water present in the mobile phase, which is representative of a conventional hydrophilic partitioning mechanism. The ZIC-HILIC based strategies described in this article represent a significant step toward more sensitive drug analysis. We observed that zwitterionic materials could govern the separation of materials, as shown by the influence of the chain length between the zwitterion groups, which contributed to the explanation of the variation in the retention period of the materials to be separated.
61. Synthesis, Characterization and Preliminary Antimicrobial and Anti-inflammatory Evaluation of New Ibuprofen Hydrazide Derivatives
Zainab D. Kamms, Mohammed K. Hadi
Zainab D. Kamms, Mohammed K. Hadi
Abstract
Non-steroidal anti-inflammatory medicines (NSAIDs) are medicines that are distributed widely across the world due to their ability to reduce pain and inflammation. In order to boost the drug’s efficacy and reduce its harmful side effect like GIT ulcers and bleeding, a newly synthesized series of 25-(1-(4-isobutylphenyl) ethyl)-1,3,4-oxadiazole-2-thiol derivatives compounds (C, C 1-3) were prepared from the reaction of ibuprofen hydrazide with carbon disulfide followed by reaction with various Aryl/alkyl halide. All target compounds were tested for antimicrobial efficacy against various strains of bacteria (G+ve, S. pyrogenes and S. aureus) and (G-ve, E. coli and Klebsiella pneumoniae). Additionally, fungus species (Candida albicans). Compound C showed good antimicrobial activity for both bacterial strains. At the same time, Compound C1 have the best anti-bacterial activity compared with other synthesized compounds for1 both (G+ve), and (G-ve) bacteria, and compound C3 was the most affected one as antifungal. The compound C2 was with lowest antimicrobial activity. All of the produced compounds were examined for their anti-inflammatory activity using (egg-white generate edema) and the compounds (C, C1, C3) showed good efficacy when compared to ibuprofen (stander) FTIR and 1H-NMR spectroscopy were used to analyze all of the final products.
62. Influences of Nitrogen, Magnesium and Soil Moisture Contents and their Interactions on Yield Quality and Tolerance Indices of Rosemary (Rosmarinus officinalis L.)
Nahla M.A. Khaleel, Abdulghany O. I. Sarmamy
Nahla M.A. Khaleel, Abdulghany O. I. Sarmamy
Abstract
The present study was carried out in the glasshouse of the Department of Biology, College of Science, Salahaddin University-Erbil, and laboratories of Research Center in Erbil Polytechnic University, from April 21st, 2019 to July 26th, 2020, to determine the effects of foliar application of nitrogen (N1:100, N2:200, and N3:300 kg. h-1) and magnesium (Mg1:0.0, Mg 2:30, and Mg3:60 kg. h-1) applied under two different soil moisture contents (SM1:100% field capacity (FC) and SM2: 60% FC) on some physiological properties and yield quality of rosemary plants (Rosmarinus officinalis L.). A factorial experiment was laid out according to a completely randomized design with four replications. Two cuttings were taken from the rosemary shoots (in March, and July, 2020). Results showed that SM2 decreased phenolic compounds in cut 1 (cut 1), dry matter percent in leaves in cut 2 and relative nitrogen yield in cut 1, cut 2 & cut 1+2. N3 increased dry matter in leaves & shoots in cut2 significantly, proline, phenolic compounds in leaves, stress tolerance index (STI), modified stress tolerance index 1(MSTIK1), & modified stress tolerance index 2 (MSTIK2). The interaction treatment SM2Mg2 increased the proline content in dry leaves. The proline content was increased by the triple interactions SM2N3Mg2 and SM2N3Mg3.
63. Synthesis, Characterization and Biological Activity of Azo Dye Derived from 2-methoxyaniline and its Complexes
Hasan S. Mohammed, Saif D. K. Alzamili
Hasan S. Mohammed, Saif D. K. Alzamili
Abstract
The azo ligand of guanine namely 8-[2-methoxyphenylazo]-guanine (MPAG) was prepared and characterized by elemental analysis, mass spectroscopy, 1H-NMR, FTIR and UV-vis spectroscopies. The Cu(II) and Zn(II) complexes of MPAG ligand were prepared under mole ratio equal to 2:1 as MPAG ligand to metal ions and characterized by 1H-NMR, FTIR, UV-vis, XRD powder and mass spectroscopies and elemental analysis, magnetic susceptibility as well as molar conductance. The solvents did not have a significant effect on the NAPAG ligand, and the MPAG ligand exhibited potential changes under different pH values. The MPAG ligand may be utilized as a colorimetric sensor for the particles of Co2+, Ni2+, Cu2+ and Zn in watery solutions. The MPAG ligand is tridentate, and the complexes are electrolyte and octahedral.
64. Protective Effects of Aqueous Cranberry Fruit Extract against Genotoxicity Induced by Cisplatin in Mice Bone Marrow Cells
Baidaa I. Mohammed, Nada N. Al-Shawi, Ali F. Hasan
Baidaa I. Mohammed, Nada N. Al-Shawi, Ali F. Hasan
Abstract
The cranberry (Vaccinium macrocarpon) is a North American native fruit and contains a very wide variety of phytochemicals which has several beneficial effects on humans.
Aim: The study was designed to assess the protective effect of cranberry fruit extract on selected genotoxic parameters induced by cisplatin in mice’s bone marrow.
Methods: 56 male albino mice were randomly divided into two equal numbers (28 mice)/for each part of the study [Part one: for the evaluation of chromosomal aberrations and the mitotic index; and Part two: for the evaluation of micronucleus index]; and for each part, mice were randomly divided into 4 groups: Group I [negative Control/orally-administered normal saline]; Group II [Orally-administered cranberry fruit extract alone]; Group III [Single IP injection of cisplatin]; Group IV [Orally-administered cranberry fruits extract followed by a single IP injection of cisplatin].
Results: Treatment with cisplatin significantly increased total chromosomal aberration (0.159 ± 0.006) and micronucleus appearance (9.740 ± 0.531) but, it has a significant decrease in mitotic index (6.020 ± 0.589) compared to that in negative control bone marrow cells. In addition, results showed that there were significant changes in the total chromosomal aberration, micronucleus appearance, and mitotic index among the Groups (II, III, IV) (0.093 ± 0.015; 0.159 ± 0.006; 0.117 ± 0.002), (5.940 ± 0.568; 9.740 ± 0.531; 8.000 ± 0.479) and (8.720 ± 0.432; 6.020 ± 0.589; 7.480 ± 0.664), respectively in bone marrow cells.
Conclusion: Cisplatin produced a pronounced effect on total chromosomal aberrations, micronucleus appearance, and mitotic index; and the cranberry fruit extract confers a protective effect against cisplatin-induced genotoxicity in mice.
Aim: The study was designed to assess the protective effect of cranberry fruit extract on selected genotoxic parameters induced by cisplatin in mice’s bone marrow.
Methods: 56 male albino mice were randomly divided into two equal numbers (28 mice)/for each part of the study [Part one: for the evaluation of chromosomal aberrations and the mitotic index; and Part two: for the evaluation of micronucleus index]; and for each part, mice were randomly divided into 4 groups: Group I [negative Control/orally-administered normal saline]; Group II [Orally-administered cranberry fruit extract alone]; Group III [Single IP injection of cisplatin]; Group IV [Orally-administered cranberry fruits extract followed by a single IP injection of cisplatin].
Results: Treatment with cisplatin significantly increased total chromosomal aberration (0.159 ± 0.006) and micronucleus appearance (9.740 ± 0.531) but, it has a significant decrease in mitotic index (6.020 ± 0.589) compared to that in negative control bone marrow cells. In addition, results showed that there were significant changes in the total chromosomal aberration, micronucleus appearance, and mitotic index among the Groups (II, III, IV) (0.093 ± 0.015; 0.159 ± 0.006; 0.117 ± 0.002), (5.940 ± 0.568; 9.740 ± 0.531; 8.000 ± 0.479) and (8.720 ± 0.432; 6.020 ± 0.589; 7.480 ± 0.664), respectively in bone marrow cells.
Conclusion: Cisplatin produced a pronounced effect on total chromosomal aberrations, micronucleus appearance, and mitotic index; and the cranberry fruit extract confers a protective effect against cisplatin-induced genotoxicity in mice.
65. Phytochemical Screening by GC/MS with Isolation and Characterization of ß-sitosterol and Stigmasterol from Iraqi Euonymus japonicus L. Leaves Parts by Different Techniques
Rasha A. Khalaf, Thukaa Z. Abdul-Jalill
Rasha A. Khalaf, Thukaa Z. Abdul-Jalill
Abstract
Euonymus japonicus L., often known as the spindle tree, is a Celastraceae family plant utilized in traditional medicine and as an attractive garden plant. The goal of this study was to identify and isolate the active compounds B-sitasterol and stigmasterol from the roots and leaves of E. japonicus by using gas chromatography/mass spectrometry (GC-MS), high performance liquid chromatography (HPLC), and reverse phase-high performance liquid chromatography (RP-HPLC) were used to investigate the chemical composition of the leaves and root of E. japonicus. This confirms the presence of b-sitosterol and stigmasterol in the leaves and roots of E. japonicus L. plant. The structure of these chemicals was clearly defined by UV spectroscopic, FTIR spectroscopic, and TLC techniques, revealing similarity to B-sitosterol and stigmasterol.
66. Fabrication of Transdermal Gel Embedded with Solid Lipid Nanoparticles of Indomethacin
Amina Hajwani, Afreen Khan, Numan Ansari, Nazir Zerdi, M. Salman Baig
Amina Hajwani, Afreen Khan, Numan Ansari, Nazir Zerdi, M. Salman Baig
Abstract
Rheumatoid/osteoarthritis is one of the most common causes for lacking behind in the health sector. Medication in the form of tablets are already available in the market but has disadvantages. When these medicines are taken orally it cause heartburn and discomfort. The introduction of transdermal drug delivery is expected to solve this problem of side effects associated with oral delivery of drug. In the present study, indomethacin was loaded in solid lipid nanoparticles (SLN) which are then embedded in Carbopol gel for transdermal application. The solvent evaporation ultrasonication method was used for making SLNs.
The formulation was evaluated for various parameters such as; particle size and zeta potential of SLN using zetasizer as an instrument and gel formulations were evaluated for pH, spreading coefficient, viscosity, visual appearance and clarity.
Gel-embedded SLN formulation was found to be a potential transdermal drug delivery system for NSAIDs like indomethacin to treat ailments like rheumatoid arthritis or osteoarthritis.
The formulation was evaluated for various parameters such as; particle size and zeta potential of SLN using zetasizer as an instrument and gel formulations were evaluated for pH, spreading coefficient, viscosity, visual appearance and clarity.
Gel-embedded SLN formulation was found to be a potential transdermal drug delivery system for NSAIDs like indomethacin to treat ailments like rheumatoid arthritis or osteoarthritis.
67. Formulation and Evaluation of Citronella Oil (Cymbopogon nardus (L.) Rendle) Cream for Acne Treatment
Tantri L. Nareswari, Fidela O. Vrince, Erga Syafitri
Tantri L. Nareswari, Fidela O. Vrince, Erga Syafitri
Abstract
Acne is a prevalent skin disorder that affects 80–85% of teenagers globally. Citronella oil is one of the natural compounds that has been known to potentially treat acne, but its application is limited due to its greasiness and uncomfortable sensation on skin. This study aimed to optimize the concentration of cetyl alcohol as a viscosity enhancer that can produce a physically stable cream preparation and to evaluate the antibacterial activity of the optimized formula against Propionibacterium acnes. Following the emulsification process, the physical characteristics of the five cream formulas, including organoleptic, homogeneity, emulsion type, pH, adhesion, specific gravity, viscosity, and stability were evaluated. Formula 3 (F3), cream formulation with 6% cetyl alcohol having physical characteristics of a white homogeneous cream with a pronounced lemongrass scent, emulsion type o/w, pH of 6.30 ± 0.02, adhesion of 16.85 ± 0.58 s, a specific gravity of 1.031 ± 0.009 g/mL, and viscosity of 4418 ± 182 m Pas was chosen as the optimized formula. F3 was then subjected to antibacterial testing against P. acne and showed a 9.35 mm inhibition zone. Cream-based citronella oil, therefore, becomes a promising preparation for acne treatment.
68. Regulation of Autophagy in Neurodegenerative Diseases: A Brief Review on Autophagy Therapy for Neurodegenerative Diseases
Anmol Kanda, Avijit Mazumder, Saumya Das, Vishnu Prabhakar, Tanya Singh, Soni Kumari, Apoorva Mishra
Anmol Kanda, Avijit Mazumder, Saumya Das, Vishnu Prabhakar, Tanya Singh, Soni Kumari, Apoorva Mishra
Abstract
Autophagy involves the breakdown of complete organelles and macromolecules in the cytoplasm of eukaryotic cells, especially proteins with extended half-lives. During this degrading phase, therapeutic, pharmacological, and fasting approaches are important. All eukaryotic cells engage in autophagy, which is an ancient and evolutionarily conserved phenomenon. It has been discovered in mammals, including humans, as well as the yeast Saccharomyces cerevisiae and the fly Drosophila melanogaster. Its significance in cell and dysfunction impairing the autophagy process that is connected to a broad array of serious illnesses, including neuronal and metabolic brain diseases. Only a concise summary of the various forms of autophagy and its molecular mechanisms, as well as how they relate to neuronal health, will be provided in this work. Negative regulations are frequently used to define the regulatory networks that govern the autophagy process. This study, however, focuses on alternative strategies to promote autophagy. Metabolic neurodegenerative diseases can be treated by activating this mechanism via a variety of drugs or mechanisms. These points are covered and discussed in this article.
69. The Use of Natural and Synthetic Polymers in the Formulation of Gastro retentive Drug Delivery System
Ahmad Ainurofiq, Amalia Daryati, Faradisania A. Murtadla, Fatimatus Salimah, Nila M. Akbar, Rizka A. Faizun
Ahmad Ainurofiq, Amalia Daryati, Faradisania A. Murtadla, Fatimatus Salimah, Nila M. Akbar, Rizka A. Faizun
Abstract
The gastric emptying process drastically reduces the bioavailability of drugs that target the stomach for their action. A gastro retentive drug delivery system (GRDDS) becomes a solution to retain drugs in the stomach and release drugs from the formulation system within a certain period. The polymer used in the GRDDS formulation is the essential excipient that can retain the drugs in the stomach. Several ways for GRDDS to maintain its existence in the stomach are using some systems, such as mucoadhesive, low-density, high-density, swellable, effervescent, and expandable systems. A polymer is a macromolecular substance with a long repeating chain consisting of natural and synthetic polymers, each with different potentials. It is considered for its ability to regulate drug release, good flow properties, can improve drug dissolution to improve bioavailability and stability during processing in the body. Combining natural and synthetic polymers is often carried out to obtain advantages and cover the existing polymer’s disadvantages. Polymers can release drugs using three different mechanisms, i.e., diffusion, degradation, and expansion. These techniques are often chosen for the formulation of GRDDS because of their more flexible system and fit for almost all types of GRDDS. The polymer used in the GRDDS system is chosen from its physicochemical properties and the number of floating times, drug release rate, viscosity, floating lag times, bioavailability, and solubility.
70. TRP Channels as Emerging Therapeutic Targets in Neurological Disorders
Avijit Mazumder, Tanya Singh, Vishnu Prabhakar, Anmol Kanda
Avijit Mazumder, Tanya Singh, Vishnu Prabhakar, Anmol Kanda
Abstract
Neurological disorders like Parkinson disease (PD), Alzheimer’s disease (AD), epilepsy, stroke, schizophrenia, depression, bipolar disorder, etc., are increasingly recognized as significant causes of death and disability globally. All these neurological disorders have several similar causes, such as disturbance in Ca2+ homeostasis and misfolded proteins deposition in the brain through impairing the function of a no. of ion channels, including TRP channels. TRP channels superfamily consists of a broad collection of non-selective Ca2+ permeable channels that plays a crucial role in regulating intracellular Ca2+ homeostasis. These channels function as cellular sensors and are stimulated by a variety of physio-chemical stimulus, and endogenous and exogenous ligands. Numerous neuronal diseases are caused by disturbances in the activity of TRP channels, which are abundantly expressed in neuronal cells. When the activity of TRP channels is disturbed under pathological conditions, there is disruption of the homeostasis of neurons via oxidative stress, Ca2+ dyshomeostasis, and mitochondrial dysfunction. Therefore, these channels act as promising therapeutic candidates for pharmacological interventions in several neurological disorders. Thus within this review, we emphasize the function of TRP channels in neurological disorders and highlight the pharmacological modulators that target TRP channels.