1. Partition Coefficient and Glutathione Penetration of Topical Antiaging: Preformulation Study
Fitria Nugrahaeni, Dewi Melani Hariyadi, Noorma Rosita
Glutathione (GSH) is a broad antioxidant of the thiol-tripeptide group, highly hydrophilic, which has limitation for topical preparations. A lipophilic surfactant is an alternative method to enhance the glutathione partition. The purpose of this study was to determine the apparent partition coefficient (APC log) of glutathione; glutathione with additional surfactant at different HLB value of HLB 4.3; 5.5; 7; 11 and selected HLB was studied for penetration. The study was conducted by dissolving glutathione in water plus various HLB surfactants. Determination method of partition coefficient was done by shake flash method. The penetration test was conducted using the parameter of decreasing Matrix Metalloproteinase-1 expression on the balb-c male skin. The results can be used as a reference for topical glutathione formulations as these results are preformulation study.
2. Formulation and Evaluation of Microemulsion Based Topical Gel of Carbamazepine
Padhiar J S, Shirolkar S V, Deshkar S S
Carbamazepine(CBZ) is a synthetic compound of the benzodiazepine class, used as an anticonvulsant and analgesic drug. Carbamazepine is relatively slowly but well absorbed after oral administration. Its plasma half-life is about 30 hours when it is given as single dose, but it is a strong inducer of hepatic enzymes and the plasma half-life shortens to about 15 hours when it is given repeatedly. Psoriasis is autoimmune disease in which genetic and environmental factors have a significant role. Carbamazepine was accidently discovered to have antipsoriatic properties. Carbamazepine was obtained as a gift sample from Lupin. Characterization of carbamazepine was carried out by melting point and IR. Carbamazepine has limited aqueous solubility so in literature Self microemulsifying drug delivery system (SMEDDS) have been reported. In the present study, a topical microemulsion based gel of Carbamazepine was prepared. The pseudo ternary phase diagram was prepared to find the microemulsion region. Various microemulsion gel formulations were prepared using carbopol-974 and poloxamer-407 in varied concentrations. Prepared formulations (FG1 to FG10) were evaluated for various parameters like color, appearance, consistency, pH, spreadability and IR. The microemulsion based gels were found to have good spreadability and pH within the range of skin pH and thus suitable to use on skin.
3. Formulation and Evaluation of Galantamine Hydrobromide Floating Matrix Tablet
Poreddy Srikanth Reddy, Penjuri Subhash Chandra bose, Vuppula Sruthi, Damineni Saritha
The aim of the present work was to prepare floating tablets of galantamine HBr using sodium alginate and xanthan gum as matrix forming carriers. Galantamine HBr is used for the treatment of mild to moderate Alzheimer’s disease and various other memory impairments, in particular those of vascular origin. The matrix tablet formulations were prepared by varying the concentrations of sodium alginate and xanthan gum. The tablets were prepared by direct compression technique using PVP K-30 as a binder and sodium bicarbonate for development of CO2
. The prepared matrix tablets were evaluated for properties such as hardness, thickness, friability, weight variation, floating lag time, compatibility using DSC and FTIR. In vitro
dissolution was carried out for 12 hrs in 0.1N HCl at 37±0.5 ºC using USP paddle type dissolution apparatus. It was noted that, all the prepared formulations had desired floating lag time and constantly floated on dissolution medium by maintaining the matrix integrity. The drug release from prepared tablets was found to vary with varying concentration of the polymers, sodium alginate and xanthan gum. From the study it was concluded that floating drug delivery system for galantamine HBr can be prepared by using sodium alginate and xanthan gum as a carrier.
4. Studies on Orally Disintegrating Tablets Prepared by Using Natural and Synthetic Superdisintegrants
Piplani Mona, Diwedi Rohini, Bhagwat Deepak Prabhakar, Pahwa Rakesh
The objective of present study was to compare the disintegration efficiency of mucilage isolated from Plantago ovata
with commonly used synthetic superdisintegrant, croscarmellose sodium in the formulation of orally disintegrating tablets. Effects of varying concentration of both superdisintegrants on disintegration time were studied. Orally disintegrating tablets of metoclopramide hydrochloride were prepared using selected superdisintegrants by direct compression technique. Prepared tablets were evaluated for weight variation, thickness, hardness, friability, disintegration time, wetting time, water absorption ratio and dissolution test. Swelling index was also investigated for comparing the swelling property of croscarmellose sodium with mucilage of Plantago ovata
. Swelling index of mucilage isolated from Plantago ovata
was found to be greater (94 ± 2.5% v/v) when compared with croscarmellose sodium (85 ± 1.5% v/v). The present study indicated that mucilage isolated from natural source proved to be more effective for their disintegrating property than the most commonly used synthetic superdisintegrant, croscarmellose sodium.
5. Preparation and Immunocharacterization of Probiotic DNA Loaded Chitosan Nanoparticles: An In Vitro and In Vivo Study
Kaur M, Bhatia A, Sethi D, Vig K, Kaur G
The rise in infectious diseases as well as non infectious immune related disorders demand the need for the development of efficient immunomodulators. The chemical based drugs employed to cure these diseases may have the side effects and are costly. In the present era, consumer awareness about the harmful effects of chemical drugs raised a need to search for natural/alternative therapy for the disease treatment. Immunotherapy is one of the alternative ways of management/modification of diseases. Probiotics have been proved to be beneficial for human beings. Even its components such as cell wall, genomic DNA, etc act as foreign antigen to eukaryotic organisms and are immune enhancers. The immune enhancing efficacy of probiotic DNA might be increased by nanoparticle assisted delivery. Chitosan nanoparticles (chitosan NP) have been greatly explored and developed for pharmaceutical applications. Hence, the present study was conducted to prepare and characterize the probiotic genomic DNA loaded chitosan nanoparticles (DLCNP) and to compare their immunomodulatory potential with Lactobacillus acidophilus
NCDC343 (LA 343) whole cell and their isolated genomic DNA (LA DNA) in vitro
as well as in experimental animals. The characterization studies revealed that nanoparticles size ranging from 350 to 515nm were prepared with a positive zeta potential in between +8.71 to +17.7mV. In vitro
experiments proved that LA 343, LA DNA, DLCNP showed immune enhancing activity; maximum being shown by DLCNP. Further, in vivo
experiments demonstrated that DLCNP show significantly higher activity than LA DNA. Moreover, study on routes of administration indicated that i.m route is best for giving LA DNA whereas, i.p route is better for nanoparticles.
6. Skin Penetration of Ubiquinone (Co-Q10) In Nanoemulsion Delivery System Using Virgin Cocunut Oil (Vco)
Tristiana Erawati M, Widji Soeratri, Noorma Rosita
Ubiquinone (co-Q10) is a topical anti-aging with low solubility in water, so its penetration into the skin is also low. To increase its penetration ubiquinone (co-Q10) was loaded in the nanoemulsion delivery system using virgin coconut oil (VCO) as oil phase. Ubiquinone (co-Q10) in nanoemulsion formula consists of; ubiquinone (co-Q10), Tween 80, Span 80, ethanol 96%, VCO and acetate buffer solution pH 4.2 ± 0.5 with concentration; 1%; 18.66%; 1.92%; 3.42%; up to 100%, respectively. The characteristics of ubiquinone (co-Q10) nanoemulsion were observed in terms of droplet morphology by transmission electron microscope (TEM) and droplet size by particle analyzer, the pH and viscosity value. The ubiquinone (co-Q10) penetration test in the nanoemulsion system was compared with the emulsion on the rat skin. Result of this research showed the droplet morphology of ubiquinone (co-Q10) in nanoemulsion was spherical. The droplet size was 93.2 ± 2.78 nm. The pH value was 4.12 ± 0.02, and the viscosity was 8.5 cPas. Penetrasi of ubiquinone (co-Q10) in nanoemulsion was deeper (269 ± 48.12 dan 993 ± 36.49 μm) than in emulsion (26.33 ± 6.43 and 110.33 ± 9.124 μm), after 2 and 6 hours sample application.
7. Design and Evaluation of Ion Activated In-Situ Ophthalmic Gel of Brimonidine Tartarate Using Kappa Carrageenan
Vazir Ashfaq Ahmed, Divakar Goli
The objective of the study was to develop optimized formulation of In-situ
gel of Brimonidine tartarate (BT), anti-glaucoma agent using Ion activated polymer; Gelrite as gelling agent, kappa carrageenan as mucoadhesive agent and Hydroxy Propyl Methyl Cellulose (HPMC E50) as release retardant polymer. The 23
factorial design was employed to optimize the formulation considering concentration of Gelrite, kappa carrageenan and Hydroxy Propyl Methyl Cellulose as independent variables, mucoadhesive force (N). Viscosity (cP) and In-vitro
percentage drug release as dependent variables. Based on mucoadhesive force (N), Viscosity(CPS) and In-vitro
percentage drug release, formulation containing concentration Gelrite (0.39%), kappa carrageenan (0.21%) and HPMC E50 (0.4%) was found to be optimized formulation developed by 23
factorial design. Formulation was prepared successfully and assessed for gelling capacity, pH, rheological studies, refractive index, optical clarity, isotonicity and as ocular irriation by hen’s egg chorioallantoic membrane (HET-CAM) Test. The overall results of this study revealed that the Brimonidine tartarate/kappa carrageenan in-situ
system can be used to enhance ocular retention time.
8. Validation of Simvastatin Analysis Methods in Human Blood Plasma (In Vitro) Using HPLC-UV Detector
Iyan Sopyan, Cynthia Jaya,
The use of simvastatin (SV) increases along with the increasing number of patients with hyperlipidemia and cardiovascular disease risk factors. Consequently, this condition leads to the increasing need of analytical determination of SV in blood plasma. Analysis of SV in human plasma using protein precipitation method and HPLC with UV detector has not been reported. This research was purpose to find out the rapid, accurate, and valid of SV analysis method in human plasma. In this research plasma samples were treated with protein precipitation method. The analyte was then analyzed using HPLC with C18
column 250×4 mm and 5 µm of particle size, the mobile phase contained of phosphate buffer 0.01 M (pH 4.0) and acetonitrile 30:70 v/v with flow rate 1 mL/minute, and detected at 239 nm. The analysis method was validated based on some parameters, such as selectivity, accuracy, precision, repeatability, linearity, LOD, LOQ, and system suitability. The result showed selectivity represented by Rs was 2.870, repeatability by its CV< 2%, and linearity by its coefficient correlation (r) 0.9992 for concentration range 0.08-0.32 ppm. Based on chromatogram peak area, LOD and LOQ were 0.0132 and 0.0440 ppm respectively, accuracy and precision were 86.25-89.36% and 0.66-1.81% were obtained. The result of system suitability test from retention time and chromatogram peak area showed by its CV < 2%. The analysis method was proved to be valid for SV analysis in human plasma.
9. Formulation and Evaluation of Chitosan-Polyaniline Nanocomposites for Controlled Release of Anticancer Drug Doxorubicin
Dillip Kumar Behera, Kampal Mishra, Padmolochan Nayak
In this present work, chitosan (CS) crosslink with polyaniline (PANI) with montmorilonite (MMT) called as (CS-PANI/MMT) and CS crosslink with PANI without MMT called as (CS-PANI) were prepared by employing the solution casting method. Further the formation of nanocomposites CS-PANI/MMT and CS-PANI were investigated using XRD, FTIR, SEM and tensile strength. Water uptake and swelling ratio of the CS-PANI and CS-PANI/MMT were found to decrease with increase in concentration of clay. Mechanical properties of the CS-PANI and CS-PANI/MMT were assessed in terms of tensile strength and extensibility using texture analyzer. Increase in tensile strength and reduction in extensibility was reported with increase in the nanoclay content. In vitro drug release study on CS-PANI and CS-PANI/MMT indicated pronounced sustained release of doxorubicin by the incorporation of clay particles in the CS polymer matrix. Overall CS-PANI/MMT nanocomposite films exhibited improved mechanical and sustained drug release properties than CS-PANI.
10. Characterization and Release of Ibuprofen in Proniosome System (Ibuprofen-Span 60-Cholesterol)
Tutiek Purwanti, Dewi Melani Hariyadi, Corry Silvia
The aim of this research was to determine influence of proniosome system which consists of ibuprofen-span 60-cholesterol with molar ratio of 2:1:0.75. The proniosome system was made by Coacervation Phase Separation Method, using ethanol 96% as solvent and glycerol 0.1% as aqueous phase. There were two formulas in this research formula I was ibuprofen non proniosome in HPMC gel base and formula II was ibuprofen proniosome in HPMC gel base. Characterization of formulas included organoleptic and pH of ibuprofen gel. Drug release was determined using diffusion cell and cellophane membrane in phosphate buffer pH 6.0 ± 0.05 at temperature 32 ± 0.5 o
C for 7 hours. The drug release (flux) of ibuprofen from formula I and II were 28.3067 ± 3.0852 µg/cm2
and 23.1900 ± 1.7658 µg/cm2
, respectively. The statistical result using independent sample T-test on degree of confident of 95% (α = 0.05) concluded that there was significant value of their fluxs. Research result revealed that release of ibuprofen proniosome system was lower than ibuprofen nonproniosome system in HPMC 4000 gel base.
11. Evaluation of the Physical Stability of Nanostructured Lipid Carrier (NLC) Meloxicam Before and After Strorage 40 Days
Rahmi Annisa, Dewi Melani, Esti Hendradi
Objective: The aims this study was to determine the effect of lipid ratio Monostearin and Miglyol 808 roomates gives the physical stability after storage 40 days. Methods: The NLC making was done by using emulsification method in the formation of NLC meloxicam, 3 different lipid ratios were used, including ratios of 6: 4, 7: 3, 8: 2. Results: NLC meloxicam physical stability of the pH, viscosity, particle size, particle morphology and entrapment efficiency. NLC meloxicam belongs to semisolid preparations with pH value range of 5.72-5.87. Increasing viscosity of NLC system is caused by the increase of solid lipid. The measurement results of particle size of three different lipid formulas indicated that the lipid particle size was <1000 nm. Entrapment efficiency test of all NLC-lipid compositions revealed quite high result (> 80%). Conclusion: The system uses lipid monostearin NLC meloxicam and Miglyol 808 at a ratio of 8: 2 is the most optimal combination shows physical stability after storage 40 days.
12. The Optimization of Maltodextrin and Arabic Gum in the Microencapsulation of Aqueous Fraction of Clinacanthus nutans Using Simplex Lattice Design
Intan Martha Cahyani, Ebta Narasukma Anggraeny, Bekti Nugraheni, Christiana Retnaningsih, V Kristina Ananingsih
The aqueous fraction of Clinacanthus nutans
leaf extracts contains flavonoids which known had antioxidative properties. To improve acceptability, this viscous and bitter aqueous fraction was microencapsulated using maltodextrin and Arabic gum. This research aims to discover the effectivity of maltodextrin and Arabic gum and the concentrations for optimum microencapsulation. Optimization design was done using Design Expert with simplex lattice design with ratios of 1:0; 0.75:0.25; 0.5:0.5; 0.25:0.75 and 0:1. The evaluations done to the results were microcapsule yield, moisture content, flow rate, and antioxidant activity. The optimum ratio of maltodextrin and Arabic gum was obtained at 0.806:0.194 with 1.49% moisture content, flow rate 4.375 g/s and antioxidant activity at the value of 842,499 ppm. The result of one-sample T-test showed that the prediction result of Design Expert did not differ significantly from the experiment result. From the data, it was concluded that the resulting equation was valid.