International Journal of

Drug Delivery Technology

ISSN: 0975 4415

Peer Review Journal

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1. Development of An Antidiabetic Phytocomposite Loaded Phytoceutical Formulation, Its Quality Control and Pharmacokinetic Studies and Establishing In Vitro- In Vivo Correlation
De Baishakhi, Bhandari Koushik, Katakam Prakash, Adiki K Shanta, Mitra Analava
This study reports the development of solid oral phytoceutical formulations with Phytocomposite (PHC), an antidiabetic poly herbal preparation as the active core material. Spherical, monolithic PHC microspheres of size range (10 -100 µm) were obtained with Hausner ratio, Carr’s index and angle of repose of 1.141± 0.010, 12.418±0.769 and 25.17±0.96 respectively. Encapsulation efficiency amongst different batches (F1-F5) ranged from 96.8- 100.7, with 99% release profile up to 12h. Conventional and sustained release tablets were prepared by direct compression and compatibility amongst polymers and the PHC checked by FTIR studies. Natural polymers viz. gum kondagogu, gum karaya, Aegle marmelos gum were used as release retardant. Optimized batch of conventional tablets (F6) showed 99.8 % release in 35 min and optimized batch of PHC-SR tablets (F12) showed 99.9% release at 12th hr, both followed zero order kinetics and non-Fickian diffusion. These optimized formulations were subjected to stability studies and the similarity factors (f2) of the conventional and SR tablets were 88.75 and 66.76 respectively. Pharmacokinetic parameters of three formulations in rat plasma were analyzed by PK Solver 2.0. In vitroin vivo correlation (IVIVC) of three different formulations showed Level A correlation in all cases.

2. Understanding the Impact of Polymer Ratio and its Concentration on Omeprazole Release from Matrix Tablets: Response Optimization Study
Tiwari R, Tiwari G, Wal P, Wal A, Maurya P
In present study, matrix tablets of Omeprazole (OPZ) were formulated by wet granulation technique using a combination of hydroxyl propyl methyl cellulose (HPMC K15M) and ethyl cellulose (EC) in varying ratios and the effect of polymer ratio as well as their concentration on drug release profile was investigated. Response surface methodology (RSM) was conducted to optimize matrix tablets. Compressed tablets were evaluated for hardness, friability, weight variation, drug content and in vitro dissolution studies. The dissolution study was performed in pH1.2 for the first 2 h and in phosphate buffer (pH 7.4) for another 5 h. The optimized formulation was compared with other formulations using similarity (ƒ2) and dissimilarity factor (ƒ1) test. The results of RSM indicated that both X1 (the blending ratio of HPMC K15M K15M and Carbopol 934P 934P) and X2 (polymer blend concentration)have significant effect on in-vitro drug release profile. Hardness, friability, weight variation and drug content were found to be in desired range. Among different formulations, matrix tablets prepared by HPMC K15M and Carbopol 934P 934P (7:3) with 15% polymer blend concentration displayed 98.85% OPZ release in 7 hr. and release kinetic was higuchi (r2= 0.9884). Similarity (f2) and dissimilarity (f1) factors demonstrated that the in vitro profiles were not similar. Finally, it was concluded that release rate of OPZ decreased proportionally with increasing polymer ratio (HPMC K15M: Carbopol 934P 934P) and decreasing polymer blend concentration.

3. Development and Validation of a Simple HPLC-UV Method for The Quantification of Andrographolide In Rabbit Plasma
Syukri Y, Widarno I S, Adewiyah A, Wibowo A, Martien R, Lukitaningsih E, Nugroho A E
In this present work, a simple, rapid and accurate HPLC-UV method has been developed for the quantification of andrographolide in rabbit plasma. The assay was performed using an XTerra® MS C18 column (150 mm X 4.6 mm, 5 μm) with a mobile phase of methanol and water (60:40), at 0.8 mL/min flow rate and UV detection of 229 nm. Andrographolide was extracted from a biological sample by applying acetonitrile as a precipitating and extraction solvent. The results showed a good linearity with r = 0.9992;  the accuracy reported as % diff was found to be -6.42 – 6.55 % while the recovery was 99.09, 98.55, and 105.14%  for low, medium and high spiked plasma, respectively. The precision (reproducibility) reached 1.08–3.20 % RSD for the sample studied. The 2.87 % relative standard deviation (RSD) value for selectivity test indicated a good selectivity of the developed method. The developed method is simple and rapid, so that it can be applied for the quantification andrographolide in animal models during pharmacokinetics studies.

4. Bosentan Monohydrate Vesicles Loaded Transdermal Drug Delivery System: In Vitro In Vivo Evaluation
Revathi M, Indira Muzib Y
This study elucidates the enhancement of the permeation of bosentan monohydrate through skin by encapsulating it in vesicles loaded transdermal delivery system. Niosomal vesicles were formulated by ether injection method. Formulation FN7 (span 60: cholesterol: poloxamer 401, 1.25:1:0.25) showed maximum entrapment efficiency of 96.7±0.037% and was optimized for loading in to transdermal system. Transdermal systems were formulated using both hydrophilic and hydrophobic polymers like HPMC, HEC and EC. Formulation F1 with HPMC was optimized based on in vitro release (99.21±1.45 %) and was further evaluated for ex-vivo permeation. The results indicate that the ex vivo release (98.13±1.65%) was as par with in vitro release and followed zero order super case- II transport mechanism. The in vivo studies were done on New Zealand male rabbits for oral and transdermal route. The results inferred no significant change in half-life of drug but a substantial difference in Tmax, AUC and MRT was observed in transdermal systems. A two fold increase in AUC was observed in transdermal route (18.609±7.251µg/ml/h) when compared to oral route (9.644±5.621µg/ml/h). A controlled release was attained up to 35h and reservoir effect was observed and this may be due to the barrier properties of skin. Drug encapsulated niosomes were released in to the skin by loosening the lipid layers and the surfactant acted as penetration enhancer. The study infers that niosomes loaded transdermal patches of bosentan monohydrate can enhance the bioavailability and provided controlled release for better therapeutic efficacy and safety of drug.

5. Virgin Coconut Oil as Oil Phase in Tretinoin Nanoemulsion
Tristiana Erawati M, Retnowati, Amalia Wardatul F, Widji Soeratri
This study was aimed to determine the characteristic and tretinoin release in nanoemulsion using virgin coconut oil (VCO) as oil phase compared with emulsion. The characteristics of the tretinoin nanoemulsion (TN) were observed in terms of droplet morphology by Transmission Electron Microscopy (TEM) and droplet size by particle analyzer and light microscope and the pH value by pH meter. The release rate of tretinoin in nanoemulsion and emulsion was measured by Franz diffusion cell using cellophane membrane. Result of this research showed the droplet morphology of tretinoin nanoemulsion and emulsion were spherical. The droplet size of tretinoin nanoemulsion (72.57 ± 18.16 nm) was smaller than tretinoin emulsion (10.54 ± 0.61 mm). The pH value of tretinoin nanoemulsion and tretinoin emulsion was 6.24 ± 0.01 and 6.21 ± 0.02. In interval times 5 – 60 minutes the tretinoin release rate (flux) in nanoemulsion was 0.158 ± 0.016 µg/cm2/minute higher than in emulsion which was 0.048 ± 0.016 g/cm2/minute. In interval times 60 – 180 minutes, tretinoin release rate (flux) in nanoemulsion was 0.046 ± 0.005 g/cm2/minute lower than in emulsion which was 0.090 ± 0.016 g/cm2/minute. In interval times 180 – 720 minutes the tretinoin release rate (flux) in nanoemulsion was 0.025 ± 0.001 g/cm2/minute which had no significant different compared to in emulsion which was 0.022 ± 0.002 g/cm2/minute. The statistical analysis of the tretinoin release rate value using independent T-test result was known that there were significant different between nanoemulsion (TN) and emulsion (TE).  Conclusion: The droplet size of tretinoin nanoemulsion was below 100 nm, pH value 6.24 ± 0.01 and the tretinoin release rate in nanoemulsion using VCO was higher than in emulsion.

6. Improved Solubility and Dissolution Rate of Ketoprofen by Beta Cyclodextrin Ternary Complexes Incorporating Hydrophilic Polymers
Mohammed Jafar, Sadath Ali, Hassan Mahmoud Ghonaim
The aim of the presentstudy wasto improve the aqueous solubility and dissolution rate of a BCS Class-IIdrug,ketoprofen by β-cyclodextrin ternary complexes incorporating hydrophilic polymers polyethylene glycol 6000 (PEG6000) and polyvinyl pyrrolidone (PVP). Initially,ketoprofen (KPF)binary complexes with β-Cyclodextrin (βCD)wereformulated by physical mixing,co-grinding, and solvent evaporation methods which was followed by ternary complex formulation of selected KPF-βCD binary complex incorporatingPEG6000 and PVP.The solvent evaporation method was used in the formulation of ternary complexesof ketoprofen, sincein the beginning of this study, it was proved to be the best methodcomparatively in yielding promising binary complexes of ketoprofen.Ketoprofen formed 1:1 M stoichiometric binary and ternary inclusion complexes as demonstrated by the AL-type of phase solubility graph. An increase in the stability constant value  (Kc) of  KPF- βCD complex in the presence of PEG6000 and PVP conceded higher complexation competency. FTIR and SEM studies evidenced the perfect ternary inclusion complex formation. Ternary complexes showed improved drug dissolution compared with Ketoprofenalone and KPF-βCD binary complex. The ternary complex containg 1:1:2 molar ratio of KPF:βCD:PEG6000exhibited 94.24% drug dissolution in 2 hours, which was significantly high in relation to ternary complexes containg PVPand it was found to follow first order release mechanism. Complex studied for stabilityshowed no significant change in physical appearance, drug content and drug dissolution characteristic indicating high stability.

7. Acyclovir Loaded Solid Lipid Nanoparticle Based Cream: A Novel Drug Delivery System
EL- Assal M I A
Objective of the present investigation was enthused by the possibility to develop solid lipid nanoparticles (SLNs) of hydrophilic drug acyclovir. Also study vitro and vivo drug delivery. Methods: Drug loaded SLNs (ACV-SLNs) were prepared by high pressure homogenization of aqueous surfactant solutions containing the drug-loaded lipids in the melted or in the solid state with formula optimization study (Different lipid concentration, drug loaded, homogenization / stirring speed and compritol 888ATO: drug ratio). ACV – SLN incorporated in cream base. The pH was evaluated and rheological study.  Drug release was evaluated and compared with simple cream- drug, ACV – SLN with compritol 888ATO and marketed cream. The potential of SLN as the carrier for dermal delivery was studied. Results: Particle size analysis of SLNs prove small, smooth, spherical shape particle ranged from 150 to 200 nm for unloaded and from 330 to 444 nm for ACV loaded particles. The EE% for optimal formula is 72% with suitable pH for skin application. Rheological behavior is shear thinning and thixotropic. Release study proved controlled drug release for SLNs especially in formula containing compritol88 ATO. Stability study emphasized an insignificant change in SLNs properties over 6 month. In-vivo study showed significantly higher accumulation of ACV in stratum corneum, dermal layer, and receptor compartment compared with blank skin. Conclusion: AVC-loaded SLNs might be beneficial in controlling drug release, stable and improving dermal delivery of antiviral agent(s).

8. Anticancer Activity of Mixed Doxorubicin and Pravastatin in Nanoemulsions Against HCT 116 Colon Cancer Cells
Mayson H Alkhatib, Duaa K Zahim, Wadiah S Backer
Combining drugs with different mechanism of action in nanocarriers is becoming a promising strategy in cancer therapy. In the present study, the anticancer activity of the combination of doxorubicin (DOX) and pravastatin (PRV) loaded in nanoemulsions (NEs) was evaluated in HCT 116 colon cancer cells. The NE formulas (NEa and NEb) consisted of different weight fractions of the surfactant mixture of Eumulgin HRE 40/ Soya phosphatidylcholine/ sodium oleate at a fixed weight ratio of 3.5:3.0:3.5, cholesterol (CHO), Tris- HCl buffer (pH 7.22), and 1-octanol. The cytotoxicity of the drug formulas, loaded in either water or NEs, was assessed through 3-(4, 5 Dimethylthiazole- 2-yl)-2, 5-diphenyl tetrazolium bromide (MTT) assay, while the mechanism of cell death was determined by observing the morphological changes of treated cells under light microscope and identifying apoptosis by using the ApopNexin FITC  kit and DAPI nuclear staining. It has been found that reducing the concentration of DOX from 15 to 7.5µM by formulating it with 7.5µM of PRV in NEa (NEa (1 DOX:1 PRV)) has preserved its cytotoxicity against HCT-116 cancer cells. The present study proved that the combination of the PRV and DOX loaded in NEa formulations improved the therapeutic potential of both of PRV and DOX as anticancer drugs.

9. Photostability Study on Character and Antioxidant Activity of Tomato Extract (Solanum lycopersicum l.)  in Nanostructured Lipid Carrier (NLC) and Conventional Creame
Noorma Rosita, Dewi Melani Haryadi, Tristiana Erawati, Rossa Patria Nanda, Widji Soeratri
The aim of this study was to investigate the ability of NLC in increasing photostability of tomato extract in term of antioxidant activity. Photostability testing on antioxidant activity of samples were conducted by accelerating method using UVB radiation 32.400 joule for 21 hours radiation. Antioxidant activity was measured by DPPH method. NLC was made by High Shear Homogenization (HPH) method at 24000 rpm for 4 cycles, while conventional creame was made by low speed at 400 rpm. The product were characterized include: pH, viscosity, and particle size. There were had difference characters and physical stability.  NLC had smaller size, more homogenous  and more stable than conventional creame. It was known that stability of antioxidant activity of tomato extract in NLC system higher than in conventional creame. That was showed with k value, as constanta of rate scavenging activity decreasing in antioxidant power between time (Sigma 2-tail < 0.005) of NLC and conventional creame were: 2.03×10-2 %/hour ±0.08 (3.94) and 4.71x 10-2 %/ hour ±0.23 (4.88) respectively.

10. Design and Evaluation of Chronotherapeutic Delivery of Terbutaline Sulphate by Pulsincap Technology
Sreejan M, Krishnaveni V, Sai Padmini K, Satyavathi K, Bhojaraju P, Madhubabu M
The aim of the present research was to develop pulsincap formulation of terbutaline sulphate for chronotherapeutic colon targeted delivery. Formaldehyde treatment was done to increase the disintegration time of capsule body. Hydrogel plug was prepared by combining hydrophilic and hydrophobic polymers to obtain the exact degree of swelling. Based on the disintegration time of the capsule bodies, M3 formulation was selected for preparation of pulsincap. The powder blend was prepared by varying the concentration of sodium starch glycolate and sodium bicarbonate concentration with terbutaline sulphate. The pulsincaps were formulated with the optimized concentration of sodium starch glycolate and sodium bicarbonate sealed with prepared hydrogel plug. FTIR study confirms that there was no incompatibility between terbutaline sulphate and polymers. The drug content was estimated by using pH 7.4 buffer solution and it was found to vary between 97.37 ± 0.67 % to 100.45 ± 0.25 %. The swelling study was carried out by using three different buffer solutions and found in the range of 50.12 ± 0.21 %to 56.75 ± 0.61 %. Formulation F9 was found to have the desired time dependent drug release pattern, and hence was considered as the optimized formulation. From this study, it can be concluded that the pulsincap formulation can serve as a useful technique for time dependent colon targeted delivery of terbutaline sulphate.

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