Current Issue : January - March Volume : 2015 Issue Number : 1 Articles : 8 Articles
Over the past few decades there has been growing interest to develop novel drug delivery systems. The system uses to minimize drug degradation and loss, to prevent harmful side-effects and increase drug bioavailability. Among drug carriers one can name oil-in-oil emulsion. Oil-in-oil (O/O) emulsion could be useful for where some drugs are either unstable in the presence of water or are insoluble in water. The present work is to develop oil-in-oil emulsion for topical delivery of ketoconazole as antifungal drug which gives controlled release with anhydrous vehicle to deliver lipophilic or hydrolytically unstable drugs. The potential components of (O/O) emulsion were castor oil, silicone oil and surfactant, among the surfactant studied only silicone emulsifier was more effective in formulating castor-silicone emulsion. Optimization of formulation factor was achieved using Box-Behnken experimental design. The variables selected include phase volume ratio, surfactant concentration and stirring time. (O/O) emulsion prepared in very less time by hand stirring spontaneous mixing of both phases. Viscosity of formulation was found to be 167.51 cPs. The globule size was found to be 4.56 µm. volume distributions 8.18 µm through intensity distribution. Ketoconazole were solubilize in the internal castor oil phase and their release from emulsion across a dialysis membrane into phosphate buffer pH 5.5 was recorded 29.76% cumulative drug is released within a period of 8 hrs....
The present study was aimed at the overall improvement in the efficacy, reduction in toxicity and enhancement of therapeutic index of 5-fluorouracil. Magnetically responsive biodegradable microparticulate delivery system of 5-fluorouracil has been developed by phase separation emulsion polymerization technique by using bovine serum albumin. The formulations were evaluated with respect to particle size analysis, entrapment efficiency, magnetite content, in-vitro magnetic responsiveness, in-vitro drug release studies, in-vivo drug targeting studies and stability studies. The formulated magnetic microspheres were found to be spherical with average particle size of 3-12 µm in diameter and incorporation efficiency up to 56.37. Result of X-ray diffractrometry confirmed the presence of magnetite in prepared 5-fluorouracil magnetic microspheres. The total percentage of Fe2O3 in the microspheres was found to be 42.53 to 55.48. In-vitro drug release after 24 hours was 89.60, 82.22, 78.41 and 76.35 for formulation F1, F2, F3 and F4 respectively. Results of in-vitro magnetic responsiveness and in-vivo tissue targeting proved that the retention of microspheres in presence of magnetic field was significantly high than those in the absence of the magnetic field. Stability studies revealed that 4°C is the most suitable temperature for storage of 5-fluorouracil loaded magnetic microspheres. Overall, this study shows that the magnetic albumin microspheres can be retained at their target site in-vivo, following the application of magnetic field and are capable of releasing their drug content for an extended period of time....
Fluticasone propionate (FP) is most often used for the treatment of several skin disorders due to its anti-inflammatory and anti proliferative effect. The aim of the present study was to formulate hydrogel of FP using combination of carbopol 934 and HPMC K4M in different concentration of 0.5, 0.75 and 1% (w/w). FP hydrogel formulations (G1-G9) were evaluated for pH, viscosity, spreadability, drug content, ex-vivo diffusion study and skin irritation study. The spreadability of G1-G9 was found in the range of 4.6-6 cm/s indicating good spreadability. The drug content of G1-G9 was found in the range of 91.4-95.7%. Cumulative % drug release of G1-G9 was in the range of 29.23-26.83%. FP hydrgel (G9) containing 1% carbopol 934 and 1% HPMC K4M showed 26.83% diffusion indicating sustained release of FP as compared to other batches. From skin irritation study it was revealed that as none of the hydrogel formulation resulted into skin irritation, FP hydrogel can be easily accepted for topical application. FP hydrogel due to sustained drug release and non irritation can be used for the treatment of several skin disorders....
The purpose of present study was to develop quality based formulation of gelrite based ophthalmic in-situ gel of olopatadine hydrochloride using HPMC E15LV polymer. The in-situ forming gel was prepared by using different concentration of gelrite. The effects of various experimental parameters were optimized by means of experimental 32 designs. Formulations were evaluated for their pH, clarity, gelation studies, viscosity, mucoadhesion index, gel strength and in-vitro drug release. Olopatadine hydrochloride containing gelrite, HPMC K15LV exhibited non-newtonian flow behavior. pH, clarity and gelation studies were found in acceptable range. From 32 optimization, gelrite was found to have significant effect on mucoadhesion index. Gelrite showed a positive effect on gel strength. HPMC K15LV was also helpful in controlling the release rate of drug. Optimized batch (F9) containing 0.5% gelrite 0.3% HPMC K15LV was exhibited all tests in acceptable limits....
The aim of the current work was to develop stable formulation of rizatriptan benzoate in the form of floating matrix tablet, in combination with two different polymers hydroxy propyl methyl cellulose (HPMC K4M) and Eudragit RLPO. The Rizatriptan benzoate in a form of gastro retentive floating sustained release dosage forms, which provides enhanced bioavailability. In the present study rizatriptan benzoate controlled release tablet were prepared with the help of the direct compression method, using sodium bicarbonate and citric acid as the gas forming agent. Rizatriptan benzoate is an antimigraine drug. The plasma half-life of drug is approximately 2-3 Hrs. The tablets were evaluated for the pre and post compression parameters such as FTIR spectroscopy, differential scanning calorimetry, weight variation, thickness, friability, hardness, drug content, in-vitro buoyancy studies, in-vitro dissolution studies and stability studies and results were within the limits. The in-vitro dissolution studies were carried out in a USP type-II apparatus in 0.1 N HCl. Among all the formulations (F1 to F9) prepared, batch F3 was the best formulation which showed buoyancy lag time 18 sec and the tablet remained buoyant for > 12 h. The in-vitro data is fitted in to different kinetic models and the best-fit was achieved with the higuchi model. Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) were performed to identify the physicochemical interaction between Rizatriptan benzoate and the polymer. The in-vitro drug release from the tablets was found to have 75.81±0.16% to 99.43±0.18% for 12 hr. Stability study was performed on the optimized formulation F3 at 40°C/ 75% RH for 3 months....
The liquid crystalline drug delivery is gaining much attention in cosmetic, chemical industries and also in the field of pharmacy. It has emerged as promising drug delivery of hydrophobic and hydrophilic drugs and excellent vehicle for drug delivery. The available prospective are increased permeability, solubility, bioadhesive nature and sustained release of various bioactive molecules. This article gives an overview of recent advances and current status of lyotropic liquid crystal as platform for drug delivery especially with respect to their preparation methods and applications....
Aim of the present study was to optimize and evaluate famotidine in situ gel by using gellan gum as gelling agent. Two level three factor full factorial design was employed to study the effect of independent variables concentration of gellan gum, calcium carbonate (X2) and sodium citrate (X3) on dependent variables viscosity (Y1) and drug content (Y2). The different concentration of gellan gum, sodium citrate and calcium carbonate changes the gel characteristics....
This study describes a 32 full factorial experimental design to optimize the formulation of atorvastatin loaded lipid nanoparticles by the high speed homogenization followed by probe sonication method. The variables drug:lipid ratio and concentration of liquid lipid were studied at three levels and arranged in a 32 factorial design to study the influence on the response variables particle size and % entrapment efficiency. From the statistical analysis of data polynomial equations were generated. The particle size and % entrapment efficiency for the R1 to R9 batches showed a wide variation of 111.11-310.76 nm and 60.64-90.42%, respectively. The atorvastain-loaded lipid nanoparticles were evaluated for particle size, entrapment efficiency, differential scanning calorimetry, fourier transform infra-red spectroscopy, X-ray diffraction and in-vitro drug release study. The optimized batch was selected from the data obtained from grid search and numerical optimization which showed an average particle size of 133.08 nm and entrapment efficiency of 92.46%. The total drug release from lipid nanoparticles in phosphate buffer pH 7.4, in 10 hours is 20.96% which indicates that the release of atorvastatin from lipid nanoparticles is sustained for longer period of time, which is required for its therapeutic action....
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