Current Issue : January - March Volume : 2016 Issue Number : 1 Articles : 4 Articles
The purpose of this research was to develop the microemulsion based in situ gelling system containing moxifloxacin for prophylaxis and treatment of the posterior segment diseases like endophthalmitis. Moxifloxacin is well reported for the treatment of endophthalmitis, it has better penetration into ocular tissues and high potency compared to many of the same class drugs. Unlike halogenated fluoroquinolones it is safe to use in higher dose and is devoid of phototoxicity. So, moxifloxacin was used as a model drug. Formulation approach provides better absorption, penetration, retention and improves bioavailability of the drug. The average conc. reached into vitreous humor from topical microemulsion in situ gelling formulation was ~0.4 µg/ml, which is far more than concentration required for therapeutic effect (i.e. > 0.047 µg/ml or >>MIC90 for S. epidermidis, a pathogen commonly responsible to cause endophthalmitis). Thus, novel microemulsion based in-situ gelling formulation could be potential drug delivery system for treatment of posterior segment diseases like endophthalmitis....
Vinpocetine (VNP) is a nootropic agent used in cerebrovascular disorders and dementia. Its bioavailability is irregular and irreproducible, due to its low solubility in the intestine and extensive first pass metabolism. The objective of our work was to prepare VNP in a self-nano-emulsifying drug delivery system (SNEDDS) and then convert it into solid-SNEDDS (S-SNEDDS) that have acceptable characteristics for tablet compression. Those tablets could be transformed into osmotic systems to control the drug release. SNEDDS composed of 10% Maisine™ 35-1, 50% Cremophor® EL and 40% Transcutol® HP was the system of choice with drug to system ratio of 2.5 mg: 0.25 gm. Its particle size was 16.97±0.32 nm and zeta potential was -12.65±4.39 mV. S-SNEDDS, loaded on Aeroperl®, possessed good flow properties; angle of repose (26.02±0.79), Hausner’s ratio (1.067±0.02) and compressibility index (6.347% ±1.37). Elementary osmotic pump (EOP) tablets and controlled porosity osmotic pump tablets (CPOP) were prepared and the in-vitro release of VNP from both systems showed promising results. Therefore, VNP loaded S-SNEDDS was successfully prepared with improved VNP solubility which might resolve its bioavailability problem then formulated into osmotically controlled dosage form to control drug release....
Buccal delivery of drug provides an alternative to the oral route of drug administration for the drugs that undergo first pass metabolism. This work was concerned with the formulation and in-vitro evaluation of eletriptan hydrobromide mucoadhesive buccal tablets. Eletriptan is used in the treatment of migraine. The objective of this study was to improve the bioavailability of the drug with reduction in dosing frequency and side effects. The tablets were prepared by direct compression method. Nine formulations were developed with varying concentrations of polymers like chitosan, sodium alginate and HPMC. FTIR studies showed no evidence on interaction with drug, polymers and excipients. The tablets were tested for weight variation, hardness, surface pH, drug content uniformity, swelling index, mucoadhesion strength and in-vitro drug release study. The in-vitro drug release profile showed that formulation (F8) which contains polymers such as chitosan and sodium alginate exhibited sustained drug release for 8 hours. The in-vitro release kinetics reveals that the formulation (F8) follows zero order and the mechanism of drug release was non-fickian....
Minoxidil as topical solution in aqueous vehicle for treatment of alopecia has a drawback of limited contact time with the scalp. Hence there is a need for suitable topical drug delivery system which would increase the contact time leading to an increase in local drug concentration and therapeutic effect. The aim of the present study was to formulate, develop and evaluate minoxidil gel for enhanced topical drug delivery using a suitable method which will prevent the formation of polymer-minoxidil complex. Formulations were prepared by using carbopol 934, carbopol 941, carbopol 974 and acupec HV 505 HC as gelling agent. The prepared formulations were evaluated for appearance, pH, drug content, viscosity, spreadability and in-vitro diffusion studies. The developed formulations were found to be stable, non-irritant to albino mice. The in-vitro drug release was found to be 97.71% over a period of 8 hrs. The similarity factor (f2) was found to be 73.48 for optimized formulation indicating that the release was similar to that of marketed formulation (Tugain 2%). The hair growth initiation time and hair growth completion time of optimized formulation was found to be 8 and 22 days respectively. The average hair length measured on 14th, 21st and 28th day after applying optimized formulation were found to be 9.90±0.20 mm, 14.67±0.19 mm. and 18.90±0.18 mm. In-vivo studies revealed that the optimized formulation was as effective as marketed formulation for topical delivery of minoxidil....
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