Cutaneous Tuberculosis is also known as dermal tuberculosis or tuberculosis cutis (extrapulmonary tuberculosis) which can occur in any age group and patients who may or may not be suffering from pulmonary tuberculosis. The current treatment given for the disease is oral therapy of anti-tubercular drugs which has many side effects such as hepatotoxicity, headache, anxiety, euphoria, insomnia, eosinophilia, hepatitis. Hence to avoid these side effects and to increase efficiency of current therapy a topical proniosomal gel of isoniazid was formulated. Coacervation phase separation method was used and proniosomal gel was formulated by using Span 20, soya lecithin, and cholesterol. Optimum concentration of 3 factors Span 20, soya lecithin, and cholesterol were determined using Box Behnken design with at 2 levels and vesicle size and entrapment efficiency as responses. The optimized proniosomal gel was characterized by vesicle size, entrapment efficiency, transmission electron microscopy (TEM), in vitro drug release, skin retention studies, skin irritation studies and stability studies. The optimised batch showed vesicle size of 2.27±1.82 µ, and entrapment efficiency of 98.15±0.25 %. The optimised formulation was stable under refrigeration condition (5°C) in amber coloured bottle, was non-irritating and showed 98.10±1.28 % release and 85±1.53 % permeation after 6 h and 436±12 µg drug was retained in the skin after 3 hrs.
Fluconazole is a synthetic antifungal drug, belonging to triazole group and mostly used to treat oral candidiasis caused by the yeast Candida albicans. Fluconazole commercially available in tablets that offer poor bioavailability, due to hepatic first pass effect and gastric instability leads to frequent dosing. Buccal drug delivery can bypass such problems of tablet and leads to increase in bioavailability. Due to low molecular weight, fluconazole can suitably administered by buccal route, hence local and targeted action can achieve. The present study was conducted to develop proniosomal gel of fluconazole by coacervation phase separation method using Span 20, cholesterol, soya lecithin, ethanol and aqueous vehicle. Based on preliminary studies surfactant and aqueous vehicle was selected. The Box Behnken design was employed to optimized proniosomes by evaluating responses like entrapment efficiency, vesicle size and drug release. The optimized proniosomes were evaluated with entrapment efficiency (96.83%), vesicle size (2µm), in vitro drug release 85.66 % (3 h) and ex vivo mucosal permeation (85.67 %) with flux (394.09 μg/cm 2 h). The optimized proniosomes were incorporated into 2% w/w Carbopol gel 934 (1:1) to obtain proniosomal gel. This optimized proniosomal gel was found with good viscosity, good spreadability and adhesiveness, also it shows maximum drug release and permeation as compared to plain gel of fluconazole. In microbiological studies, optimized formulation shows the maximum inhibitory effect as compared to plain gel of drug, which concluded that optimized proniosomal gel exerted local and targeted buccal delivery with good fungistatic effect than plain gel of fluconazole against Candida albicans.
There are various approaches commonly used for gastric retention, one of which is raft forming system. Floating oral in situ gel is a type of raft forming system. The present work concerns with the formulation, evaluation and optimization of floating oral in situ gel of Itopride Hydrochloride for controlled release. Gellan gum has been used as a gel forming polymer and calcium carbonate as cross linking agent and Ca 2+ ion source, and HPMC K100M as release retardant. The floating oral in situ gel undergoes gelation by ion sensitive mechanism. In this formulation 3 2 factorial designs was performed and the effect of variation in concentration of gellan gum and HPMC K100M on drug release at 1 h, 6 h, and viscosity was evaluated. The gel was evaluated for other parameters like floating lag time, floating duration, gel strength, density, pH, in vitro drug release, drug content, and in vitro gelling capacity. The results of 3 2 full factorial design revealed that the concentration of gellan gum and of HPMC K100M significantly affected the dependent variables i.e. drug release at 1 h, at 6 h, and viscosity. A controlled release profile was observed for these formulations. The drug release mechanism was found to follow Korsmeyer-Peppas model. In vivo studies revealed higher T max of gel compared to plain drug which is suggestive of slower absorption. However the AUC 0-12 h was found to be nearly 90% higher than plain drug.
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