FORMULATION AND EVALUATION OF SIMVASTATIN LOADED MICROEMULSION BASED GEL: IN VITRO CHARACTERIZATION

M. Saifee, Pragati Bhaske, Reshma Toshniwal
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Abstract

The Simvastatin loaded microemulsion based gel was formulated and in-vitro evaluation was done for the treatment of diabetic wound healing. Simvastatin is BCS class II drug which promotes wound healing by increasing the production of vascular endothelial growth factor (VEGF). Microemulsions (MEs) are oil and water colloidal system stabilized by the mixture of surfactant and co-surfactant offering enhance skin permeability for both hydrophobic and hydrophilic drugs. At first, microemulsion (ME) was prepared by water titration method and the existence of ME region was determined using pseudo-ternary phase diagram. Formulations were prepared using oil (oleic acid), Tween 80 and PEG 400 as surfactant and co-surfactant. Optimization of formulation was done using 32 factorial designs. Carbopol 940 was used as gelling agent for preparing microemulsion gel. The formulations were evaluated for physical appearance globule size, polydispersity index, zeta potential, percent transmittance, thermodynamic stability, dilution test, drug content, and in vitro drug release. The optimized formulation of ME showed average globule size of 151 nm and the optimized ME gel had a homogeneous texture, showed good spreadability and in vitro drug release. The present study indicates the simvastatin loaded microemulsion gel could act as promising vehicle for topical drug delivery of drug for diabetic wound healing.
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辛伐他汀微乳凝胶的制备与评价:体外表征
制备了辛伐他汀微乳凝胶,并对其在糖尿病创面愈合中的作用进行了体外评价。辛伐他汀是BCS II类药物,通过增加血管内皮生长因子(VEGF)的产生来促进伤口愈合。微乳是一种由表面活性剂和助表面活性剂混合稳定的油水胶体体系,对疏水和亲水药物都具有增强皮肤渗透性的作用。首先采用水滴定法制备微乳液,并用伪三元相图确定微乳液区是否存在。以油(油酸)、Tween 80和peg400为表面活性剂和助表面活性剂制备了配方。采用32因子设计对配方进行优化。以卡波波尔940为胶凝剂制备微乳液凝胶。考察了制剂的物理外观、粒径、多分散性指数、zeta电位、透光率、热力学稳定性、稀释试验、药物含量和体外释放度。优化后的ME凝胶平均粒径为151 nm,结构均匀,具有良好的涂敷性和体外释药效果。本研究表明,辛伐他汀微乳凝胶可作为糖尿病创面局部给药的载体。
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