Development of amphotericin b Based organogels against mucocutaneous fungal infections

Amphotericin B is a broad spectrum antifungal agent used to treat fungal infections. Organogel is a semisolid preparation in which the apolar phase gets immobilized within spaces of the three-dimensional structure. The current study aimed at the formulation and comparative evaluation of sorbitan monostearate organogels and pluronic lecithin organogels (PLO). Different compositions of span 60 based organogels were prepared by varying the concentrations of the span 60 and PLO gels were prepared by varying the concentration of Pluronic F 127. The developed organogels were subjected to various characteristics such as pH, viscosity, spreadability, extrudability, and drug release studies. The optimized formulations were evaluated against Candida albicans and carried out ex vivo release study. The optimized formulation was selected from span 60 based organogels, and pluronic lecithin organogels were S1 and P1, respectively. The optimized formulation (S1) showed effective inhibition against Candida albicans. The skin irritation test was carried out on albino mice for optimized formulations and results showed that no irritation to the skin. Based on the results, organogels prepared by sorbitan monostearate showed better antifungal activity, and also all the formulations were found to be stable and safe throughout the study period.

两性霉素B（Amphotericin B）是一种广谱抗真菌药物，用于临床治疗真菌感染。有机凝胶（Organogel）属于半固体制剂，其非极性相可被固定于三维网络结构的孔隙内。本研究旨在制备单硬脂酸山梨坦有机凝胶与泊洛沙姆卵磷脂有机凝胶（Pluronic Lecithin Organogels, PLO），并对两类凝胶开展对比评价。研究中，通过调节司盘60（Span 60）的用量，制备了一系列不同配比的司盘60基有机凝胶；同时通过改变泊洛沙姆F127（Pluronic F 127）的浓度，构建了泊洛沙姆卵磷脂有机凝胶体系。对所制备的所有有机凝胶样品，依次开展了pH值、黏度、铺展性、挤出性及药物释放行为等多项表征与评价。针对筛选得到的最优处方，本研究进一步开展了针对白色念珠菌（Candida albicans）的抑菌活性测试，同时完成了离体释药实验。本次研究分别从司盘60基有机凝胶与泊洛沙姆卵磷脂有机凝胶中筛选出最优处方S1与P1，其中最优处方S1对白色念珠菌展现出显著的抑菌效果。此外，本研究以白化小鼠为动物模型，对最优处方开展了皮肤刺激性试验，结果显示该处方无皮肤刺激性。综合全部实验结果可知，由单硬脂酸山梨坦制备的有机凝胶具备更优异的抗真菌活性，且所有受试处方在整个研究周期内均表现出良好的稳定性与安全性。