Sudhakar Beeravelli, Varma J N Ravi, Murthy K V Ramana
Department of Pharmaceutical Technology, A.U. College of Pharmaceutical Sciences, Andhra University, Visakhapatnam, Andhra Pradesh, India-530003.
Curr Drug Deliv. 2014;11(4):521-30. doi: 10.2174/1567201810666140109113830.
The goal of effective treatment for dermal fungal infections could be highly beneficial by the delivery of antifungal drugs on skin from liposomal application. Topical delivery involves minimizing the flux of the drug through the skin while maximizing its retention on the skin. The aim of the present work was the investigation of the effects of lipids and cholesterol for the development of liposomal formulations as potential carriers for antifungal agent terbinafine HCl. Phospholipon 90H (hydrogenated phosphatidylcholine) and dimyristoylglycero-3-phosphocholine (DMPC) along with cholesterol were used for preparation of liposomes by ethanol injection method and characterized for drug content, entrapment efficiency, size, zetapotential, vesicle morphology, stability, FTIR, in vitro and ex vivo drug retention studies.
Drug entrapment ranged between 39.46±0.91% to 70.39±0.71%. Vesicles showed good morphological characters with a narrow size distribution, in the size range of 206.9 to 344.8 nm. Gum karaya gel loaded with liposomal dispersion showed prolonged drug retention on the rat skin during ex vivo studies compared to liposomal dispersion and gum karaya plain gel loaded with drug.
The prolonged retention of drug by the gum karaya gel loaded with liposomal dispersion could effectively exhibit the antifungal activity for prolonged periods for cutaneous delivery.
通过脂质体在皮肤上应用来递送抗真菌药物，对于皮肤真菌感染的有效治疗目标可能具有极大的益处。局部给药涉及在使药物透过皮肤的通量最小化的同时，使其在皮肤上的保留最大化。本研究的目的是考察脂质和胆固醇对作为抗真菌剂盐酸特比萘芬潜在载体的脂质体制剂开发的影响。使用磷脂90H（氢化磷脂酰胆碱）、二肉豆蔻酰甘油-3-磷酸胆碱（DMPC）以及胆固醇，通过乙醇注入法制备脂质体，并对其药物含量、包封率、粒径、ζ电位、囊泡形态、稳定性、傅里叶变换红外光谱（FTIR）、体外和离体药物保留进行研究。
药物包封率在39.46±0.91%至70.39±0.71%之间。囊泡呈现出良好的形态特征，粒径分布狭窄，粒径范围在206.9至344.8纳米之间。在离体研究中，与脂质体分散体以及载药的刺梧桐树胶普通凝胶相比，载有脂质体分散体的刺梧桐树胶凝胶在大鼠皮肤上显示出延长的药物保留时间。
载有脂质体分散体的刺梧桐树胶凝胶对药物的延长保留可有效地在皮肤给药中长时间展现抗真菌活性。
