Department of Pharmaceutics, Poona College of Pharmacy, Bharati Vidyapeeth University, Pune, Maharashtra, India.
Drug Dev Ind Pharm. 2010 Aug;36(8):946-53. doi: 10.3109/03639040903585150.
Niosomal delivery can prove an alternative to improve the poor skin penetration and residence of the topical antifungal drugs that account for the long treatment regimes in cutaneous mycosis.
To investigate niosomes as carriers for dermal delivery of ciclopirox olamine (CPO), a broad spectrum antifungal drug.
Niosomes were prepared by ethanol injection method using Span 60, cholesterol, diacetyl phosphate according to 3(2) factorial design and evaluated for physicochemical parameters, in vitro and ex vivo deposition in skin and stability study.
Unilamellar CPO niosomes of size 170-280 nm, entrapment efficiency 38-68%, and sufficient electrokinetic stability were obtained. Percent drug deposition in artificial membrane varied from 12.75 to 92.74. Deposition of CPO into rat skin from niosomal dispersion and its gel was significantly higher than that of plain CPO solution and its marketed product. Obtained niosomes possessed sufficient stability on storage.
Increasing amounts of Span 60 and cholesterol increase the vesicle size probably because of entrapment of CPO-ionized molecules in the aqueous compartment and interaction of its unionized counterpart with the bilayer constituents leading to increase in bilayer thickness. Consequently, the percent entrapment efficiency also increased. However, increasing Span 60 levels decreased the in vitro percent drug deposition. This might be attributed to the larger size of vesicles produced by high amounts of surfactant that showed poor deposition. The optimized batch possessed sufficient stability.
The results of this investigation suggest that niosomes are promising tools for cutaneous retention of CPO.
将药物制成脂质体，可改善某些外用抗真菌药物经皮渗透差和滞留时间短的问题，从而减少皮肤真菌感染的治疗时间。
研究将环吡酮胺（CPO）制成脂质体，作为一种新型透皮给药载体。
采用乙醇注入法，以司盘 60、胆固醇、双醋磷脂为辅料，按照 3（2）析因设计，制备并评价了脂质体的理化性质、体外和体内皮肤沉积以及稳定性。
成功制备了粒径为 170-280nm、包封率为 38%-68%、具有足够电动稳定性的单层 CPO 脂质体。人工膜中药物的沉积百分比在 12.75%-92.74%之间。与 CPO 溶液及其市售产品相比，CPO 脂质体及其凝胶在大鼠皮肤中的药物沉积明显更高。储存过程中获得的脂质体具有足够的稳定性。
随着司盘 60 和胆固醇用量的增加，囊泡的粒径可能会增大，这可能是由于 CPO-离子化分子被包封在水相中，以及其非离子化部分与双层成分相互作用导致双层厚度增加。因此，包封效率也随之增加。然而，司盘 60 用量的增加会降低体外药物沉积百分比。这可能是由于高浓度表面活性剂产生的较大囊泡导致沉积效果不佳。优化后的批次具有足够的稳定性。
本研究结果表明，脂质体是提高 CPO 皮肤滞留率的一种有前途的工具。
