Center for Novel Drug Delivery System, Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, N. P. Marg, Matunga (E), Mumbai, 400 019, India.
Drug Deliv Transl Res. 2013 Dec;3(6):587-92. doi: 10.1007/s13346-012-0083-1.
Niosomes are reported to increase the skin permeation and bioavailability of topically applied drug molecules. However, very few studies were reported for nanometer-sized niosome vesicles. The aim of the present study was to prepare minoxidil-loaded niosomal formulation using ethanol injection method. Surfactant screening showed that only Span 60, Span 20, and Tween 20 with cholesterol have capability of nano size vesicle formation. The formed niosomes were characterized for entrapment efficiency, vesicle size, scanning electron microscope, and physical stability. By modulation of surfactant and cholesterol ratio maximum entrapment up to 34.70 ± 1.1 % with size of 470 ± 27 nm was obtained (Span 60/cholesterol ratio of 1:2). The vesicle size obtained was between 150 and 800 nm that was depending on cholesterol ratio and type of nonionic surfactant employed. The in vitro skin permeation study showed that an increase in cholesterol concentration in niosome vesicles increases minoxidil skin retention. Niosome formulation prepared with 1:2 ratio of Span 60 and cholesterol showed 17.21 ± 3.2 % skin retention of minoxidil, which is more than eightfold as compared to control minoxidil gel.
尼奥斯omes 据报道可以增加皮肤渗透和局部应用药物分子的生物利用度。然而，很少有研究报道纳米级尼奥斯ome 囊泡。本研究旨在采用乙醇注入法制备米诺地尔负载的尼奥斯ome 制剂。表面活性剂筛选表明，只有 Span 60、Span 20 和 Tween 20 与胆固醇具有形成纳米大小囊泡的能力。对包封效率、囊泡大小、扫描电子显微镜和物理稳定性进行了表征。通过调节表面活性剂和胆固醇的比例，最大包封率可达 34.70±1.1%，粒径为 470±27nm（Span 60/胆固醇比例为 1:2）。获得的囊泡大小在 150 至 800nm 之间，这取决于胆固醇的比例和所使用的非离子表面活性剂的类型。体外皮肤渗透研究表明，尼奥斯ome 囊泡中胆固醇浓度的增加会增加米诺地尔的皮肤滞留。用 Span 60 和胆固醇 1:2 比例制备的尼奥斯ome 制剂使米诺地尔的皮肤滞留率达到 17.21±3.2%，是对照米诺地尔凝胶的八倍以上。
