Abd Eman, Roberts Michael S, Grice Jeffrey E
Therapeutics Research Centre, Translational Research Institute, School of Medicine, University of Queensland, Brisbane, Qld., Australia.
Skin Pharmacol Physiol. 2016;29(1):24-30. doi: 10.1159/000441040. Epub 2015 Nov 6.
BACKGROUND/AIMS: A range of vesicles is now widely used to carry various solutes into and through the epidermis. These usually have the active solute encapsulated within and may be modified to confer flexibility and skin penetration enhancement. Here, we compared the ability of five different vesicle systems to deliver a model hydrophilic drug, caffeine, into and through excised human skin.
In addition to lipids, the vesicle excipients included eucalyptol or oleic acid as penetration enhancers, and decyl polyglucoside as a non-ionic surfactant. Vesicle particle sizes ranged between 135 and 158 nm, and caffeine encapsulation efficiencies were between 46 and 66%. Caffeine penetration and permeation were measured using high-performance liquid chromatography.
We found that niosomes, which are liposomes containing a non-ionic surfactant, and transferosomes (ultraflexible vesicles) showed significantly greater penetration into the skin and permeation across the stratum corneum. Significant enhancement of caffeine penetration into hair follicles was found for transferosomes and those liposomes containing oleic acid.
We conclude that targeted delivery of the hydrophilic drug caffeine into the skin compartments can be modified using optimized vesicular formulations.
背景/目的：目前，一系列囊泡被广泛用于将各种溶质输送到表皮内并穿过表皮。这些囊泡通常将活性溶质包裹在内部，并且可以进行修饰以赋予其灵活性并增强皮肤渗透性。在此，我们比较了五种不同囊泡系统将模型亲水性药物咖啡因输送到离体人皮肤内并穿过皮肤的能力。
除脂质外，囊泡辅料包括桉叶油素或油酸作为渗透促进剂，以及癸基聚葡萄糖苷作为非离子表面活性剂。囊泡粒径在135至158纳米之间，咖啡因包封率在46%至66%之间。使用高效液相色谱法测量咖啡因的渗透和透过情况。
我们发现，含有非离子表面活性剂的脂质体——非离子型脂质体，以及传递体（超柔性囊泡）显示出对皮肤的渗透和对角质层的透过能力明显更强。对于传递体和含有油酸的脂质体，发现咖啡因向毛囊的渗透显著增强。
我们得出结论，使用优化的囊泡制剂可以改变亲水性药物咖啡因向皮肤各层的靶向递送。
