Dept. of Pharmaceutical Technology, Faculty of Pharmacy, Istanbul University, Beyazıt, 34116 Istanbul, Turkey.
Dept. of Analytical Chemistry, Faculty of Pharmacy, Istanbul University, Beyazıt, 34116 Istanbul, Turkey.
Int J Pharm. 2018 Nov 15;551(1-2):133-140. doi: 10.1016/j.ijpharm.2018.08.053. Epub 2018 Aug 29.
The nanomicelles have recently drawn a great deal of attention for drug delivery into the skin. However, these carriers have only deposited in hair follicles and furrows, and drug in the micelles may not therapeutically reach into viable skin layers. The aim of this study was to formulate a combination of nanomicelles with terpenes to overcome this challenge and evaluate their potential for topical drug delivery into the skin. The nanomicelles were characterised with respect to size, size distribution (PDI), zeta potential, morphology and encapsulation efficiency (%). The drug accumulation and penetration were examined by tape stripping method in the skin. The colloidal stability of nanomicelles was followed with respect to size and PDI values. The nanomicelles were about 25-30 nm in size with narrow distribution. All of them had slightly negative surface charge, spherical shapes and high encapsulation efficiency (%). The tape stripping data revealed that nanomicelles consisting of terpinolene led to accumulation of more drug in the stripped skin as compared with commercial product and nanomicelles without terpene. Also, micelle formulations consisting of terpinolene (2.0%) had the highest colloidal stability. Consequently, combination of nanomicelles with terpinolene could be a feasible approach for enhancement of skin drug delivery.
毫微胶束最近引起了人们对药物经皮递药的极大关注。然而，这些载体仅沉积在毛囊和皱纹中，毫微胶束中的药物可能无法在治疗上到达有活力的皮肤层。本研究的目的是将毫微胶束与萜烯结合起来，以克服这一挑战，并评估其在皮肤局部递药中的潜力。毫微胶束的粒径、粒径分布（PDI）、Zeta 电位、形态和包封效率（%）进行了表征。采用胶带剥离法研究了药物在皮肤中的蓄积和渗透情况。考察了毫微胶束的胶体稳定性，包括粒径和 PDI 值。毫微胶束的粒径约为 25-30nm，分布较窄。它们都带有轻微的负表面电荷、球形和高包封效率（%）。胶带剥离数据显示，与商业产品和不含萜烯的毫微胶束相比，由萜品烯组成的毫微胶束可使更多的药物蓄积在剥离的皮肤中。此外，含有 2.0%萜品烯的胶束制剂具有最高的胶体稳定性。因此，毫微胶束与萜烯的结合可能是增强皮肤药物递送的一种可行方法。
