Span 40-based niosomes were employed as nanocarriers to improve cutaneous absorption of salidroside . The niosomal formulation with a molar proportion of Span 40 to cholesterol of 4:3 showed the highest transdermal flux and skin deposition of salidroside. The transdermal flux of the 4:3 niosomal formulation was significantly greater than that of the aqueous solution. Salidroside-loaded niosomes showed good biocompatibility with skin tissue, human epidermal immortal keratinocytes (HaCaT), and human embryonic skin fibroblasts (CCC-ESF). The fluorescence intensity of HaCaT cells after uptake of coumarin 6-labeled niosomes was similar to that observed after uptake of the aqueous suspension. The fluorescence intensity of CCC-ESF cells was greater than that of the aqueous suspension after incubation for 10 min, but was not significantly different after 60 min. Further investigation revealed that internalization of niosomes by HaCaT cells may be achieved through pinocytotic vesicles and macropinocytosis, which consumes energy, rather than via lysosomes. In CCC-ESF cells, pinocytotic vesicles and lysosomes were both important mediators of endocytosis. The niosome formulations reported here could improve the dermal and transdermal salidroside delivery, and the in vitro cell uptake evaluation results serve as a basis for further research into the mechanisms through which niosomes enhance drug permeability.
Finasteride, a selective Type II 5α-reductase inhibitor, has been approved as an oral drug for the treatment and prevention of androgenetic alopecia (AGA). The daily administration of finasteride by oral route may lead to various undesirable systemic side effects. In the present study, finasteride niosomes (FIN-NIS) as a dermal topical delivery system were developed evaluated in vitro / in vivo in an attempt to overcome the limitations of the oral administration of finasteride, enhance the retention of finasteride into hair follicles, and cause fewer adverse effects. FIN-NIS were prepared by ethanol injection method and characterized for particle size, entrapment efficiency (EE), in vitro release and in vitro skin retention. Testosterone-induced AGA mice model was used to evaluate the therapeutic effect of FIN-NIS. The results show that the particle size of FIN-NIS was about 260 nm with a good loading capacity, and the EE was greater than 90%. FIN-NIS had the sustained-release effect to some extent. Compared with the hydroethanolic solution of finasteride (FIN-hydroethanol) and finasteride suspension (FIN-suspension), FIN-NIS showed higher drug concentration in the excised rat skin, especially in the hair follicle area. The drug accumulation of FIN-NIS in the hair follicles was 20 times higher than that of FIN-hydroalcohol. In addition, FIN-NIS was more effective to promote hair regeneration in AGA mice than FIN-suspension, and the effectiveness of FIN-NIS even exceeded that of minoxidil . In conclusion, FIN-NIS could become a promising dermal topical delivery system for enhancing the performance of finasteride for the management of AGA and avoiding the possible risk of systemic side effects associated with oral administration.
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