Evaluation of transdermal salidroside delivery using niosomes via in vitro cellular uptake

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• 作者：Yongtai Zhang ; Kai Zhang ; Zhonghua Wu ; Teng Guo ; Beini Ye ; Mingyun Lu ; Jihui Zhao ; Chunyun Zhu ; Nianping Feng ; ^{npfeng@hotmail.com" class="auth_mail" title="E-mail the corresponding author} ; ^{npfeng@shutcm.edu.cn" class="auth_mail" title="E-mail the corresponding author}
• 关键词：BC ; blank control ; CCC-ESF ; human embryonic skin fibroblasts ; CH ; chlorpromazine hydrochloride ; Chol ; cholesterol ; DAH ; 5-[N ; N-dimethyl]amiloride hydrochloride ; DLS ; dynamic light scattering ; DMEM/High ; high-glucose Dulbecco&rsquo ; s modified Eagle&rsquo ; s medium ; DMSO ; dimethyl sulfoxide ; EDTA ; ethylene diamine tetraacetic acid ; EE ; entrapment efficiency ; FACS ; fluorescent-activated cell sorting ; FBS ; fetal bovine serum ; GS ; genistein ; HaCaT ; human epidermal immortal keratinocytes ; HE ; hematoxyl
• 刊名：International Journal of Pharmaceutics
• 出版年：2015
• 出版时间：15 January 2015
• 年：2015
• 卷：478
• 期：1
• 页码：138-146
• 全文大小：2102 K

文摘

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.