title: Evaluation of transdermal salidroside delivery using niosomes via in vitro cellular uptake.
abstract: 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.
authors.affiliation: Department of Pharmaceutical Sciences, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Yongtai
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: Department of Pharmaceutical Sciences, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Kai
authors.initials: K
authors.lastname: Zhang
authors.affiliation: Department of Pharmaceutical Sciences, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Zhonghua
authors.initials: Z
authors.lastname: Wu
authors.affiliation: Department of Pharmaceutical Sciences, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Teng
authors.initials: T
authors.lastname: Guo
authors.affiliation: Department of Pharmaceutical Sciences, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Beini
authors.initials: B
authors.lastname: Ye
authors.affiliation: Department of Pharmaceutical Sciences, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Mingyun
authors.initials: M
authors.lastname: Lu
authors.affiliation: Department of Pharmaceutical Sciences, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Jihui
authors.initials: J
authors.lastname: Zhao
authors.affiliation: Department of Pharmaceutical Sciences, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Chunyun
authors.initials: C
authors.lastname: Zhu
authors.affiliation: Department of Pharmaceutical Sciences, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China. Electronic address: npfeng@hotmail.com.
authors.forename: Nianping
authors.initials: N
authors.lastname: Feng
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D001692:Biological Transport / Q000187:drug effects; D002460:Cell Line; D002784:Cholesterol / Q000737:chemistry; D005960:Glucosides / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D006601:Hexoses / Q000737:chemistry; D006801:Humans; D066298:In Vitro Techniques; D008081:Liposomes; D008297:Male; D008819:Mice, Nude; D010636:Phenols / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D017207:Rats, Sprague-Dawley; D012867:Skin / Q000187:drug effects / Q000378:metabolism; D012967:Sodium Dodecyl Sulfate / Q000737:chemistry
chemical_list: D005960:Glucosides; D006601:Hexoses; D008081:Liposomes; D010636:Phenols; D012967:Sodium Dodecyl Sulfate; C061705:sorbitan monopalmitate; D002784:Cholesterol; C009172:rhodioloside
keywords: Biocompatibility; Cellular uptake; Endocytosis; Nanocarrier; Topical administration