Transfersomes improved delivery of ascorbic palmitate into the viable epidermis for enhanced treatment of melasma

doi:10.1016/j.ijpharm.2021.121059

	Transfersomes improved delivery of ascorbic palmitate into the viable epidermis for enhanced treatment of melasma
	Li, Junjun 1,2; Duan, Nianxiu 1; Song, Sha 1; Nie, Di 1; Yu, Miaorong 1; Wang, Jie 1; Xi, Ziyue 1; Li, Jingyi 1; Sheng, Yingjie 1; Xu, Can 3
刊名	INTERNATIONAL JOURNAL OF PHARMACEUTICS
	2021-10-25
卷号	608 页码:10
关键词	Transfersome Drug delivery Ascorbic palmitate Viable epidermis Melasma treatment
ISSN号	0378-5173
DOI	10.1016/j.ijpharm.2021.121059
通讯作者	Wei, Yan(ywei@shu.edu.cn) ; Gan, Yong(ygan@simm.ac.cn)
英文摘要	Ascorbic palmitate (AP) is widely used in the topical pharmaceutical or cosmetic formulations for melasma treatment. However, the presence of the skin barriers makes it difficult for the highly lipophilic drug molecules to traverse the stratum corneum (SC) and diffuse into the viable epidermis (EP) to reach the melanocytes, thereby exerting suboptimal antimelasma effects. Herein, AP was encapsulated into the transfersomes (TFs), yielding APTFs. AP-TFs utilized the deformability of TFs to squeeze through the skin pores in the SC under the transepidermal hydration gradient forces, leading to 14.1-fold increase in AP accumulation to the EP. AP-TFs could slowly release the encapsulated AP, while whether the released AP or transfersomal AP showed comparable uptake into the melanocytes, thereby exerting similar inhibitory effects on tyrosinase activity and melanogenesis. Ultimately, in the rat melasma model, AP-TFs showed superior antimelasma efficacy to free AP, with effective relief of oxidative stress and inflammation in the skin. Moreover, AP-TFs did not induce skin irritation. Therefore, the study provides a safe and effective approach to elevating the delivery of highly lipophilic drugs to the EP for enhanced treatment of melasma.
资助项目	National Natural Science Foundation of China[82025032] ; National Natural Science Foundation of China[81872428] ; National Natural Science Foundation of China[81703010] ; National Key R&D Program of China[2020YFE0201700] ; China Postdoctoral Science Foundation[2016M600342]
WOS关键词	TRANSDERMAL DELIVERY ; DRUG CARRIERS ; SKIN ; VESICLES ; FORMULATION ; LIPOSOMES ; BEHAVIOR ; INSULIN
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	ELSEVIER
WOS记录号	WOS:000696700800003
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/297863]
专题	中国科学院上海药物研究所
通讯作者	Wei, Yan; Gan, Yong
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China 2.Univ Sci & Technol China, Nano Sci & Technol Inst, Suzhou 215123, Peoples R China 3.Changhai Hosp, Dept Gastroenterol, Shanghai 200433, Peoples R China 4.Shanghai Univ, Inst Translat Med, Shanghai 200011, Peoples R China
推荐引用方式 GB/T 7714	Li, Junjun,Duan, Nianxiu,Song, Sha,et al. Transfersomes improved delivery of ascorbic palmitate into the viable epidermis for enhanced treatment of melasma[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2021,608:10.
APA	Li, Junjun.,Duan, Nianxiu.,Song, Sha.,Nie, Di.,Yu, Miaorong.,...&Gan, Yong.(2021).Transfersomes improved delivery of ascorbic palmitate into the viable epidermis for enhanced treatment of melasma.INTERNATIONAL JOURNAL OF PHARMACEUTICS,608,10.
MLA	Li, Junjun,et al."Transfersomes improved delivery of ascorbic palmitate into the viable epidermis for enhanced treatment of melasma".INTERNATIONAL JOURNAL OF PHARMACEUTICS 608(2021):10.