Mechanism of transdermal permeation promotion of lipophilic drugs by ethosomes

Li Yang,1,* Lifang Wu,1,* Dongze Wu,2 Deshun Shi,3 Tai Wang,4 Xiaoliang Zhu4 1Department of Dermatology, Nanfang Hospital, Southern Medical University, Guangzhou, 2Department of Medicine and Therapeutics, The Prince of Wales Hospital, The Chinese University of Hong Kong, Hong Kong, 3Department of D...

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Autores principales:	Yang L, Wu L, Wu D, Shi D, Wang T, Zhu X
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2017
Materias:	Ethosomes mechanism percutaneous confocal laser scanning microscopy (CLSM) Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/dfd205f81ec5442697ca1d2510cb5887
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spelling	oai:doaj.org-article:dfd205f81ec5442697ca1d2510cb58872021-12-02T03:11:45ZMechanism of transdermal permeation promotion of lipophilic drugs by ethosomes1178-2013https://doaj.org/article/dfd205f81ec5442697ca1d2510cb58872017-04-01T00:00:00Zhttps://www.dovepress.com/mechanism-of-transdermal-permeation-promotion-of-lipophilic-drugs-by-e-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Li Yang,1,* Lifang Wu,1,* Dongze Wu,2 Deshun Shi,3 Tai Wang,4 Xiaoliang Zhu4 1Department of Dermatology, Nanfang Hospital, Southern Medical University, Guangzhou, 2Department of Medicine and Therapeutics, The Prince of Wales Hospital, The Chinese University of Hong Kong, Hong Kong, 3Department of Dermatology, The First People’s Hospital of Foshan, Foshan, 4Department of Dermatology, Nanfang Hospital, Southern Medical University, Guangzhou, People’s Republic of China *These authors contributed equally to this work Abstract: Ethosomes can promote the penetration of lipophilic drugs into the skin, but the underlying mechanism is still unknown. The purpose of this study was to investigate the mechanism of transdermal permeation promotion of lipophilic drugs by ethosomes. The formulation of ethosomes was optimized using the Box–Behnken experimental design, in which Rhodamine B and 1-palmitoyl-2-{12-[(7-nitro-2-1,3-benzoxadiazol-4-yl)amino]dodecanoyl}-sn-glycero-3-phosphocholine were used to simulate a model lipophilic drug and act as a fluorescent tracer of ethosomal phospholipids, respectively. Liposomes with the same phospholipid concentration and a hydroethanolic solution with the same ethanol concentration were also prepared as controls. The percutaneous progression of the above fluorescent preparations was observed by confocal laser scanning microscopy, and the fluorescence intensity of the images was analyzed. The optimized ethosome formulation consisted of 2.45% yolk phospholipids, 30% ethanol, and 67.55% distilled water. The percutaneous permeation of Rhodamine B in the optimized ethosomes was superior to that in hydroethanolic solution (P<0.05) and liposomes (P<0.05). The ethosomes could penetrate the skin via the percutaneous pathway of the hair follicle and stratum corneum, while during the process of penetration, the vesicles were broken and the phospholipids were retained in the upper epidermis, with the test compounds penetrating gradually. The superior percutaneous penetration of ethosomes was linked to the synergistic effects of their ingredients. The percutaneous pathways of ethosomes included open hair follicles and stratum corneum pathways. In addition, the vesicles might break up during percutaneous penetration in the superficial layer of the skin, allowing the test compounds to keep permeating into the deeper layer alone, while the phospholipid was retained in the upper epidermis. Keywords: ethosomes, mechanism, percutaneous, confocal laser scanning microscopy, CLSMYang LWu LWu DShi DWang TZhu XDove Medical PressarticleEthosomesmechanismpercutaneousconfocal laser scanning microscopy (CLSM)Medicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 12, Pp 3357-3364 (2017)
institution	DOAJ
collection	DOAJ
language	EN
topic	Ethosomes mechanism percutaneous confocal laser scanning microscopy (CLSM) Medicine (General) R5-920
spellingShingle	Ethosomes mechanism percutaneous confocal laser scanning microscopy (CLSM) Medicine (General) R5-920 Yang L Wu L Wu D Shi D Wang T Zhu X Mechanism of transdermal permeation promotion of lipophilic drugs by ethosomes
description	Li Yang,1,* Lifang Wu,1,* Dongze Wu,2 Deshun Shi,3 Tai Wang,4 Xiaoliang Zhu4 1Department of Dermatology, Nanfang Hospital, Southern Medical University, Guangzhou, 2Department of Medicine and Therapeutics, The Prince of Wales Hospital, The Chinese University of Hong Kong, Hong Kong, 3Department of Dermatology, The First People’s Hospital of Foshan, Foshan, 4Department of Dermatology, Nanfang Hospital, Southern Medical University, Guangzhou, People’s Republic of China *These authors contributed equally to this work Abstract: Ethosomes can promote the penetration of lipophilic drugs into the skin, but the underlying mechanism is still unknown. The purpose of this study was to investigate the mechanism of transdermal permeation promotion of lipophilic drugs by ethosomes. The formulation of ethosomes was optimized using the Box–Behnken experimental design, in which Rhodamine B and 1-palmitoyl-2-{12-[(7-nitro-2-1,3-benzoxadiazol-4-yl)amino]dodecanoyl}-sn-glycero-3-phosphocholine were used to simulate a model lipophilic drug and act as a fluorescent tracer of ethosomal phospholipids, respectively. Liposomes with the same phospholipid concentration and a hydroethanolic solution with the same ethanol concentration were also prepared as controls. The percutaneous progression of the above fluorescent preparations was observed by confocal laser scanning microscopy, and the fluorescence intensity of the images was analyzed. The optimized ethosome formulation consisted of 2.45% yolk phospholipids, 30% ethanol, and 67.55% distilled water. The percutaneous permeation of Rhodamine B in the optimized ethosomes was superior to that in hydroethanolic solution (P<0.05) and liposomes (P<0.05). The ethosomes could penetrate the skin via the percutaneous pathway of the hair follicle and stratum corneum, while during the process of penetration, the vesicles were broken and the phospholipids were retained in the upper epidermis, with the test compounds penetrating gradually. The superior percutaneous penetration of ethosomes was linked to the synergistic effects of their ingredients. The percutaneous pathways of ethosomes included open hair follicles and stratum corneum pathways. In addition, the vesicles might break up during percutaneous penetration in the superficial layer of the skin, allowing the test compounds to keep permeating into the deeper layer alone, while the phospholipid was retained in the upper epidermis. Keywords: ethosomes, mechanism, percutaneous, confocal laser scanning microscopy, CLSM
format	article
author	Yang L Wu L Wu D Shi D Wang T Zhu X
author_facet	Yang L Wu L Wu D Shi D Wang T Zhu X
author_sort	Yang L
title	Mechanism of transdermal permeation promotion of lipophilic drugs by ethosomes
title_short	Mechanism of transdermal permeation promotion of lipophilic drugs by ethosomes
title_full	Mechanism of transdermal permeation promotion of lipophilic drugs by ethosomes
title_fullStr	Mechanism of transdermal permeation promotion of lipophilic drugs by ethosomes
title_full_unstemmed	Mechanism of transdermal permeation promotion of lipophilic drugs by ethosomes
title_sort	mechanism of transdermal permeation promotion of lipophilic drugs by ethosomes
publisher	Dove Medical Press
publishDate	2017
url	https://doaj.org/article/dfd205f81ec5442697ca1d2510cb5887
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_version_	1718401891077980160

Mechanism of transdermal permeation promotion of lipophilic drugs by ethosomes

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