Compound antimalarial ethosomal cataplasm: preparation, evaluation, and mechanism of penetration enhancement

Shuo Shen, Shu-Zhi Liu, Yu-Shi Zhang, Mao-Bo Du, Ai-Hua Liang, Li-Hua Song, Zu-Guang Ye Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing, People’s Republic of China Abstract: Malaria is still a serious public health problem in some parts of the worl...

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Autores principales:	Shen S, Liu SZ, Zhang YS, Du MB, Liang AH, Song LH, Ye ZG
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2015
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/96a49ce8d0314322b90695c1a22c2e62
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spelling	oai:doaj.org-article:96a49ce8d0314322b90695c1a22c2e622021-12-02T05:14:28ZCompound antimalarial ethosomal cataplasm: preparation, evaluation, and mechanism of penetration enhancement1178-2013https://doaj.org/article/96a49ce8d0314322b90695c1a22c2e622015-06-01T00:00:00Zhttp://www.dovepress.com/compound-antimalarial-ethosomal-cataplasm-preparation-evaluation-and-m-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Shuo Shen, Shu-Zhi Liu, Yu-Shi Zhang, Mao-Bo Du, Ai-Hua Liang, Li-Hua Song, Zu-Guang Ye Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing, People’s Republic of China Abstract: Malaria is still a serious public health problem in some parts of the world. The problems of recurrence and drug resistance are increasingly more serious. Thus, it is necessary to develop a novel antimalarial agent. The objectives of this study were to construct a novel compound antimalarial transdermal nanosystem–ethosomal cataplasm, to investigate its characteristics and efficiency, and to systematically explore the penetration-enhancing mechanisms of ethosomal cataplasm. Artesunate-loaded ethosomes and febrifugine-loaded ethosomes were prepared, and their characteristics were evaluated. Drug-loaded ethosomes were incorporated in the matrix of cataplasm to form the compound antimalarial ethosomal cataplasm. With the help of ethosomal technology, the accumulated permeation quantity of artesunate significantly increased at 8 hours after administration, which was 1.57 times as much as that of conventional cataplasm. Soon after administration, the ethosomal cataplasm could make a large quantity of antimalarial drug quickly penetrate through skin, then the remaining drug in the ethosomal cataplasm could be steadily released. These characteristics of ethosomal cataplasm are favorable for antimalarial drugs to kill Plasmodium spp. quickly and prevent the resurgence of Plasmodium spp. As expected, the ethosomal cataplasm showed good antimalarial efficiency in this experiment. The negative conversion rates were 100% and the recurrence rates were 0% at all dosages. The mechanism of penetration enhancement of the ethosomal cataplasm was systematically explored using an optics microscope, polarization microscope, and transmission electron microscopy. The microstructure, ultrastructure, and birefringent structure in skin were observed. Data obtained in this study showed that the application of ethosomal technology to antimalarial cataplasm could improve the transdermal delivery of drug, enhance the efficacy, and facilitate practical application in clinic. Keywords: ethosomes, transdermal drug-delivery systems, artesunate, febrifugineShen SLiu SZZhang YSDu MBLiang AHSong LHYe ZGDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2015, Iss default, Pp 4239-4253 (2015)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Shen S Liu SZ Zhang YS Du MB Liang AH Song LH Ye ZG Compound antimalarial ethosomal cataplasm: preparation, evaluation, and mechanism of penetration enhancement
description	Shuo Shen, Shu-Zhi Liu, Yu-Shi Zhang, Mao-Bo Du, Ai-Hua Liang, Li-Hua Song, Zu-Guang Ye Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing, People’s Republic of China Abstract: Malaria is still a serious public health problem in some parts of the world. The problems of recurrence and drug resistance are increasingly more serious. Thus, it is necessary to develop a novel antimalarial agent. The objectives of this study were to construct a novel compound antimalarial transdermal nanosystem–ethosomal cataplasm, to investigate its characteristics and efficiency, and to systematically explore the penetration-enhancing mechanisms of ethosomal cataplasm. Artesunate-loaded ethosomes and febrifugine-loaded ethosomes were prepared, and their characteristics were evaluated. Drug-loaded ethosomes were incorporated in the matrix of cataplasm to form the compound antimalarial ethosomal cataplasm. With the help of ethosomal technology, the accumulated permeation quantity of artesunate significantly increased at 8 hours after administration, which was 1.57 times as much as that of conventional cataplasm. Soon after administration, the ethosomal cataplasm could make a large quantity of antimalarial drug quickly penetrate through skin, then the remaining drug in the ethosomal cataplasm could be steadily released. These characteristics of ethosomal cataplasm are favorable for antimalarial drugs to kill Plasmodium spp. quickly and prevent the resurgence of Plasmodium spp. As expected, the ethosomal cataplasm showed good antimalarial efficiency in this experiment. The negative conversion rates were 100% and the recurrence rates were 0% at all dosages. The mechanism of penetration enhancement of the ethosomal cataplasm was systematically explored using an optics microscope, polarization microscope, and transmission electron microscopy. The microstructure, ultrastructure, and birefringent structure in skin were observed. Data obtained in this study showed that the application of ethosomal technology to antimalarial cataplasm could improve the transdermal delivery of drug, enhance the efficacy, and facilitate practical application in clinic. Keywords: ethosomes, transdermal drug-delivery systems, artesunate, febrifugine
format	article
author	Shen S Liu SZ Zhang YS Du MB Liang AH Song LH Ye ZG
author_facet	Shen S Liu SZ Zhang YS Du MB Liang AH Song LH Ye ZG
author_sort	Shen S
title	Compound antimalarial ethosomal cataplasm: preparation, evaluation, and mechanism of penetration enhancement
title_short	Compound antimalarial ethosomal cataplasm: preparation, evaluation, and mechanism of penetration enhancement
title_full	Compound antimalarial ethosomal cataplasm: preparation, evaluation, and mechanism of penetration enhancement
title_fullStr	Compound antimalarial ethosomal cataplasm: preparation, evaluation, and mechanism of penetration enhancement
title_full_unstemmed	Compound antimalarial ethosomal cataplasm: preparation, evaluation, and mechanism of penetration enhancement
title_sort	compound antimalarial ethosomal cataplasm: preparation, evaluation, and mechanism of penetration enhancement
publisher	Dove Medical Press
publishDate	2015
url	https://doaj.org/article/96a49ce8d0314322b90695c1a22c2e62
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Compound antimalarial ethosomal cataplasm: preparation, evaluation, and mechanism of penetration enhancement

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