Preparation and in vitro and in vivo Study of Asiaticoside-Loaded Nanoemulsions and Nanoemulsions-Based Gels for Transdermal Delivery

Huimin Li,1,* Qian Peng,2,* Yisha Guo,3 Xiaohui Wang,1 Li Zhang1 1Department of Pharmacy, Logistics College of Chinese People’s Armed Police Forces, Tianjin 300309, People’s Republic of China; 2Jiangsu Hengrui Pharmaceutical Co. LTD, Jiangsu 222000, People’s Republic of...

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Autores principales:	Li H, Peng Q, Guo Y, Wang X, Zhang L
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2020
Materias:	asiaticoside transdermal delivery system permeation enhancer nanoemulsions Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/e67269c965d74bc4bebd7d727eb553ad
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spelling	oai:doaj.org-article:e67269c965d74bc4bebd7d727eb553ad2021-12-02T10:33:41ZPreparation and in vitro and in vivo Study of Asiaticoside-Loaded Nanoemulsions and Nanoemulsions-Based Gels for Transdermal Delivery1178-2013https://doaj.org/article/e67269c965d74bc4bebd7d727eb553ad2020-05-01T00:00:00Zhttps://www.dovepress.com/preparation-and-in-vitro-and-in-vivo-study-of-asiaticoside-loaded-nano-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Huimin Li,1,* Qian Peng,2,* Yisha Guo,3 Xiaohui Wang,1 Li Zhang1 1Department of Pharmacy, Logistics College of Chinese People’s Armed Police Forces, Tianjin 300309, People’s Republic of China; 2Jiangsu Hengrui Pharmaceutical Co. LTD, Jiangsu 222000, People’s Republic of China; 3Characteristic Medical Center of the Chinese People’s Armed Police Forces, Tianjin 300162, People’s Republic of China*These authors contributed equally to this workCorrespondence: Li Zhang; Xiaohui WangDepartment of Pharmacy, Logistics College of Chinese People’s Armed Police Forces, Tianjin 300309, People’s Republic of ChinaTel +86-13302086775; +86-13302023963Email zhli62tianjin@163.com; 1517183319@qq.comPurpose: Asiaticoside (ASI), a compound of triterpene pentacyclic saponins, has apparently therapeutic efficacy on human hypertrophic scar. However, the characteristics of large molecular weight, low water solubility and poor lipophilicity do not favor the diffusion through the stratum corneum (SC). Therefore, it is expected that the development of a transdermally delivered formulation may enhance the permeability ratio (Qn) of ASI for its clinical application. In this study, we designed asiaticoside-loaded nanoemulsions (ASI-NEs) and nanoemulsions-based gels (ASI-NBGs) and studied their mechanism for transdermal delivery.Methods: The preparation of ASI-NEs was optimized by simplex lattice design (SLD). The ex vivo transdermal penetration and the in vivo pharmacokinetics studies were studied, respectively. The skin irritation of ASI-NEs and ASI-NBGs was measured on normal and damaged skin in rabbits, and the transcutaneous mechanisms of ASI-NEs and ASI-NBGs were determined by HE stained and confocal laser scanning microscopy (CLSM).Results: The mean particle size of ASI-NEs was 132± 5.84nm. The ex vivo skin permeation study veriﬁed that the Qn of the optimized ASI-NEs and ASI-NBGs was about 13.65 times and 5.05 times higher than that of the ordinary ASI-G group. In vivo, the pharmacokinetics studies showed that ASI-NEs and ASI-NBGs reached the peak value in the skin quickly and maintained stable release for a long time with high bioavailability. ASI-NEs and ASI-NBGs were proved to be safe when applied for topical skin usage, and they could play a therapeutic role through the skin mainly by acting on the microstructure of the SC and by means of the skin adnexal pathways.Conclusion: ASI-NEs and ASI-NBGs were effectively developed to overcome the barrier properties of the skin and show high drug penetration through the transdermal route. In addition, we found that ASI-NEs and ASI-NBGs are safe when applied through transdermal delivery system.Keywords: asiaticoside, transdermal delivery system, permeation enhancer, nanoemulsionsLi HPeng QGuo YWang XZhang LDove Medical Pressarticleasiaticosidetransdermal delivery systempermeation enhancernanoemulsionsMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 15, Pp 3123-3136 (2020)
institution	DOAJ
collection	DOAJ
language	EN
topic	asiaticoside transdermal delivery system permeation enhancer nanoemulsions Medicine (General) R5-920
spellingShingle	asiaticoside transdermal delivery system permeation enhancer nanoemulsions Medicine (General) R5-920 Li H Peng Q Guo Y Wang X Zhang L Preparation and in vitro and in vivo Study of Asiaticoside-Loaded Nanoemulsions and Nanoemulsions-Based Gels for Transdermal Delivery
description	Huimin Li,1,* Qian Peng,2,* Yisha Guo,3 Xiaohui Wang,1 Li Zhang1 1Department of Pharmacy, Logistics College of Chinese People’s Armed Police Forces, Tianjin 300309, People’s Republic of China; 2Jiangsu Hengrui Pharmaceutical Co. LTD, Jiangsu 222000, People’s Republic of China; 3Characteristic Medical Center of the Chinese People’s Armed Police Forces, Tianjin 300162, People’s Republic of China*These authors contributed equally to this workCorrespondence: Li Zhang; Xiaohui WangDepartment of Pharmacy, Logistics College of Chinese People’s Armed Police Forces, Tianjin 300309, People’s Republic of ChinaTel +86-13302086775; +86-13302023963Email zhli62tianjin@163.com; 1517183319@qq.comPurpose: Asiaticoside (ASI), a compound of triterpene pentacyclic saponins, has apparently therapeutic efficacy on human hypertrophic scar. However, the characteristics of large molecular weight, low water solubility and poor lipophilicity do not favor the diffusion through the stratum corneum (SC). Therefore, it is expected that the development of a transdermally delivered formulation may enhance the permeability ratio (Qn) of ASI for its clinical application. In this study, we designed asiaticoside-loaded nanoemulsions (ASI-NEs) and nanoemulsions-based gels (ASI-NBGs) and studied their mechanism for transdermal delivery.Methods: The preparation of ASI-NEs was optimized by simplex lattice design (SLD). The ex vivo transdermal penetration and the in vivo pharmacokinetics studies were studied, respectively. The skin irritation of ASI-NEs and ASI-NBGs was measured on normal and damaged skin in rabbits, and the transcutaneous mechanisms of ASI-NEs and ASI-NBGs were determined by HE stained and confocal laser scanning microscopy (CLSM).Results: The mean particle size of ASI-NEs was 132± 5.84nm. The ex vivo skin permeation study veriﬁed that the Qn of the optimized ASI-NEs and ASI-NBGs was about 13.65 times and 5.05 times higher than that of the ordinary ASI-G group. In vivo, the pharmacokinetics studies showed that ASI-NEs and ASI-NBGs reached the peak value in the skin quickly and maintained stable release for a long time with high bioavailability. ASI-NEs and ASI-NBGs were proved to be safe when applied for topical skin usage, and they could play a therapeutic role through the skin mainly by acting on the microstructure of the SC and by means of the skin adnexal pathways.Conclusion: ASI-NEs and ASI-NBGs were effectively developed to overcome the barrier properties of the skin and show high drug penetration through the transdermal route. In addition, we found that ASI-NEs and ASI-NBGs are safe when applied through transdermal delivery system.Keywords: asiaticoside, transdermal delivery system, permeation enhancer, nanoemulsions
format	article
author	Li H Peng Q Guo Y Wang X Zhang L
author_facet	Li H Peng Q Guo Y Wang X Zhang L
author_sort	Li H
title	Preparation and in vitro and in vivo Study of Asiaticoside-Loaded Nanoemulsions and Nanoemulsions-Based Gels for Transdermal Delivery
title_short	Preparation and in vitro and in vivo Study of Asiaticoside-Loaded Nanoemulsions and Nanoemulsions-Based Gels for Transdermal Delivery
title_full	Preparation and in vitro and in vivo Study of Asiaticoside-Loaded Nanoemulsions and Nanoemulsions-Based Gels for Transdermal Delivery
title_fullStr	Preparation and in vitro and in vivo Study of Asiaticoside-Loaded Nanoemulsions and Nanoemulsions-Based Gels for Transdermal Delivery
title_full_unstemmed	Preparation and in vitro and in vivo Study of Asiaticoside-Loaded Nanoemulsions and Nanoemulsions-Based Gels for Transdermal Delivery
title_sort	preparation and in vitro and in vivo study of asiaticoside-loaded nanoemulsions and nanoemulsions-based gels for transdermal delivery
publisher	Dove Medical Press
publishDate	2020
url	https://doaj.org/article/e67269c965d74bc4bebd7d727eb553ad
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Preparation and in vitro and in vivo Study of Asiaticoside-Loaded Nanoemulsions and Nanoemulsions-Based Gels for Transdermal Delivery

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