Capsaicin-loaded nanolipoidal carriers for topical application: design, characterization, and in vitro/in vivo evaluation

Xia-Rong Wang,1 Si-Qian Gao,1 Xiao-Qian Niu,1 Long-Jian Li,2 Xiao-Ying Ying,1 Zhong-Jie Hu,2 Jian-Qing Gao1,3 1Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, 2Zhejiang Provincial Corps Hospital of Chinese People’s Armed Police Forces, Jiaxin...

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Autores principales:	Wang XR, Gao SQ, Niu XQ, Li LJ, Ying XY, Hu ZJ, Gao JQ
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2017
Materias:	Capsaicin Nanolipoidal carriers Topical application Hot-plate test Carrageenan-induced paw edema Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/95840784528f4124a578c606deae59c8
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spelling	oai:doaj.org-article:95840784528f4124a578c606deae59c82021-12-02T03:58:30ZCapsaicin-loaded nanolipoidal carriers for topical application: design, characterization, and in vitro/in vivo evaluation1178-2013https://doaj.org/article/95840784528f4124a578c606deae59c82017-05-01T00:00:00Zhttps://www.dovepress.com/capsaicin-loaded-nanolipoidal-carriers-for-topical-application-design--peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Xia-Rong Wang,1 Si-Qian Gao,1 Xiao-Qian Niu,1 Long-Jian Li,2 Xiao-Ying Ying,1 Zhong-Jie Hu,2 Jian-Qing Gao1,3 1Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, 2Zhejiang Provincial Corps Hospital of Chinese People’s Armed Police Forces, Jiaxing, Zhejiang, 3Jiangsu Engineering Research Center for New-Type External and Transdermal Preparations, Jiangsu, People’s Republic of China Abstract: Capsaicin has been used in clinical applications for the treatment of pain disorders and inflammatory diseases. Given the strong pungency and high oil/water partition coefficient of capsaicin, capsaicin-loaded nanolipoidal carriers (NLCs) were designed to increase permeation and achieve the analgesic, anti-inflammatory effect with lower skin irritation. Capsaicin-loaded NLCs were prepared and later optimized by the Box–Behnken design. The physicochemical characterizations, morphology, and encapsulation of the capsaicin-loaded NLCs were subsequently confirmed. Capsaicin-loaded NLCs and capsaicin-loaded NLCs gel exhibited sustained release and no cytotoxicity properties. Also, they could significantly enhance the penetration amount, permeation flux, and skin retention amounts of capsaicin due to the application of NLCs. To study the topical permeation mechanism of capsaicin, 3,3'-dioctadecyloxacarbocyanine perchlorate (Dio) was used as a fluorescent dye. Dio-loaded NLCs and Dio-loaded NLCs gel could effectively deliver Dio up to a skin depth of 260 and 210 µm, respectively, primarily through the appendage route on the basis of version skin sections compared with Dio solution, which only delivered Dio up to 150 µm. In vivo therapeutic experiments demonstrated that capsaicin-loaded NLCs and capsaicin-loaded NLCs gel could improve the pain threshold in a dose-dependent manner and inhibit inflammation, primarily by reducing the prostaglandin E2 levels in the tissue compared with capsaicin cream and capsaicin solution. Meanwhile, skin irritation was reduced, indicating that application of NLCs could decrease the irritation caused by capsaicin. Overall, NLCs may be a potential carrier for topical delivery of capsaicin for useful pain and inflammation therapy. Keywords: capsaicin-loaded NLCs, prescription optimization, analgesic, anti-inflammation, hot-plate test, carrageenan-induced paw edemaWang XRGao SQNiu XQLi LJYing XYHu ZJGao JQDove Medical PressarticleCapsaicinNanolipoidal carriersTopical applicationHot-plate testCarrageenan-induced paw edemaMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 12, Pp 3881-3898 (2017)
institution	DOAJ
collection	DOAJ
language	EN
topic	Capsaicin Nanolipoidal carriers Topical application Hot-plate test Carrageenan-induced paw edema Medicine (General) R5-920
spellingShingle	Capsaicin Nanolipoidal carriers Topical application Hot-plate test Carrageenan-induced paw edema Medicine (General) R5-920 Wang XR Gao SQ Niu XQ Li LJ Ying XY Hu ZJ Gao JQ Capsaicin-loaded nanolipoidal carriers for topical application: design, characterization, and in vitro/in vivo evaluation
description	Xia-Rong Wang,1 Si-Qian Gao,1 Xiao-Qian Niu,1 Long-Jian Li,2 Xiao-Ying Ying,1 Zhong-Jie Hu,2 Jian-Qing Gao1,3 1Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, 2Zhejiang Provincial Corps Hospital of Chinese People’s Armed Police Forces, Jiaxing, Zhejiang, 3Jiangsu Engineering Research Center for New-Type External and Transdermal Preparations, Jiangsu, People’s Republic of China Abstract: Capsaicin has been used in clinical applications for the treatment of pain disorders and inflammatory diseases. Given the strong pungency and high oil/water partition coefficient of capsaicin, capsaicin-loaded nanolipoidal carriers (NLCs) were designed to increase permeation and achieve the analgesic, anti-inflammatory effect with lower skin irritation. Capsaicin-loaded NLCs were prepared and later optimized by the Box–Behnken design. The physicochemical characterizations, morphology, and encapsulation of the capsaicin-loaded NLCs were subsequently confirmed. Capsaicin-loaded NLCs and capsaicin-loaded NLCs gel exhibited sustained release and no cytotoxicity properties. Also, they could significantly enhance the penetration amount, permeation flux, and skin retention amounts of capsaicin due to the application of NLCs. To study the topical permeation mechanism of capsaicin, 3,3'-dioctadecyloxacarbocyanine perchlorate (Dio) was used as a fluorescent dye. Dio-loaded NLCs and Dio-loaded NLCs gel could effectively deliver Dio up to a skin depth of 260 and 210 µm, respectively, primarily through the appendage route on the basis of version skin sections compared with Dio solution, which only delivered Dio up to 150 µm. In vivo therapeutic experiments demonstrated that capsaicin-loaded NLCs and capsaicin-loaded NLCs gel could improve the pain threshold in a dose-dependent manner and inhibit inflammation, primarily by reducing the prostaglandin E2 levels in the tissue compared with capsaicin cream and capsaicin solution. Meanwhile, skin irritation was reduced, indicating that application of NLCs could decrease the irritation caused by capsaicin. Overall, NLCs may be a potential carrier for topical delivery of capsaicin for useful pain and inflammation therapy. Keywords: capsaicin-loaded NLCs, prescription optimization, analgesic, anti-inflammation, hot-plate test, carrageenan-induced paw edema
format	article
author	Wang XR Gao SQ Niu XQ Li LJ Ying XY Hu ZJ Gao JQ
author_facet	Wang XR Gao SQ Niu XQ Li LJ Ying XY Hu ZJ Gao JQ
author_sort	Wang XR
title	Capsaicin-loaded nanolipoidal carriers for topical application: design, characterization, and in vitro/in vivo evaluation
title_short	Capsaicin-loaded nanolipoidal carriers for topical application: design, characterization, and in vitro/in vivo evaluation
title_full	Capsaicin-loaded nanolipoidal carriers for topical application: design, characterization, and in vitro/in vivo evaluation
title_fullStr	Capsaicin-loaded nanolipoidal carriers for topical application: design, characterization, and in vitro/in vivo evaluation
title_full_unstemmed	Capsaicin-loaded nanolipoidal carriers for topical application: design, characterization, and in vitro/in vivo evaluation
title_sort	capsaicin-loaded nanolipoidal carriers for topical application: design, characterization, and in vitro/in vivo evaluation
publisher	Dove Medical Press
publishDate	2017
url	https://doaj.org/article/95840784528f4124a578c606deae59c8
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Capsaicin-loaded nanolipoidal carriers for topical application: design, characterization, and in vitro/in vivo evaluation

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