Sequential release of salidroside and paeonol from a nanosphere-hydrogel system inhibits ultraviolet B-induced melanogenesis in guinea pig skin

Li-Hua Peng,1 Shen-Yao Xu,1 Ying-Hui Shan,1 Wei Wei,1 Shuai Liu,1 Chen-Zhen Zhang,1 Jia-He Wu,1 Wen-Quan Liang,1 Jian-Qing Gao1,2 1Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, 2Novel Transdermal Research Center of Jiangsu Province, Changzhou, People...

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Autores principales:	Peng LH, Xu SY, Shan YH, Wei W, Liu S, Zhang CZ, Wu JH, Liang WQ, Gao JQ
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2014
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/888e52a8575c4203a798b3bde27fab8a
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spelling	oai:doaj.org-article:888e52a8575c4203a798b3bde27fab8a2021-12-02T02:42:20ZSequential release of salidroside and paeonol from a nanosphere-hydrogel system inhibits ultraviolet B-induced melanogenesis in guinea pig skin1178-2013https://doaj.org/article/888e52a8575c4203a798b3bde27fab8a2014-04-01T00:00:00Zhttp://www.dovepress.com/sequential-release-of-salidroside-and-paeonol-from-a-nanosphere-hydrog-a16495https://doaj.org/toc/1178-2013 Li-Hua Peng,1 Shen-Yao Xu,1 Ying-Hui Shan,1 Wei Wei,1 Shuai Liu,1 Chen-Zhen Zhang,1 Jia-He Wu,1 Wen-Quan Liang,1 Jian-Qing Gao1,2 1Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, 2Novel Transdermal Research Center of Jiangsu Province, Changzhou, People's Republic of China Abstract: Melanin is the one of most important pigments for skin color in mammals. Excessive biosynthesis of melanin induces various pigment disorders. Much effort has been made to develop regulators to minimize skin pigmentation abnormalities. However, only a few of them are used, primarily because of safety concerns and low efficiency. In this study, we aimed to construct a novel nanosphere-gel for sequential delivery of salidroside and paeonol, to investigate the synergistic effects of these drugs in anti-melanogenesis, and to decrease their potential for toxicity in high dosage. Nanospheres were prepared and characterized for their particle size, polydispersity index, zeta potential, and morphological properties. The optimized nanospheres were incorporated in carbomer hydrogel with both paeonol and salidroside entrapped to form a dual drug-releasing nanosphere-gel. With this nanosphere-gel, rapid release of salidroside from the hydrogel followed by sustained release of paeonol from the nanosphere was achieved. Using a classical model of the melanogenesis response to ultraviolet exposure, it was shown that the anti-melanogenesis effects of the dual drug-releasing system, in which the doses of the individual drugs were decreased by half, was obviously enhanced when compared with the effects of the single drug preparations. Mechanistically, the burst release of salidroside from the hydrogel may enable prompt suppression of melanocyte proliferation on exposure to ultraviolet B radiation, while the paeonol released in a sustained manner can provide continuous inhibition of tyrosinase activity in melanocytes. Combined delivery of salidroside and paeonol was demonstrated to be a promising strategy for enhancing the therapeutic efficacy of these agents in anti-melanogenesis and reducing their toxicity, so may have great potential in nanomedicine. Keywords: nanosphere, sequential drug release, anti-melanogenesis, salidroside, paeonolPeng LHXu SYShan YHWei WLiu SZhang CZWu JHLiang WQGao JQDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2014, Iss Issue 1, Pp 1897-1908 (2014)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Peng LH Xu SY Shan YH Wei W Liu S Zhang CZ Wu JH Liang WQ Gao JQ Sequential release of salidroside and paeonol from a nanosphere-hydrogel system inhibits ultraviolet B-induced melanogenesis in guinea pig skin
description	Li-Hua Peng,1 Shen-Yao Xu,1 Ying-Hui Shan,1 Wei Wei,1 Shuai Liu,1 Chen-Zhen Zhang,1 Jia-He Wu,1 Wen-Quan Liang,1 Jian-Qing Gao1,2 1Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, 2Novel Transdermal Research Center of Jiangsu Province, Changzhou, People's Republic of China Abstract: Melanin is the one of most important pigments for skin color in mammals. Excessive biosynthesis of melanin induces various pigment disorders. Much effort has been made to develop regulators to minimize skin pigmentation abnormalities. However, only a few of them are used, primarily because of safety concerns and low efficiency. In this study, we aimed to construct a novel nanosphere-gel for sequential delivery of salidroside and paeonol, to investigate the synergistic effects of these drugs in anti-melanogenesis, and to decrease their potential for toxicity in high dosage. Nanospheres were prepared and characterized for their particle size, polydispersity index, zeta potential, and morphological properties. The optimized nanospheres were incorporated in carbomer hydrogel with both paeonol and salidroside entrapped to form a dual drug-releasing nanosphere-gel. With this nanosphere-gel, rapid release of salidroside from the hydrogel followed by sustained release of paeonol from the nanosphere was achieved. Using a classical model of the melanogenesis response to ultraviolet exposure, it was shown that the anti-melanogenesis effects of the dual drug-releasing system, in which the doses of the individual drugs were decreased by half, was obviously enhanced when compared with the effects of the single drug preparations. Mechanistically, the burst release of salidroside from the hydrogel may enable prompt suppression of melanocyte proliferation on exposure to ultraviolet B radiation, while the paeonol released in a sustained manner can provide continuous inhibition of tyrosinase activity in melanocytes. Combined delivery of salidroside and paeonol was demonstrated to be a promising strategy for enhancing the therapeutic efficacy of these agents in anti-melanogenesis and reducing their toxicity, so may have great potential in nanomedicine. Keywords: nanosphere, sequential drug release, anti-melanogenesis, salidroside, paeonol
format	article
author	Peng LH Xu SY Shan YH Wei W Liu S Zhang CZ Wu JH Liang WQ Gao JQ
author_facet	Peng LH Xu SY Shan YH Wei W Liu S Zhang CZ Wu JH Liang WQ Gao JQ
author_sort	Peng LH
title	Sequential release of salidroside and paeonol from a nanosphere-hydrogel system inhibits ultraviolet B-induced melanogenesis in guinea pig skin
title_short	Sequential release of salidroside and paeonol from a nanosphere-hydrogel system inhibits ultraviolet B-induced melanogenesis in guinea pig skin
title_full	Sequential release of salidroside and paeonol from a nanosphere-hydrogel system inhibits ultraviolet B-induced melanogenesis in guinea pig skin
title_fullStr	Sequential release of salidroside and paeonol from a nanosphere-hydrogel system inhibits ultraviolet B-induced melanogenesis in guinea pig skin
title_full_unstemmed	Sequential release of salidroside and paeonol from a nanosphere-hydrogel system inhibits ultraviolet B-induced melanogenesis in guinea pig skin
title_sort	sequential release of salidroside and paeonol from a nanosphere-hydrogel system inhibits ultraviolet b-induced melanogenesis in guinea pig skin
publisher	Dove Medical Press
publishDate	2014
url	https://doaj.org/article/888e52a8575c4203a798b3bde27fab8a
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Sequential release of salidroside and paeonol from a nanosphere-hydrogel system inhibits ultraviolet B-induced melanogenesis in guinea pig skin

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