pH-sensitive and folic acid-targeted MPEG-PHIS/FA-PEG-VE mixed micelles for the delivery of PTX-VE and their antitumor activity

Yan Di,1 Ting Li,1 Zhihong Zhu,1 Fen Chen,2 Lianqun Jia,2 Wenbing Liu,3 Xiumei Gai,1 Yingying Wang,1 Weisan Pan,1 Xinggang Yang1 1Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, 2Key Laboratory of Ministry of Education for TCM Viscera-State Theory and Applicatio...

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Autores principales:	Di Y, Li T, Zhu Z, Chen F, Jia L, Liu W, Gai X, Wang Y, Pan W, Yang X
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2017
Materias:	pH sensitive folic acid targeting mixed micelles drug delivery tumor Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/5828670ffdcc4d4ab39c742d9acb2d70
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spelling	oai:doaj.org-article:5828670ffdcc4d4ab39c742d9acb2d702021-12-02T02:32:08ZpH-sensitive and folic acid-targeted MPEG-PHIS/FA-PEG-VE mixed micelles for the delivery of PTX-VE and their antitumor activity1178-2013https://doaj.org/article/5828670ffdcc4d4ab39c742d9acb2d702017-08-01T00:00:00Zhttps://www.dovepress.com/ph-sensitive-and-folic-acid-targeted-mpeg-phisfa-peg-ve-mixed-micelles-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Yan Di,1 Ting Li,1 Zhihong Zhu,1 Fen Chen,2 Lianqun Jia,2 Wenbing Liu,3 Xiumei Gai,1 Yingying Wang,1 Weisan Pan,1 Xinggang Yang1 1Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, 2Key Laboratory of Ministry of Education for TCM Viscera-State Theory and Applications, Liaoning University of Traditional Chinese Medicine, 3Key Laboratory of Structure-Based Drug Design & Discovery, Shenyang Pharmaceutical University, Ministry of Education, Shenyang, China Abstract: The aim of this study was to simultaneously introduce pH sensitivity and folic acid (FA) targeting into a micelle system to achieve quick drug release and to enhance its accumulation in tumor cells. Paclitaxel-(+)-α-tocopherol (PTX-VE)-loaded mixed micelles (PHIS/FA/PM) fabricated by poly(ethylene glycol) methyl ether-poly(histidine) (MPEG-PHIS) and folic acid-poly(ethylene glycol)-(+)-α-tocopherol (FA-PEG-VE) were characterized by dynamic light scattering and transmission electron microscopy (TEM). The mixed micelles had a spherical morphology with an average diameter of 137.0±6.70 nm and a zeta potential of -48.7±4.25 mV. The drug encapsulation and loading efficiencies were 91.06%±2.45% and 5.28%±0.30%, respectively. The pH sensitivity was confirmed by changes in particle size, critical micelle concentration, and transmittance as a function of pH. MTT assay showed that PHIS/FA/PM had higher cytotoxicity at pH 6.0 than at pH 7.4, and lower cytotoxicity in the presence of free FA. Confocal laser scanning microscope images demonstrated a time-dependent and FA-inhibited cellular uptake. In vivo imaging confirmed that the mixed micelles targeted accumulation at tumor sites and the tumor inhibition rate was 85.97%. The results proved that the mixed micelle system fabricated by MPEG-PHIS and FA-PEG-VE is a promising approach to improve antitumor efficacy. Keywords: pH sensitive, folic acid targeting, mixed micelles, drug delivery, in vivo antitumor activityDi YLi TZhu ZChen FJia LLiu WGai XWang YPan WYang XDove Medical PressarticlepH sensitivefolic acid targetingmixed micellesdrug deliverytumorMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 12, Pp 5863-5877 (2017)
institution	DOAJ
collection	DOAJ
language	EN
topic	pH sensitive folic acid targeting mixed micelles drug delivery tumor Medicine (General) R5-920
spellingShingle	pH sensitive folic acid targeting mixed micelles drug delivery tumor Medicine (General) R5-920 Di Y Li T Zhu Z Chen F Jia L Liu W Gai X Wang Y Pan W Yang X pH-sensitive and folic acid-targeted MPEG-PHIS/FA-PEG-VE mixed micelles for the delivery of PTX-VE and their antitumor activity
description	Yan Di,1 Ting Li,1 Zhihong Zhu,1 Fen Chen,2 Lianqun Jia,2 Wenbing Liu,3 Xiumei Gai,1 Yingying Wang,1 Weisan Pan,1 Xinggang Yang1 1Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, 2Key Laboratory of Ministry of Education for TCM Viscera-State Theory and Applications, Liaoning University of Traditional Chinese Medicine, 3Key Laboratory of Structure-Based Drug Design & Discovery, Shenyang Pharmaceutical University, Ministry of Education, Shenyang, China Abstract: The aim of this study was to simultaneously introduce pH sensitivity and folic acid (FA) targeting into a micelle system to achieve quick drug release and to enhance its accumulation in tumor cells. Paclitaxel-(+)-α-tocopherol (PTX-VE)-loaded mixed micelles (PHIS/FA/PM) fabricated by poly(ethylene glycol) methyl ether-poly(histidine) (MPEG-PHIS) and folic acid-poly(ethylene glycol)-(+)-α-tocopherol (FA-PEG-VE) were characterized by dynamic light scattering and transmission electron microscopy (TEM). The mixed micelles had a spherical morphology with an average diameter of 137.0±6.70 nm and a zeta potential of -48.7±4.25 mV. The drug encapsulation and loading efficiencies were 91.06%±2.45% and 5.28%±0.30%, respectively. The pH sensitivity was confirmed by changes in particle size, critical micelle concentration, and transmittance as a function of pH. MTT assay showed that PHIS/FA/PM had higher cytotoxicity at pH 6.0 than at pH 7.4, and lower cytotoxicity in the presence of free FA. Confocal laser scanning microscope images demonstrated a time-dependent and FA-inhibited cellular uptake. In vivo imaging confirmed that the mixed micelles targeted accumulation at tumor sites and the tumor inhibition rate was 85.97%. The results proved that the mixed micelle system fabricated by MPEG-PHIS and FA-PEG-VE is a promising approach to improve antitumor efficacy. Keywords: pH sensitive, folic acid targeting, mixed micelles, drug delivery, in vivo antitumor activity
format	article
author	Di Y Li T Zhu Z Chen F Jia L Liu W Gai X Wang Y Pan W Yang X
author_facet	Di Y Li T Zhu Z Chen F Jia L Liu W Gai X Wang Y Pan W Yang X
author_sort	Di Y
title	pH-sensitive and folic acid-targeted MPEG-PHIS/FA-PEG-VE mixed micelles for the delivery of PTX-VE and their antitumor activity
title_short	pH-sensitive and folic acid-targeted MPEG-PHIS/FA-PEG-VE mixed micelles for the delivery of PTX-VE and their antitumor activity
title_full	pH-sensitive and folic acid-targeted MPEG-PHIS/FA-PEG-VE mixed micelles for the delivery of PTX-VE and their antitumor activity
title_fullStr	pH-sensitive and folic acid-targeted MPEG-PHIS/FA-PEG-VE mixed micelles for the delivery of PTX-VE and their antitumor activity
title_full_unstemmed	pH-sensitive and folic acid-targeted MPEG-PHIS/FA-PEG-VE mixed micelles for the delivery of PTX-VE and their antitumor activity
title_sort	ph-sensitive and folic acid-targeted mpeg-phis/fa-peg-ve mixed micelles for the delivery of ptx-ve and their antitumor activity
publisher	Dove Medical Press
publishDate	2017
url	https://doaj.org/article/5828670ffdcc4d4ab39c742d9acb2d70
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pH-sensitive and folic acid-targeted MPEG-PHIS/FA-PEG-VE mixed micelles for the delivery of PTX-VE and their antitumor activity

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