Folate-conjugated pluronic/polylactic acid polymersomes for oral delivery of paclitaxel

被引：32
作者：
Pan, Xiao Qian [1 ]
Gong, Yan Chun [1 ]
Li, Zi Ling [1 ]
Li, Yu Ping [1 ]
Xiong, Xiang Yuan [1 ]
机构：
[1] Jiangxi Sci & Technol Normal Univ, Sch Life Sci, Sch Pharmaceut Sci, Nanchang 330013, Jiangxi, Peoples R China
来源：
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES | 2019年 / 139卷
基金：
中国国家自然科学基金;
关键词：
Polymersome; Folic acid; Oral delivery; Paclitaxel; Polylactic acid; VITAMIN-E-TPGS; ANTICANCER DRUG-DELIVERY; IN-VITRO; P-GLYCOPROTEIN; CO-DELIVERY; NANOPARTICLES; BIOAVAILABILITY; RELEASE; PERMEABILITY; ABSORPTION;
D O I：
10.1016/j.ijbiomac.2019.07.224
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Cancer chemotherapy and the patient's life will be more convenient if oral administration of anti-cancer drugs can be achieved. The feasibility of folate-targeted Pluronic F127/polylactic acid (FA-F127-PLA) polymersomes as the oral delivery carriers of paclitaxel (PTX) has been explored in this study. PTX loaded in FA-F127-PLA and PLA-F127-PLA polymersomes showed biphasic release behaviors in simulated gastric and intestinal fluids. PTX loaded in FA-F127-PLA polymersomes exhibited higher cytotoxicity and cellular uptake than PTX loaded in PLA-F127-PLA polymersomes. In vivo pharmacokinetic studies in rats showed that oral PTX loaded in FA-F127-PLA polymersomes had a higher bioavailability than oral PTX loaded in PLA-F127-PLA polymersomes. D-a-tocopheryl poly(ethylene glycol) 1000 succinate (TPGS or Vitamin E TPGS) was also added to the FA-F127-PLA polymersomes as an optimization agent. Compared with PTX-loaded FA-F127-PLA polymersome, PTX-loaded FA-F127-PLA/TPGS mixed polymersomes showed even better cytotoxic ability, more cellular uptake and higher bioavailability. The above results indicate that FA-F127-PLA and FA-F127-PLA/TPGS mixed polymersomes could be good candidates for the oral delivery carrier of anti-cancer drugs. (C) 2019 Elsevier B.V. All rights reserved.
引用
收藏
页码：377 / 386
页数：10
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