Preparation and functional characterization of tumor-targeted folic acid-chitosan conjugated nanoparticles loaded with mitoxantrone
来源期刊：中南大学学报(英文版)2015年第9期
论文作者：WANG Wei TONG Chun-yi LIU Xing-yan LI Tao LIU Bin XIONG Wei
文章页码：3311 - 3317
Key words：folic acid; chitosan; nanoparticles; mitoxantrone; tumor targeting
Abstract: Folic acid conjugated chitosan was prepared by cross-linking reaction with 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC), and then used as a template to prepare folic acid-chitosan (FA-CS) conjugated nanoparticles and load mitoxantrone nanoparticles (FA-CSNP/MTX). Drug dissolution testing, CCK-8 method, and confocal microscopy were used to detect their controlled-release capability in different situations and the specific uptake by HONE1 cells. The experimental results show that the nanoparticles have uniform size distribution of 48-58 nm. The highest encapsulation rate of the particles on mitoxantrone hydrochloride (MTX) is (77.5±1.9)%, and the drug loading efficiency is (18.4±0.4)%. The sustained release effect, cell growth inhibition activity and targeting effect of the FA-CS/MTX nanoparticles are good in artificial gastric fluid and intestinal fluid. It is demonstrated that the FA-CSNP system is a potentially useful system for the targeted delivery of anticancer drug MTX.
WANG Wei(王炜)1, TONG Chun-yi(童春义)2, LIU Xing-yan(刘星言)1, LI Tao(李涛)1, LIU Bin(刘斌)2, XIONG Wei(熊炜)3
(1. Dongguan Research Center, Guangdong Medical College, Dongguan 523808, China;
2. College of Biology, Hunan University, Changsha 410082, China;
3. Department of Ophthalmology and Eye Research Center, The 2nd Xiangya Hospital,
Central South University, Changsha 410011, China)
Abstract:Folic acid conjugated chitosan was prepared by cross-linking reaction with 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC), and then used as a template to prepare folic acid-chitosan (FA-CS) conjugated nanoparticles and load mitoxantrone nanoparticles (FA-CSNP/MTX). Drug dissolution testing, CCK-8 method, and confocal microscopy were used to detect their controlled-release capability in different situations and the specific uptake by HONE1 cells. The experimental results show that the nanoparticles have uniform size distribution of 48-58 nm. The highest encapsulation rate of the particles on mitoxantrone hydrochloride (MTX) is (77.5±1.9)%, and the drug loading efficiency is (18.4±0.4)%. The sustained release effect, cell growth inhibition activity and targeting effect of the FA-CS/MTX nanoparticles are good in artificial gastric fluid and intestinal fluid. It is demonstrated that the FA-CSNP system is a potentially useful system for the targeted delivery of anticancer drug MTX.
Key words:folic acid; chitosan; nanoparticles; mitoxantrone; tumor targeting
