Preparation and evaluation of folic acid modified succinylated gelatin micelles for targeted delivery of doxorubicin

Research paper by Yunfei Wang, Jin Ren; Yonghua Liu; Rong Liu; Liangliang Wang; Qinglan Yuan; Jianming He; Yamin Nie; Jing Xu; Jingmou Yu

Indexed on: 30 Jun '18Published on: 21 Jun '18Published in: Journal of Drug Delivery Science and Technology


Publication date: August 2018 Source:Journal of Drug Delivery Science and Technology, Volume 46 Author(s): Yunfei Wang, Jin Ren, Yonghua Liu, Rong Liu, Liangliang Wang, Qinglan Yuan, Jianming He, Yamin Nie, Jing Xu, Jingmou Yu In this study, novel folic acid modified succinylated gelatin (FA-SG) micelles were prepared and used as drug carrier in folate-receptor (FR) targeted antitumor therapy. FA-SG copolymer was synthesized and characterized by 1H NMR and fluorescence spectroscopy. Doxorubicin-loaded FA-SG (DOX-FA-SG) micelles were prepared by a dialysis method. The shape of DOX-FA-SG micelles was almost spherical by transmission electron microscopy analysis. The mean diameter of DOX-FA-SG micelles was 277 nm, and the DOX-loading content was 12.4%. In vitro drug release of DOX-loaded micelles showed sustained release behavior for 168 h. DOX-FA-SG demonstrated significantly greater cellular uptake and cytotoxicity against FR-positive MCF-7 cells than the non-targeted DOX-loaded micelles. Importantly, DOX-FA-SG micelles exhibited higher antitumor activity in MCF-7 tumor-bearing mice than doxorubicin hydrochloride (DOX⋅HCl) and DOX-loaded micelles without FA modification. Taken together, FA-SG micelles could be an effective carrier for targeted drug delivery. Graphical abstract