作者: Chuan Yang , Shao Qiong Liu , Shrinivas Venkataraman , Shu Jun Gao , Xiyu Ke
DOI: 10.1016/J.JCONREL.2015.03.027
关键词:
摘要: Amphiphilic polycarbonate/PEG copolymer with a star-like architecture was designed to facilitate unique supramolecular transformation of micelles vesicles in aqueous solution for the efficient delivery anticancer drugs. The star-shaped amphipilic block synthesized by initiating ring-opening polymerization trimethylene carbonate (TMC) from methyl cholate through combination metal-free organo-catalytic living and post-polymerization chain-end derivatization strategies. Subsequently, self-assembly polymer into nanosized anti-cancer drug studied. DOX physically encapsulated dialysis loading level significant (22.5% weight) DOX. Importantly, DOX-loaded nanoparticles self-assembled exhibited greater kinetic stability higher capacity than prepared cholesterol-initiated diblock analogue. advantageous disparity is believed be due (diblock copolymer) (star-like that possess core space as well ability such structures encapsulate effectively inhibited proliferation 4T1, MDA-MB-231 BT-474 cells, IC50 values 10, 1.5 1.0mg/L, respectively. injected 4T1 tumor-bearing mice enhanced accumulation tumor tissue permeation retention (EPR) effect. demonstrated growth inhibition free without causing body weight loss or cardiotoxicity. emanating provided requisite modification interfacial curvature generate high have potential use an carrier cancer therapy.