期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 471, 期 1-2, 页码 28-36出版社
ELSEVIER
DOI: 10.1016/j.ijpharm.2014.05.010
关键词
pH-sensitive; Citraconic anhydride; Polymeric micelle; Drug delivery; Doxorubicin
资金
- National Science Foundation for Excellent Young Scholars [51222304]
- Young teachers' scientific research foundation of Sichuan University [2014SCU11015]
- National Science Foundation of China (NSFC) [31170921, 31370972, 51133004, 81361140343]
- National Basic Research Program of China (National 973 program) [2011CB606206]
- Program for Changjiang Scholars and Innovative Research Team in University [IRT1163]
A novel pH-sensitive polymeric micelle was reported. Methoxy poly(ethylene glycol)-b-poly(epsilon-caprolactone) copolymer with citraconic amide as pH-sensitive bond was synthesized (mPEG-pH-PCL). The copolymers self-assembled into micelles to encapsulate anticancer drug doxorubicin (DOX). The morphology, size and size distribution, drug release profile and in vitro anticancer activity of the DOX loaded mPEG-pH-PCL micelles were studied. The results showed that the mean size of the micelles was around 120 nm, the drug loading content and encapsulation efficiency of the mPEG-pH-PCL micelles were 6.8% and 54.3%, respectively. The mean diameter and size distribution of the mPEG-pH-PCL micelles increased significantly when soaking in medium with pH 5.5. The drug release of micelles in pH 5.5 was much faster than that in pH 7.4. The confocal laser microscopy and flow cytometry measurements indicated that the weak acidity of endosomes broke the citraconic amide bonds in the copolymer backbones and triggered the fast release of DOX. The in vitro IC50 of the drug loaded mPEG-pH-PCL micelles was lower than that of drug loaded polymeric micelles without pH-sensitivity to both HepG2 and 4T1 cancer cells. (C) 2014 Elsevier B.V. All rights reserved.
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