Journal
INTERNATIONAL JOURNAL OF PHARMACEUTICS
Volume 452, Issue 1-2, Pages 363-373Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2013.05.003
Keywords
Linear-dendritic block copolymers; pH-sensitive; Specific drug targeting; Cellular uptake; Pharmacokinetics
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Funding
- National Science and Technology of China for New Drug Development [2009ZX09310-004]
- Graduate Cultivation and Innovation of Jiangsu Province [CXLX11-0787]
- State Key Laboratory of Natural Medicines, China Pharmaceutical University [SKL-NMKF201222]
- Fundamental Research Funds, the Ministry of Education [JKY2009039]
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A novel amphiphilic linear-dendritic block copolymer, semi-polyamidoamine-b-poly(D,L-lactic acid) (PALA) was synthesized and evaluated for its potential as a drug delivery system in this study. PALA was self-assembled in aqueous solution to form nanomicelles with low critical micelle concentration; antitumor drug docetaxel (DTX) was successfully encapsulated into micelles. The prepared micelles demonstrated pH-induced charge conversion and dimension changes. In vitro drug release suggested susceptibility of DTX-loaded micelles to acidic microenvironment. Hemolysis and cytotoxicity testing also indicated in vitro biocompatibility of PALA. Pharmacokinetic study in rats proved that DTX-loaded PALA micelles enhanced the AUC of DTX and prolonged drug clearance in comparison to conventional DTX injection (Taxotere (R)). It was concluded that self-assembled micelles from linear-dendritic block copolymer PALA demonstrated potential for intracellular delivery of anticancer molecules, and that its safety and efficacy in chemotherapy should be further studied. (C) 2013 Elsevier B. V. All rights reserved.
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