期刊
JOURNAL OF PHARMACEUTICAL SCIENCES
卷 102, 期 4, 页码 1318-1332出版社
WILEY-BLACKWELL
DOI: 10.1002/jps.23470
关键词
10-hydroxycamptothecin; micelle; folate; chitosan; cancer; targeted drug delivery; cancer chemotherapy
资金
- Natural Science Foundation Committee of China [NSFC 81202467, 30672015, 30700779, 30800257, 30970776, 81000666, 81071194, 31050110123, 81171395]
- Ministry of Science and Technology for new drug development [2009ZX09310-004]
- Natural Science Foundation of Jiangsu Province in China [BK2012232, BK2011389]
- Natural Science Research Project of Universities in Jiangsu Province of China [11KJB350004]
- Priority Academic Program Development of Jiangsu Higher Education Institutions
10-Hydroxycamptothecin (HCPT) is an effective anticancer drug against various types of solid tumors. But the antitumor efficacy of HCPT is far from satisfactory because of its poor physicochemical properties, short circulating half-life, low stability, and nonspecific toxicity to normal tissues. Therefore, a targeted delivery strategy for HCPT to pathological sites is eagerly needed to overcome these limitations. The folate-modified N-succinyl-N-octyl chitosan (folate-SOC) micelle was chosen in this study and served as the targeted delivery system for HCPT to improve the antitumor efficacy. The water-insoluble anticancer drug HCPT was encapsulated into the folate-SOC micelles by the dialysis method. The near-spherical HCPT-loaded folate-SOC (HCPT/folate-SOC) micelles were formed in aqueous media with diameter of about 100200 nm. The HCPT/folate-SOC micelles displayed a good stability, reasonable drug-loading content (about 10%), and sustained release behavior for the water-insoluble HCPT. Compared with free HCPT, HCPT/folate-SOC micelles exhibited a significant enhancement of cellular uptake, higher cytotoxicity against folate receptor positive tumor cell (Bel-7402), excellent tumor-targeting capability and substantially better antitumor efficacy on the nude mice bearing Bel-7402 xenografts. These results demonstrate the potential of folate-SOC micelles as long-term stable and effective drug delivery systems in cancer therapy. (c) 2013 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 102:13181332, 2013
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