期刊
JOURNAL OF CONTROLLED RELEASE
卷 170, 期 1, 页码 74-82出版社
ELSEVIER
DOI: 10.1016/j.jconrel.2013.04.024
关键词
Oral delivery; Nanoparticles; Taurocholic acid; Cancer therapy
资金
- National Research Foundation of Korea (NRF)
- Ministry of Education, Science and Technology [2010-0021427]
- National Research Foundation of Korea [2010-0021427] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
We have synthesized taurocholic acid (TCA) linked heparin-docetaxel (DTX) conjugates for oral delivery of anticancer drug. The ternary biomolecular conjugates formed self-assembly nanoparticles where docetaxel was located inside the core and taurocholic acid was located on the surface of the nanoparticles. The coupled taurocholic acid in the nanoparticles had enhanced oral absorption, presumably through the stimulation of a bile acid transporter of the small intestine. The oral absorption profile demonstrated that the concentration of the conjugates in plasma is about 6 fold higher than heparin alone. An anti-tumor study in MDA-MB231 and KB tumor bearing mice showed significant tumor growth inhibition activity by the ternary biomolecular conjugates. Ki-67 histology study also showed evidence of anticancer activity of the nanoparticles. Finally, non-invasive imaging using a Kodak Molecular Imaging System demonstrated that the nanoparticles were accumulated efficiently in tumors. Thus, this approach for oral delivery using taurocholic acid in the ternary biomolecular conjugates is promising for treatment of various types of cancer. (C) 2013 Elsevier B.V. All rights reserved.
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