Reduction of the Side Effects of an Antitumor Agent, KRN5500, by Incorporation of the Drug into Polymeric Micelles |
| |
| Authors: | Yasuhiro Matsumura Masayuki Yokoyama Kazunori Kataoka Teruo Okano Yasuhisa Sakurai Takanori Kawaguchi Tadao Kakizoe |
| |
| Affiliation: | Department of Medicine;Institute of Biomedical Engineering, Tokyo Women's Medical University, 8–1 Kawadacho, Shinjuku-ku, Tokyo 162–8666,;Department of Materials Science, Graduate School of Engineering, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-8656 and;2nd Department of Pathology, Fukushima Medical University, School of Medicine, 1 Hikarigaoka, Fukushima-shi, Fukushima 960–1247,;The Director, National Cancer Center Hospital, 5-1-1 Tsukiji, Chuo-ku, Tokyo 104-0045, |
| |
| Abstract: | ![]()
For intravenous (i.v.) injection of a water-insoluble antitumor drug, KRN5500, we have successfully incorporated KRN5500 into polymeric micelles. In the present study, in vitro and in vivo antitumor activity against several human tumor cell lines and toxicity in mice of polymeric micelles incorporating KRN5500 (KRN/m) were evaluated in comparison with those of the prototype KRN5500. KRN/m was found to express similar antitumor activity to KRN5500 in the in vitro and in vivo systems. However, the vascular damage and liver focal necrosis observed with KRN5500 i.v. injection were not seen when KRN/m was administered i.v. Therefore, we expect that KRN/m will be superior to KRN5500 for clinical use and that the methodology of polymeric micelle drug carrier systems can be applied to other water-insoluble drugs. |
| |
| Keywords: | DDS Micelles KRN5500 |
|
|
