Open AccessReduction of the Side Effects of an Antitumor Agent, KRN5500, by Incorporation of the Drug into Polymeric Micelles
Author(s) -
Matsumura Yasuhiro,
Yokoyama Masayuki,
Kataoka Kazunori,
Okano Teruo,
Sakurai Yasuhisa,
Kawaguchi Takanori,
Kakizoe Tadao
Publication year - 1999
Publication title -
japanese journal of cancer research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.035
H-Index - 141
eISSN - 1349-7006
pISSN - 0910-5050
DOI - 10.1111/j.1349-7006.1999.tb00675.x
Subject(s) - micelle , in vivo , drug , in vitro , pharmacology , toxicity , chemistry , necrosis , biological activity , biochemistry , medicine , biology , organic chemistry , microbiology and biotechnology , aqueous solution
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.