通过将抗肿瘤药物KRN5500包封于聚合物胶束中来降低其副作用。
Reduction of the side effects of an antitumor agent, KRN5500, by incorporation of the drug into polymeric micelles.
作者信息
Matsumura Y, Yokoyama M, Kataoka K, Okano T, Sakurai Y, Kawaguchi T, Kakizoe T
机构信息
Department of Medicine, National Cancer Center Hospital, Tokyo.
出版信息
Jpn J Cancer Res. 1999 Jan;90(1):122-8. doi: 10.1111/j.1349-7006.1999.tb00675.x.
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 anti-tumor 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.
对于静脉注射一种水不溶性抗肿瘤药物KRN5500，我们已成功地将KRN5500载入聚合物胶束中。在本研究中，将载入KRN5500的聚合物胶束（KRN/m）与原型KRN5500相比，评估了其对几种人类肿瘤细胞系的体外和体内抗肿瘤活性以及在小鼠体内的毒性。发现KRN/m在体外和体内系统中表现出与KRN5500相似的抗肿瘤活性。然而，静脉注射KRN5500时观察到的血管损伤和肝局灶性坏死在静脉注射KRN/m时未出现。因此，我们期望KRN/m在临床应用中将优于KRN5500，并且聚合物胶束药物载体系统的方法可应用于其他水不溶性药物。
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