Enhanced in vivo

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• 作者：Tomoyuki Okuda ; Shigeru Kawakami ; Yuriko Higuchi ; Taku Satoh ; Yoshimi Oka ; Masayuki Yokoyama ; Fumiyoshi Yamashita ; Mitsuru Hashida
• 关键词：Fenretinide ; 4-HPR ; Retinoid ; Polymeric micelle ; Controlled release ; Drug delivery system
• 刊名：International Journal of Pharmaceutics
• 出版年：2009
• 出版时间：21 May 2009
• 年：2009
• 卷：373
• 期：1-2
• 页码：100-106
• 全文大小：561 K

文摘

Fenretinide (N-(4-hydroxyphenyl)retinamide, 4-HPR) is a synthetic retinoid with high antitumor activity against a variety of malignant cells in vitro, and is a promising candidate for cancer chemoprevention and chemotherapy. To enhance the antitumor efficacy of 4-HPR in vivo, 4-HPR were encapsulated into polymeric micelles for tumor targeting by enhanced permeability and retention effects. 4-HPR encapsulated in poly(ethylene glycol)–poly(benzyl aspartate) block copolymer micelles were prepared by the evaporation method. The mean particle size of 4-HPR encapsulated in polymeric micelles was about 173 nm. After intravenous injection into tumor-bearing mice, the delivery of 4-HPR by polymeric micelles increased the blood concentration and enhanced the tumor accumulation of 4-HPR over the injection of the 4-HPR encapsulated in oil-in-water (O/W) emulsions. Tumor growth was significantly delayed following treatment by 4-HPR encapsulated in polymeric micelles, which demonstrated the improved in vivo antitumor efficacy of 4-HPR. In addition, 4-HPR encapsulated in polymeric micelles did not cause any body weight loss. These results suggest that polymeric micelles are a promising and effective carrier of 4-HPR in order to enhance tumor delivery and have potential application in the treatment of solid tumor.