Yokoyama M, Okano T, Sakurai Y, Fukushima S, Okamoto K, Kataoka K
Institute of Biomedical Engineering, Tokyo Women's Medical University, Tokyo, Japan.
J Drug Target. 1999;7(3):171-86. doi: 10.3109/10611869909085500.
The anticancer drug, adriamycin (ADR), was incorporated by physical entrapment into polymeric micelles for selective delivery to a murine solid tumor colon adenocarcinoma 26 (C 26). In vivo antitumor activity of ADR was greatly enhanced by this incorporation into polymeric micelles. Using one polymeric micelle delivery system, the tumor completely disappeared at two doses, while free ADR exhibited a fair inhibition effect on tumor growth only at the maximum tolerated dose. Biodistribution analysis revealed that the physically entrapped micellar ADR accumulated at tumor sites in a highly selective manner. These results indicate that these polymeric micelles are a promising system for delivering hydrophobic anticancer drugs selectively to solid tumor sites using a passive targeting mechanism.
抗癌药物阿霉素（ADR）通过物理包封法被载入聚合物胶束中，以实现对小鼠实体瘤结肠腺癌26（C26）的选择性递送。通过将阿霉素载入聚合物胶束，其体内抗肿瘤活性得到了极大增强。使用一种聚合物胶束递送系统，在两种剂量下肿瘤完全消失，而游离阿霉素仅在最大耐受剂量时才对肿瘤生长表现出一定的抑制作用。生物分布分析表明，物理包封的胶束阿霉素以高度选择性的方式在肿瘤部位蓄积。这些结果表明，这些聚合物胶束是一种很有前景的系统，可利用被动靶向机制将疏水性抗癌药物选择性地递送至实体瘤部位。
