Yokoyama M, Fukushima S, Uehara R, Okamoto K, Kataoka K, Sakurai Y, Okano T
Institute of Biomedical Engineering, Tokyo Women's Medical College, Japan.
J Control Release. 1998 Jan 2;50(1-3):79-92. doi: 10.1016/s0168-3659(97)00115-6.
An anticancer drug adriamycin (ADR) was incorporated into polymeric micelles forming from poly(ethylene glycol)-poly(aspartic acid) block copolymer by chemical conjugation and physical entrapment. Structural stability of the polymeric micelles was found to be dependent on both the contents of chemically conjugated and physically entrapped ADR. The polymeric micelle with high contents of the chemically conjugated ADR and the physically entrapped ADR expressed very high in vivo antitumor activity against murine C 26 tumor, while the polymeric micelle with only the chemically conjugated ADR showed negligible in vivo activity. This indicates that the physically entrapped ADR played a major role in antitumor activity in vivo. For the polymeric micelle with the high ADR contents, it was found that a dimer of adriamycin molecules formed and that this dimer was physically entrapped in the inner core of the micelle as well as intact ADR.
一种抗癌药物阿霉素（ADR）通过化学偶联和物理包封被载入由聚（乙二醇）-聚（天冬氨酸）嵌段共聚物形成的聚合物胶束中。发现聚合物胶束的结构稳定性取决于化学偶联和物理包封的阿霉素的含量。化学偶联阿霉素和物理包封阿霉素含量高的聚合物胶束对小鼠C26肿瘤表现出非常高的体内抗肿瘤活性，而仅含有化学偶联阿霉素的聚合物胶束在体内的活性可忽略不计。这表明物理包封的阿霉素在体内抗肿瘤活性中起主要作用。对于阿霉素含量高的聚合物胶束，发现形成了阿霉素分子二聚体，并且该二聚体与完整阿霉素一起被物理包封在胶束的内核中。
