Okamoto Y, Konno A, Togawa K, Kato T, Tamakawa Y, Amano Y
Br J Cancer. 1986 Mar;53(3):369-75. doi: 10.1038/bjc.1986.61.
Cisplatin (CDDP) was microcapsulated with ethylcellulose. Sustained release of CDDP from the microcapsule, particularly non-protein-bound CDDP, which should have antitumour activity, was demonstrated by an in vitro test. Using a bioassay, it was proven that the biological activity of CDDP was not affected by the microencapsulation process. When CDDP-mc were infused into the maxillary artery of patients with carcinoma of the maxillary sinus or oral cavity, the CDDP level in the circulating blood was significantly lower than that of the patients given non-encapsulated CDDP intravenously. However, a significantly higher CDDP concentration in tumour tissue was found in patients treated with CDDP-mc. These results suggest that selective arterial infusion of CDDP-mc could exert intensive topical antitumour effects on lesions through microinfarction effects, and prolonged drug release, with minimum systemic side effects.
顺铂(CDDP)用乙基纤维素进行了微囊化。体外试验证明了CDDP从微囊中持续释放,特别是未与蛋白质结合的具有抗肿瘤活性的CDDP。通过生物测定法证实,微囊化过程不影响CDDP的生物活性。当将顺铂微囊(CDDP-mc)注入上颌窦或口腔癌患者的上颌动脉时,循环血液中的CDDP水平明显低于静脉注射未微囊化CDDP的患者。然而,接受CDDP-mc治疗的患者肿瘤组织中的CDDP浓度明显更高。这些结果表明,选择性动脉内注入CDDP-mc可通过微梗死效应和延长药物释放,对病变发挥强烈的局部抗肿瘤作用,同时使全身副作用最小化。