Polymer delivery of camptothecin against 9L gliosarcoma: release, distribution, and efficacy.
作者： Phillip B. Storm , John L. Moriarity , Betty Tyler , Peter C. Burger , Henry Brem
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摘要: Camptothecin is a potent antineoplastic agent that has shown efficacy against multiple tumor lines in vitro; unfortunately, systemic toxicity limited its vivo efficacy. This the first study to investigate release, biodistribution, and of camptothecin from biodegradable polyanhydride polymer. Tritiated was incorporated into polymers were implanted intracranially 16 male Fischer 344 rats animals followed up 21 days post-implant. A concentration 11–45 μg camptothecin-sodium/mg brain tissue within 3 mm radius polymer disc, with levels 0.1 at outermost margin rat brain, 7 site implantation. These concentrations are therapeutic ranges for human glioma tested camptothecin-sodium vitro. The evaluated 9L gliosarcoma compared 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU). divided four groups. Group 1 (control) had median survival 17 days. 2 (3.8% BCNU polymer) 23 (P=0.006). (20% 25 (P=0.023). 4 (50% 69 (P<0.001). Drug loadings 20% 50% released intact 1000 h We conclude p(CPP : SA) releases camptothecin-sodium, produces tumoricidal levels, results little or no toxicity, prolongs model.
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