A biodegradable injectable thermoplastic for localized camptothecin delivery

被引:20
作者
Hatefi, A
Knight, D
Amsden, B [1 ]
机构
[1] Univ Alberta, Fac Pharm & Pharmaceut Sci, Edmonton, AB K7L 3N6, Canada
[2] Queens Univ, Dept Chem Engn, Kingston, ON K7L 3N6, Canada
基金
加拿大自然科学与工程研究理事会;
关键词
injectable thermoplastic; biodegradable polymer; camptothecin; stability;
D O I
10.1002/jps.20045
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Camptothecin is an example of a potent drug with a short half-life that would benefit from a localized drug depot system that maintains its stability prior to being released. For this reason, a thermoplastic, biodegradable polymer drug depot was prepared and characterized, and the in vitro release of camptothecin examined. epsilon-Caprolactone oligomers were prepared by ring-opening polymerization initiated by various alcohols. The polymers were characterized via differential scanning calorimeter (DSC) for thermal transitions, and via a parallel plate rheometer for melt viscosity. Camptothecin was loaded into the oligomers and released into PBS buffer. The viscosity of the oligomers was alterable by the initiator used. The oligomers were semi-crystalline with melting points between 37 and 45degreesC. Camptothecin was released from the oligomers in a diffusion-controlled manner, with the release rate increasing as the melt viscosity of the oligomer decreased. The unreleased camptothecin remained in its active lactone form for a period of up to 16 weeks. (C) 2004 Wiley-Liss, Inc. and the American Pharmacists Association.
引用
收藏
页码:1195 / 1204
页数:10
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