Allen C, Han J, Yu Y, Maysinger D, Eisenberg A
Department of Chemistry, McGill University, 801 Sherbrooke Street West, Montreal, Canada.
J Control Release. 2000 Feb 3;63(3):275-86. doi: 10.1016/s0168-3659(99)00200-x.
Block copolymer micelles formed from copolymers of poly(caprolactone)-b-poly(ethylene oxide) (PCL-b-PEO) were investigated as a drug delivery vehicle for dihydrotestosterone (DHT). The physical parameters of the PCL-b-PEO micelle-incorporated DHT were measured, including the loading capacity of the micelles for DHT, the apparent partition coefficient of DHT between the micelles and the external medium and the kinetics of the release of DHT from the micelle solution. The MTT survival assay was used to assess the in vitro biocompatibility of PCL-b-PEO micelles in HeLa cell cultures. The biological activity of the micelle-incorporated DHT was evaluated in HeLa cells which had been co-transfected with the expression vectors for the androgen receptor and the MMTV-LUC reporter gene. The PCL-b-PEO micelles were found to have a high loading capacity for DHT and the release profile of the drug from the micelle solution was found to be a slow steady release which continued over a 1-month period. The biological activity of the micelle-incorporated DHT was found to be fully retained.
研究了由聚己内酯-b-聚环氧乙烷(PCL-b-PEO)共聚物形成的嵌段共聚物胶束作为二氢睾酮(DHT)的药物递送载体。测量了载有PCL-b-PEO胶束的DHT的物理参数,包括胶束对DHT的负载能力、DHT在胶束与外部介质之间的表观分配系数以及DHT从胶束溶液中的释放动力学。采用MTT存活试验评估PCL-b-PEO胶束在HeLa细胞培养物中的体外生物相容性。在已与雄激素受体和MMTV-LUC报告基因的表达载体共转染的HeLa细胞中评估了载有胶束的DHT的生物学活性。发现PCL-b-PEO胶束对DHT具有高负载能力,并且药物从胶束溶液中的释放曲线为缓慢稳定释放,持续1个月。发现载有胶束的DHT的生物学活性完全保留。