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Biodegradable hollow fibres for the controlled release of drugs

机译:可生物降解的中空纤维,用于控制药物的释放

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摘要

Biodegradable hollow fibres of poly-l-lactic acid (PLLA) filled with a suspension of the contraceptive hormone levonorgestrel in castor oil were implanted subcutaneously in rats to study the rate of drug release, rate of biodegradation and tissue reaction caused by the implant. The in vivo drug release was compared with the release in vitro using different release media. Fibres, disinfected with alcohol showed a zero-order release, both in vitro and in vivo, for over 6 months. Fibres, either γ-sterilized or disinfected with alcohol were harvested at time intervals ranging from 1 d to 6 months after implantation. Molecular weights of PLLA, tensile strengths, and remaining amounts of drug were determined as a function of time.ududThe tissue reaction can be described as a very moderate foreign body reaction with the initial presence of macrophages, which are gradually replaced by fibroblasts which form a collagen capsule. Molecular weight determinations of PLLA showed a decrease from an initial Mw of 1.59x10 5 to 5.5 × 10 4 in 4 months (after alcohol sterilization). A gradual decrease in fibre strength with time was observed which did not significantly impair the release rate of levonorgestrel.
机译:在大鼠皮下植入填充有避孕激素左炔诺孕酮悬浮液的聚-1-乳酸(PLLA)可生物降解的中空纤维,以研究其释放速率,生物降解速率和植入物引起的组织反应。使用不同的释放介质将体内药物释放与体外释放进行了比较。用酒精消毒的纤维在体外和体内均显示零级释放超过6个月。植入后1 d至6个月的时间间隔收获经过γ灭菌或酒精消毒的纤维。将PLLA的分子量,抗张强度和药物残留量作为时间的函数进行确定。 ud ud组织反应可以描述为非常缓慢的异物反应,最初存在巨噬细胞,然后逐渐被成纤维细胞所取代形成胶原蛋白胶囊。在四个月内(酒精灭菌后),PLLA的分子量测定结果显示,其初始Mw从1.59x10 5降低到5.5×10 4。观察到纤维强度随时间逐渐降低,这并未显着损害左炔诺孕酮的释放速率。

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