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新型聚-DL-乳酸-聚己内酯共聚物柔性药物释放系统,用于环丙沙星的持续释放。

Novel poly-DL-lactide-polycaprolactone copolymer based flexible drug delivery system for sustained release of ciprofloxacin.

机构信息

Department of Pharmaceutical Sciences, University of the Sciences in Philadelphia, 600 S. 43rd Street, Philadelphia, PA 19104, USA.

出版信息

Drug Deliv. 2011 May;18(4):236-45. doi: 10.3109/10717544.2010.528070. Epub 2010 Dec 28.

DOI:10.3109/10717544.2010.528070
PMID:21189060
Abstract

This research evaluated 7525DLPCL for soft flexible drug delivery systems. The effect of ciprofloxacin hydrochloride (CIP) loading at three levels (10, 20, and 30%), on thermo-mechanical properties was studied. CIP release was monitored for 12 weeks. Addition of CIP to 7525DLPCL caused an increase in compressive modulus of 7525DLPCL. CIP release was found to be sigmoidal with two phenomena (apart from a minor burst) contributing to release-diffusion and later diffusion plus erosion. An increased burst was observed with greater CIP loading and the majority of CIP (> 70%) was released as an effect of diffusion plus erosion. Additional factors, like the effect of CIP particle size, had no significant effect on drug release. Change in the implant shape from a cylinder (5 mm diameter; 3 mm thickness) to disc (6 mm diameter, 0.5 mm thickness) also failed to show a significant impact on drug release. Erosion of 7525DLPCL is a major contributing factor towards this release and other factors like shape of implants and particle size of drug have little effect on CIP release. Such flexible drug delivery systems offer new avenues for long-term skeletal drug delivery of antibiotics for conditions like osteomyelitis or periodontitis.

摘要

本研究评估了 7525DLPCL 用于软弹性药物传递系统。研究了三种浓度(10%、20%和 30%)的盐酸环丙沙星(CIP)负载对热机械性能的影响。监测了 12 周的 CIP 释放情况。向 7525DLPCL 中添加 CIP 会导致 7525DLPCL 的压缩模量增加。CIP 的释放呈 S 形,两种现象(除了轻微的突释外)有助于释放-扩散,随后是扩散加侵蚀。随着 CIP 负载的增加,突释增加,并且大多数 CIP(>70%)由于扩散加侵蚀而释放。其他因素,如 CIP 粒径的影响,对药物释放没有显著影响。将植入物的形状从圆柱体(5mm 直径;3mm 厚度)改变为圆盘(6mm 直径,0.5mm 厚度)也未能显示出对药物释放的显著影响。7525DLPCL 的侵蚀是这种释放的主要因素,而其他因素,如植入物的形状和药物的粒径,对 CIP 的释放影响不大。这种灵活的药物输送系统为治疗骨髓炎或牙周炎等疾病的抗生素的长期骨骼药物输送提供了新途径。

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