Kaur Manpreet, Sharma Sumit, Sinha V R
University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh 160014, India.
University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh 160014, India..
Mater Sci Eng C Mater Biol Appl. 2017 Mar 1;72:492-500. doi: 10.1016/j.msec.2016.11.092. Epub 2016 Nov 25.
Poly(lactic-co-glycolic acid) (PLGA) (75:25) and polycaprolactone (PCL) microspheres were fabricated for prolonged release of aceclofenac by parenteral administration. Microspheres encapsulating aceclofenac were designed to release the drug at controlled rate for around one month. Biodegradable microspheres were prepared by solvent emulsification evaporation method in different polymer:drug ratios (1:1, 2:1 and 3:1). After drug loading, PLGA and PCL microspheres showed a controlled size distribution with an average size of 11.75μm and 3.81μm respectively and entrapment efficiency in the range of 90±0.72% to 91.06±4.01% with PLGA and 83.01±2.13% to 90.4±2.11% with PCL. Scanning electron microscopy has confirmed good spherical structures of microspheres. The percent yield of biodegradable polymeric microspheres ranged between 30.95±10.14% to 92.84±3.15% and 47.33±4.72% to 80±3.60% for PLGA and PCL microspheres respectively. PLGA microspheres followed Higuchi release pattern while Korsmeyer-Peppas explained the release pattern of PCL microspheres. Stability studies of microspheres were also carried out by storing the preparations at 2-8°C for 30, 60 and 90days and evaluating them for entrapment efficiency, residual drug content and polymer drug compatability. In-vivo studies showed significant anti-inflammatory activity of microspheres upto 48hours using the carrageenan induced rat paw oedema model.
制备了聚乳酸-乙醇酸共聚物（PLGA）（75:25）和聚己内酯（PCL）微球，用于通过肠胃外给药实现醋氯芬酸的长效释放。包裹醋氯芬酸的微球设计为以可控速率释放药物约一个月。采用溶剂乳化蒸发法，以不同的聚合物与药物比例（1:1、2:1和3:1）制备了可生物降解的微球。载药后，PLGA和PCL微球呈现出可控的粒径分布，平均粒径分别为11.75μm和3.81μm，PLGA的包封率在90±0.72%至91.06±4.01%之间，PCL的包封率在83.01±2.13%至90.4±2.11%之间。扫描电子显微镜证实了微球具有良好的球形结构。可生物降解聚合物微球的产率分别为：PLGA微球在30.95±10.14%至92.84±3.15%之间，PCL微球在47.33±4.72%至80±3.60%之间。PLGA微球遵循Higuchi释放模式，而Korsmeyer-Peppas模型解释了PCL微球的释放模式。还通过将制剂在2-8°C下储存30、60和90天，并评估其包封率、残留药物含量和聚合物-药物相容性，对微球进行了稳定性研究。体内研究表明，使用角叉菜胶诱导的大鼠足趾水肿模型，微球在长达48小时内具有显著的抗炎活性。
