Comparative Assessment of In Vitro Release Kinetics of Calcitonin Polypeptide from Biodegradable Microspheres
Comparative Assessment of In Vitro Release Kinetics of Calcitonin Polypeptide from Biodegradable Microspheres
复制标题
可生物降解微球降钙素多肽体外释放动力学的比较评估
DOI：
10.1080/15227950290097633
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发表时间：
2002
期刊：
影响因子：
6
通讯作者：
G. Betageri
中科院分区：
文献类型：
--
作者：
S. Prabhu;J. L. Sullivan;G. Betageri
本研究的目的是比较多肽药物降钙素(CT)的缓释注射微球的体外释放动力学，以优化聚丙交酯-乙交酯(PLGA)共聚生物可降解微球的药物释放特性。采用改进的溶剂挥发复乳法制备了微球。释放动力学研究在硅烷化试管和透析袋中进行，其中微球悬浮并孵育在磷酸盐缓冲盐水中，以固定的间隔采样，并使用改进的Lowry蛋白质分析程序分析药物含量。观察到最初的猝发，大约50%的药物在24小时内从微球中释放，75%在3天内释放。随后是3周的缓释期，在此期间另有10%-15%的药物释放。透析袋的药物释放较为缓慢，50%的CT在4天后才释放，75%的CT在12天后释放。扫描电子显微镜显示，悬浮在水溶液中5天的球形颗粒具有通道状结构和多孔的表面。差示扫描量热法研究表明，CT在微球中以非晶态和晶态的混合形式存在。总体而言，这些研究表明，CT从PLGA微球中持续释放3周是可行的，从透析袋中释放药物比从管子中释放更可预测。
The objective of our study was to compare the in vitro release kinetics of a sustained-release injectable microsphere formulation of the polypeptide drug, calcitonin (CT), to optimize the characteristics of drug release from poly-(lactide-co-glycolide) (PLGA) copolymer biodegradable microspheres. A modified solvent evaporation and double emulsion technique was used to prepare the microspheres. Release kinetic studies were carried out in silanized tubes and dialysis bags, whereby microspheres were suspended and incubated in phosphate buffered saline, sampled at fixed intervals, and analyzed for drug content using a modified Lowry protein assay procedure. An initial burst was observed whereby about 50% of the total dose of the drug was released from the microspheres within 24 hr and 75% within 3 days. This was followed by a period of slow release over a period of 3 weeks in which another 10-15% of drug was released. Drug release from the dialysis bags was more gradual, and 50% CT was released only after 4 days and 75% after 12 days of release. Scanning electron micrographs revealed spherical particles with channel-like structures and a porous surface after being suspended in an aqueous solution for 5 days. Differential scanning calorimetric studies revealed that CT was present as a mix of amorphous and crystalline forms within the microspheres. Overall, these studies demonstrated that sustained release of CT from PLGA microspheres over a 3-week period is feasible and that release of drug from dialysis bags was more predictable than from tubes.
影响因子：
56.9
作者：
GREF, R;MINAMITAKE, Y;LANGER, R
通讯作者：
LANGER, R