可固化mPEG-PDLLA胶束作为载体的新型吲哚美辛口服给药系统的体外研究

Ammar Ouahab  沈  雁  平其能  涂家生

可固化mPEG-PDLLA胶束作为载体的新型吲哚美辛口服给药系统的体外研究

Ammar Ouahab 沈雁平其能涂家生

Solidified mPEG-PDLLA micelles as a novel oral delivery system of indomethacin

Ammar Ouahab

摘要

摘要:
本研究旨在制备吲哚美辛固化聚合物胶束 (IND-SPM), 并研究其体外释放特性。IND-SPM以交联聚维酮XL-10作为载体, 并以聚乙二醇单甲醚−聚乳酸嵌段共聚物 (mPEG-PDLLA) 作为药物载体, 通过溶液吸收法, 用旋转蒸发仪蒸发溶剂后制得吲哚美辛固化聚合物胶束 (IND-SPM)。取IND 20 mg, 以PBS 250 mL为溶出介质进行体外溶出度实验。结果表明, 30 min内吲哚美辛的释放量高于90% (w/w)。DSC, ¹H NMR和SEM结果证明IND被包裹在mPEG-PDLLA中。随着聚合物的用量的增加,吲哚美辛的溶解度可提高4.6倍。IND-SPM适用于开发成片剂或胶囊剂。

Abstract:
In this study, indomethacin (IND) loaded solidified-polymeric micelles (IND-SPM) were prepared. Their in vitro characteristics were investigated. Methoxy-poly(ethylene glycol) poly(D, L-lactide) copolymer (mPEG-PDLLA) was used as IND carrier. The preparation of IND-SPM was conducted by solution-absorption method and evaporation by rotary evaporator. Polyplasdone XL-10 was used as adsorbent. The solution-absorption method was conducted by the following procedure; IND and mPEG-PDLLA were dissolved in acetone, followed by addition of polyplasdone XL-10 and stirred to obtain a suspension. The powder of IND- SPM was simply obtained after the organic solvent was completely evaporated. More than 90% (w/w) of IND (20 mg) in the powder was dissolved in 250 mL PBS within 30 min. DSC, ¹H NMR and SEM results proved that IND was encapsulated within mPEG-PDLLA. The solubility of IND in the system increased 4.6 times with the highest amount of copolymer. The solidified particles were found to be suitable for the formulation of tablets or capsules.

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