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改良乳液溶剂蒸发法制备核壳微球。

Modified emulsion solvent evaporation method for fabricating core-shell microspheres.

机构信息

Department of Pharmaceutics, Guiyang Medical University, No. 9 Beijing Road, 550004 Guiyang, China.

出版信息

Int J Pharm. 2013 Aug 16;452(1-2):227-32. doi: 10.1016/j.ijpharm.2013.05.020. Epub 2013 May 18.

Abstract

Solvent evaporation/extraction method is widely used for core-shell microspheres fabrication. However, the solvent evaporation rate, as an essential factor for polymers phase separation, is difficult to control which results in failure of complete phase separation between polymers. At the present study, the selective dissolution technique was used to improve the phase separation, and successfully fabricate core-shell microspheres for controlled delivery of drug with reduced initial burst release. The core-shell microspheres were prepared with poly(l-lactic-co-glycolic acid) (PLGA) and poly(l-lactic acid) (PLLA), and aspirin was used as model drug. Ethyl acetate (EtAc) was applied to ameliorate the phase separation during the preparation process. The ratio of dichloromethane (DCM)/EtAc seriously affected the distribution of polymer molecules and the formation of the core-shell structure. The internal morphology of the microspheres varied depending on the amount of EtAc. Core-shell structure with a dense core of PLLA and a shell of PLGA was well formed when 2 ml EtAc was used. The differential scanning calorimeters (DSC) results showed two distinct melting points which confirmed a completely polymer phased separation occurred. These microspheres showed sustained release of aspirin for at least 456 h with a little burst release (3.49%).

摘要

溶剂挥发/萃取法广泛用于核壳微球的制备。然而,作为聚合物相分离的关键因素,溶剂挥发速率难以控制,导致聚合物之间无法完全相分离。在本研究中,采用选择性溶解技术来改善相分离,成功制备了用于控制药物释放的核壳微球,降低了初始突释。以聚(乳酸-共-乙醇酸)(PLGA)和聚(乳酸)(PLLA)为原料,阿司匹林为模型药物,采用乙酸乙酯(EtAc)改善制备过程中的相分离。二氯甲烷(DCM)/EtAc 的比例严重影响聚合物分子的分布和核壳结构的形成。微球的内部形态取决于 EtAc 的用量。当使用 2 毫升 EtAc 时,形成了具有致密 PLLA 核和 PLGA 壳的核壳结构。差示扫描量热仪(DSC)结果显示两个明显的熔点,证实了完全的聚合物相分离。这些微球表现出阿司匹林的持续释放,至少 456 小时,突释很少(3.49%)。

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