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使用聚(L-乳酸)的微囊化。I:制备技术对微囊性质的影响。

Microencapsulation using poly(L-lactic acid). I: Microcapsule properties affected by the preparative technique.

作者信息

Jalil R, Nixon J R

机构信息

Chelsea Department of Pharmacy, King's College London.

出版信息

J Microencapsul. 1989 Oct-Dec;6(4):473-84. doi: 10.3109/02652048909031167.

Abstract

Microcapsules were prepared using a poly (L-lactic acid) (L = PLA), mol. wt. 43,200, by an emulsification and solvent evaporation technique. Phenobarbitone (PB) was used as a reference drug, (core to polymer ratio, 1:1). Both the o/w and w/o emulsion system were investigated in order to study microcapsule properties affected by the preparative technique. In the o/w system, dichloromethane (DCM) was used to dissolve L = PLA and PB and the resulting solution was dispersed in 1 per cent aqueous gelatin solution. Subsequent evaporation of the DCM resulted in the formation of microcapsules. PB was found to be poorly encapsulated within microcapsules from this o/w system. PB content in the microcapsules was found to improve using PB saturated aqueous gelatin solution as the continuum. In the w/o system, acetonitrile (AN) was used as a solvent for L-PLA and PB and light liquid paraffin (LLP), containing 2 per cent w/w Span 40, as the continuous phase. PB loading in the microcapsules was found to be very high from this w/o system. Microcapsules from the o/w system were very small compared to microcapsules obtained from the w/o system. The morphology of the microcapsules and the surface properties were found to be affected distinctly by the two techniques. Microcapsules from the o/w system showed a smooth and less porous surface, whereas a highly porous surface containing embedded PB crystals was found in the microcapsules from the w/o system.

摘要

采用乳化溶剂蒸发技术,以分子量为43200的聚(L-乳酸)(L = PLA)制备微胶囊。使用苯巴比妥(PB)作为参比药物(芯材与聚合物比例为1:1)。研究了水包油(o/w)和油包水(w/o)乳液体系,以考察制备技术对微胶囊性质的影响。在o/w体系中,用二氯甲烷(DCM)溶解L = PLA和PB,所得溶液分散于1%的明胶水溶液中。随后DCM的蒸发导致微胶囊的形成。发现该o/w体系制备的微胶囊对PB的包封效果较差。使用PB饱和明胶水溶液作为连续相时,微胶囊中的PB含量有所提高。在w/o体系中,用乙腈(AN)作为L-PLA和PB的溶剂,用含有2%(w/w)司盘40的轻质液状石蜡(LLP)作为连续相。发现该w/o体系制备的微胶囊中PB载药量非常高。与w/o体系制备的微胶囊相比,o/w体系制备的微胶囊非常小。发现两种技术对微胶囊的形态和表面性质有明显影响。o/w体系制备的微胶囊表面光滑且孔隙较少,而w/o体系制备的微胶囊表面高度多孔且含有嵌入的PB晶体。

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