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分散介质流变性对乳化法制备聚合物微球的影响。

Influence of rheology of dispersion media in the preparation of polymeric microspheres through emulsification method.

机构信息

Pharmaceutics Research Projects Laboratory, Department of Pharmaceutical Sciences, Dr. H.S. Gour University, Sagar, 470003, India.

出版信息

AAPS PharmSciTech. 2009;10(4):1295-300. doi: 10.1208/s12249-009-9315-1. Epub 2009 Oct 31.

Abstract

Chitosan microspheres as drug delivery system have attained importance and attracted the attention of researchers in last few years. This study was aimed toward the elucidation of the effect of viscosity of external oil phase on the properties of microspheres prepared by emulsification method. Chitosan microspheres were prepared utilizing oil phase of different viscosity viz. castor oil, heavy liquid paraffin, light liquid paraffin and mixture of light paraffin, and petroleum ether (1:1 v/v ratio). Microspheres prepared in highly viscous castor oil exhibited an average size of 11.52+/-0.57 microm with a percentage drug entrapment of 43.12+/-2.14. On the other hand, very small microspheres of 3.15+/-0.04 microm and 68.87+/-1.03% drug entrapment were obtained when mixture of liquid paraffin and petroleum ether was utilized as oil phase. Effect of viscosity on percent mucoadhesion, percent drug entrapment, zeta potential, percent process yield, etc. of microspheres has been observed. In vitro drug release in phosphate buffer pH 7.4 was determined for different batch of microspheres. The results revealed a difference in the drug release pattern of the different microspheres prepared as a function of viscosity of different oil phase. Use of low viscose oil resulted in the formulation of spherical and small size microspheres. This work was a part of our ongoing thrust and project to develop microparticulate drug delivery system.

摘要

壳聚糖微球作为药物传递系统在近几年得到了重视,并引起了研究人员的关注。本研究旨在阐明外部油相的粘度对乳化法制备的微球性质的影响。利用不同粘度的油相(蓖麻油、重液体石蜡、轻液体石蜡和轻液体石蜡与石油醚的混合物(1:1v/v 比))制备壳聚糖微球。在高粘度的蓖麻油中制备的微球平均粒径为 11.52±0.57μm,药物包封率为 43.12±2.14%。另一方面,当使用液体石蜡和石油醚的混合物作为油相时,得到了粒径非常小的 3.15±0.04μm 和 68.87±1.03%药物包封率的微球。观察了粘度对微球的粘膜粘附百分比、药物包封百分比、Zeta 电位、工艺收率等的影响。在磷酸盐缓冲液 pH7.4 中测定了不同批次微球的体外药物释放。结果表明,不同粘度油相制备的微球的药物释放模式存在差异。使用低粘度油可形成球形和粒径较小的微球。这项工作是我们正在进行的开发微粒药物传递系统的项目的一部分。

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