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用于炔诺酮肟控释的戊二醛和乙二醛交联壳聚糖微球

Glutaraldehyde and glyoxal cross-linked chitosan microspheres for controlled delivery of centchroman.

作者信息

Gupta K C, Jabrail Fawzi Habeeb

机构信息

Department of Chemistry, Polymer Research Laboratory, Indian Institute of Technology, Roorkee 247 667, India.

出版信息

Carbohydr Res. 2006 May 1;341(6):744-56. doi: 10.1016/j.carres.2006.02.003. Epub 2006 Feb 24.

Abstract

Glutaraldehyde and glyoxal cross-linked microspheres were prepared using chitosan with different molecular weights (MWs) and degrees of deacetylation (DDAs) for sustained release of centchroman under physiological conditions. The DDA in chitosan was determined by different methods, and the samples were categorized as chitosan with low (48%), medium (62%), and high (75%) DDA. The size and shape of the microspheres were determined by scanning electron microscopy (SEM), and hydrophobicity was determined by adsorption of Rose Bengal dye on microspheres cross-linked with glutaraldehyde or glyoxal. The effect of MW, DDA, and degree of cross-linking in microspheres was studied on the degree of swelling, as well as by the loading and release of centchroman. The glyoxal cross-linked microspheres were more compact and hydrophobic and showed better sustained release in companion to chitosan microspheres and glutaraldehyde cross-linked microspheres. The linear fractional release of centchroman with the square root of time indicated a Fickian behavior of centchroman, and the microspheres also showed zero-order release kinetics for centchroman.

摘要

使用具有不同分子量(MWs)和脱乙酰度(DDAs)的壳聚糖制备戊二醛和乙二醛交联的微球,用于在生理条件下持续释放炔诺孕酮。壳聚糖中的脱乙酰度通过不同方法测定,样品分为低脱乙酰度(48%)、中脱乙酰度(62%)和高脱乙酰度(75%)的壳聚糖。通过扫描电子显微镜(SEM)测定微球的大小和形状,通过孟加拉玫瑰红染料在戊二醛或乙二醛交联的微球上的吸附来测定疏水性。研究了微球中分子量、脱乙酰度和交联度对溶胀程度以及炔诺孕酮的负载和释放的影响。与壳聚糖微球和戊二醛交联微球相比,乙二醛交联微球更致密、更疏水,并且显示出更好的持续释放性能。炔诺孕酮的线性分数释放与时间的平方根表明炔诺孕酮具有菲克行为,并且微球对炔诺孕酮也显示出零级释放动力学。

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