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负载万古霉素的羟丙基甲基纤维素微粒包埋于可注射的热敏壳聚糖水凝胶中。

Vancomycin-loaded HPMC microparticles embedded within injectable thermosensitive chitosan hydrogels.

作者信息

Mahmoudian M, Ganji F

机构信息

Department of Biomedical Engineering, Faculty of Chemical Engineering, Tarbiat Modares University, P. O. Box 14115-114, Tehran, Islamic Republic of Iran.

出版信息

Prog Biomater. 2017 May;6(1-2):49-56. doi: 10.1007/s40204-017-0066-x. Epub 2017 Apr 26.

Abstract

Antibiotic use is an essential method for the treatment of bacterial infections. In certain cases, antibiotics are not effective because of the distribution problems caused by physiological barriers in the body. Such problems are thought to be minimized by development of sustained release systems which involve implantation of antibiotic loaded polymeric systems directly to the site of infection. In this work, a new composite vancomycin hydrochloride release system based on HPMC microparticles and chitosan/glycerophosphate (Ch/Gp) thermosensitive hydrogel was designed for the aim of local treatment of osteomyelitis. Vancomycin-loaded HPMC microparticles (Van-HPMCs) were prepared by spray drying method. The SEM results showed that these particles had a mean diameter of 1.5-6.4 μm with a narrow size distribution and homogeneous particle production. Their drug encapsulation efficiency was 72.6%. The Van-HPMCs were embedded in an injectable Ch/Gp solution to introduce a composite drug release platform (Van/HPMC-Ch/Gp). In vitro release studies indicated that inclusion of the Van-HPMCs into the Ch/Gp hydrogel caused a reduction in both the release rate and total amount of vancomycin release, which suggests that HPMC microparticles entrapped into the Ch/Gp hydrogels showed more suitable sustained release kinetics for local antibiotics delivery.

摘要

抗生素的使用是治疗细菌感染的重要方法。在某些情况下,由于体内生理屏障导致的分布问题,抗生素并不有效。人们认为,通过开发持续释放系统可以将此类问题降至最低,该系统涉及将负载抗生素的聚合物系统直接植入感染部位。在这项工作中,为了局部治疗骨髓炎,设计了一种基于羟丙基甲基纤维素(HPMC)微粒和壳聚糖/甘油磷酸酯(Ch/Gp)热敏水凝胶的新型复合盐酸万古霉素释放系统。通过喷雾干燥法制备了负载万古霉素的HPMC微粒(Van-HPMCs)。扫描电子显微镜(SEM)结果表明,这些微粒的平均直径为1.5 - 6.4μm,粒径分布窄且颗粒生成均匀。其药物包封率为72.6%。将Van-HPMCs嵌入可注射的Ch/Gp溶液中,以引入复合药物释放平台(Van/HPMC-Ch/Gp)。体外释放研究表明,将Van-HPMCs加入Ch/Gp水凝胶中会导致万古霉素释放速率和释放总量降低,这表明包埋在Ch/Gp水凝胶中的HPMC微粒在局部抗生素递送方面表现出更合适的持续释放动力学。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cf6a/5433964/c57662d32c2a/40204_2017_66_Fig1_HTML.jpg

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