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利福喷汀用于骨与关节结核给药系统的研制及体外特性研究

Development and in vitro characterization of drug delivery system of rifapentine for osteoarticular tuberculosis.

作者信息

Wu Jun, Zuo Yi, Hu Yunjiu, Wang Jian, Li Jidong, Qiao Bo, Jiang Dianming

机构信息

Department of Orthopedics, The First Affiliated Hospital of Chongqing Medical University, Chongqing, People's Republic of China.

Research Center for Nano-Biomaterials, Analytical and Testing Center, Sichuan University, Chengdu, Sichuan, People's Republic of China.

出版信息

Drug Des Devel Ther. 2015 Mar 5;9:1359-66. doi: 10.2147/DDDT.S78407. eCollection 2015.

DOI:10.2147/DDDT.S78407
PMID:25834394
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4357616/
Abstract

The study was to develop and evaluate the rifapentine-loaded poly(lactic acid-co-glycolic acid) (PLGA) microspheres (RPMs) for the treatment of osteoarticular tuberculosis to avoid critical side effects caused by oral regimens of antibiotics or intravenous antibiotics. The RPMs were spherical with rough surfaces, and elevated amounts of rifapentine in the formulation markedly increased the particle size and drug loading, while decreased the size distribution and entrapment efficiency. The highest drug loading and encapsulation efficiency of RPMs were 23.93%±3.93% and 88.49%±8.49%, respectively. After the initial rapid drug release, the release rate gradually decreased, and approximately 80% of the encapsulated rifapentine was released after 30 days of incubation. Moreover, RPMs could effectively inhibit the growth of Staphylococcus aureus. With increasing rifapentine content, the inhibition zones were continuously enlarged while the minimal inhibitory concentration values decreased. These results suggested that RPMs were bioactive and controlled release delivery systems for the treatment of osteoarticular tuberculosis.

摘要

本研究旨在开发并评估载利福喷丁的聚乳酸-乙醇酸共聚物（PLGA）微球（RPMs），用于治疗骨关节结核，以避免口服抗生素或静脉注射抗生素方案所引起的严重副作用。RPMs呈球形，表面粗糙，制剂中利福喷丁含量的增加显著增大了粒径和载药量，同时降低了粒径分布和包封率。RPMs的最高载药量和包封率分别为23.93%±3.93%和88.49%±8.49%。在最初的快速药物释放后，释放速率逐渐降低，孵育30天后，约80%的包封利福喷丁被释放。此外，RPMs可有效抑制金黄色葡萄球菌的生长。随着利福喷丁含量的增加，抑菌圈不断扩大，而最低抑菌浓度值降低。这些结果表明，RPMs是用于治疗骨关节结核的生物活性控释给药系统。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b00/4357616/9e3b01c584e8/dddt-9-1359Fig7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b00/4357616/c2b4db0e68b2/dddt-9-1359Fig1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b00/4357616/a33a2e20276f/dddt-9-1359Fig2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b00/4357616/2fad5b56148c/dddt-9-1359Fig3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b00/4357616/8ced895a7607/dddt-9-1359Fig4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b00/4357616/7fb5c24c39f1/dddt-9-1359Fig5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b00/4357616/489f8f1b142a/dddt-9-1359Fig6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b00/4357616/9e3b01c584e8/dddt-9-1359Fig7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b00/4357616/c2b4db0e68b2/dddt-9-1359Fig1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b00/4357616/a33a2e20276f/dddt-9-1359Fig2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b00/4357616/2fad5b56148c/dddt-9-1359Fig3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b00/4357616/8ced895a7607/dddt-9-1359Fig4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b00/4357616/7fb5c24c39f1/dddt-9-1359Fig5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b00/4357616/489f8f1b142a/dddt-9-1359Fig6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9b00/4357616/9e3b01c584e8/dddt-9-1359Fig7.jpg

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