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载美罗培南聚(DL 乳酸-co-乙醇酸)纳米粒的制备及其控制释放研究

High glycolic poly (DL lactic co glycolic acid) nanoparticles for controlled release of meropenem.

机构信息

Department of Biotechnology, Indian Institute of Technology Madras, Chennai 600036, India.

出版信息

Biomed Pharmacother. 2013 Jun;67(5):431-6. doi: 10.1016/j.biopha.2013.02.004. Epub 2013 Feb 27.

DOI:10.1016/j.biopha.2013.02.004
PMID:23583192
Abstract

Nanospheres of low molecular weight poly lactic co glycolic acid (PLGA) with high glycolic acid content (10:90) and polylactic acid (PLA) are synthesized and loaded with meropenem, a broad spectrum antibiotic. The loading efficiency of the drug is 82 and 70% in PLGA 10:90 and PLA respectively. The rate of drug release is higher with PLGA 10:90 (3.2 μg/s) than with PLA (2.4 μg/s). Eighty and 60% of the encapsulated drug is released from the two polymers in 30 days respectively. Initial burst followed by sustained drug release is observed which is mathematically explained using a biphasic model. The drug release from the former polymer leads to two times lower E. coli growth than the release from the latter. The nanoparticles are biocompatible with no significant effect on the viability of 3T3 cells. This study indicates that PLGA 10:90 can be used for the delivery of antibiotics for interim period, especially for post orthopaedic surgeries.

摘要

低分子量聚乳酸-乙醇酸共聚物(PLGA)纳米球具有高乙醇酸含量(10:90)和聚乳酸(PLA)被合成并负载美罗培南,一种广谱抗生素。药物的载药量分别为 82%和 70%在 PLGA 10:90 和 PLA 中。PLGA 10:90 的药物释放速度(3.2μg/s)高于 PLA(2.4μg/s)。在 30 天内,两种聚合物分别释放了 80%和 60%的包裹药物。观察到初始突释后持续释放药物,这可以用两相模型进行数学解释。与后者相比,前一种聚合物释放的药物导致大肠杆菌生长降低了两倍。纳米粒子具有生物相容性,对 3T3 细胞的活力没有显著影响。这项研究表明,PLGA 10:90 可用于输送抗生素,特别是用于骨科手术后的临时治疗。

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