The behavior of PLGA microspheres containing rifampicin in alveolar macrophages
The behavior of PLGA microspheres containing rifampicin in alveolar macrophages
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DOI：
10.1016/j.colsurfb.2009.10.036
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发表时间：
2010-03-01
影响因子：
5.8
通讯作者：
Haga, M.
中科院分区：
文献类型：
--
作者：
Onoshita, T.;Shimizu, Y.;Haga, M.
我们开发了一种用于治疗结核病的肺部药物输送系统，该系统使用聚（乳酸-羟基乙酸）微球（RFP- plga MS）包封利福平（RFP），这是一种生物相容性聚合物。本研究采用大鼠肺泡巨噬细胞系NR8383，研究RFP- plga MS被巨噬细胞摄取后的行为和RFP的代谢。制备的RFP-PLGA质谱呈球形，平均直径1.9 μ m，被NR8383细胞以能量依赖的方式有效吸收。荧光显微镜研究表明，细胞摄取的RPF-PLGA MS在吞噬溶酶体中定位并降解。虽然RFP代谢产生了少量的3-甲酰基利福霉素SV (3-FRSV)，但几乎所有的RFP都保持不变。因此，我们认为RFP被释放到细胞质中，药物效力完好无损。基于这些结果，RFP- plga质谱将有效地递送抗结核药物，如RFP，并将成为肺部和其他组织的潜在有用的药物递送工具。(C) 2009 Elsevier B.V.版权所有
We have developed a pulmonary drug delivery system for the treatment Of tuberculosis using rifampicin (RFP) encapsulated in poly-(lactic-co-glycolic acid) microspheres (RFP-PLGA MS), which is a biocompatible polymer. In this study, the behavior of RFP-PLGA MS and the metabolism of RFP were investigated after their uptake by rnacrophages using the rat alveolar macrophage cell line, NR8383. The prepared RFP-PLGA MS were spherical with an average diameter of 1.9 mu m and were taken up effectively by NR8383 cells in an energy-dependent manner. It was shown by fluorescent microscopic studies that the RPF-PLGA MS taken up by the cells were localized in phago-lysosomes and then degraded. Although a small amount of 3-formylrifamycin SV (3-FRSV) was generated by the metabolism of RFP, almost all RFP remained unchanged. It was considered, therefore, that RFP was released into the cytosol with drug potency intact.Based on these results, RFP-PLGA MS will be effective for the delivery of antituberculosis drugs such as RFP, and will be a potentially useful drug delivery tool for Pulmonary and possibly other tissues as well. (C) 2009 Elsevier B.V. All rights reserved.