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首页> 外文期刊>Journal of drug targeting >Chloramphenicol-incorporated poly lactide-co-glycolide (PLGA) nanoparticles: formulation, characterization, technetium-99m labeling and biodistribution studies.
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Chloramphenicol-incorporated poly lactide-co-glycolide (PLGA) nanoparticles: formulation, characterization, technetium-99m labeling and biodistribution studies.

机译：氯霉素结合的聚丙交酯-共-乙交酯（PLGA）纳米颗粒：制剂，表征，tech 99m标记和生物分布研究。

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摘要

Chloramphenicol-loaded (CHL) poly-d,l-lactic-co-glycolic acid (PLGA) nanoparticles (NPs) were prepared by emulsification solvent evaporation technique either by using polyvinyl alcohol (PVA) as emulsion stabilizer or polysorbate-80 (PS-80) as surfactant and characterised by transmission electron microscopy, zeta-potential measurements. The NPs were radiolabeled with technetium-99m ((99m)Tc) by stannous reduction method. Labeling conditions were optimised to achieve high-labeling efficiency, in vitro and in vivo (serum) stability. The labeled complexes also showed very low transchelation as determined by DTPA challenge test. Biodistribution studies of (99m)Tc-labeled complexes were performed after intravenous administration in mice. The CHL-loaded PLGA NPs coated with PS-80 exhibited relatively high brain uptake with comparatively low accumulation in bone marrow to that of free drug and CHL-loaded PLGA NPs (PVA, used as emulsion stabilizer) at 24 h post injection time period. This indicates the usefulness of the above delivery system for prolonged use of the antibiotic.
机译：通过使用聚乙烯醇（PVA）作为乳液稳定剂或聚山梨酯80（PS-PS），通过乳化溶剂蒸发技术制备了负载氯霉素（CHL）的聚-d，l-乳酸-乙醇酸共聚物（PLGA）纳米粒子（NPs）。 80）作为表面活性剂，并通过透射电子显微镜，ζ电位测量进行表征。通过亚锡还原法将tech用99m（（99m）Tc）放射性标记。优化标记条件以实现高标记效率，体外和体内（血清）稳定性。标记的复合物还显示出非常低的转运，如通过DTPA激发试验所确定的。 （99m）Tc标记的复合物的生物分布研究是在小鼠静脉内给药后进行的。注射后24小时，与PS-80和PLL NPs（PVA，用作乳液稳定剂）相比，涂有PS-80的CHL负载的PLGA NPs在骨髓中的蓄积量相对较高，而在骨髓中的蓄积量则相对较低。这表明上述递送系统对于长时间使用抗生素是有用的。

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