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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Poly(D,L-lactide-co-glycolide)/montmorillonite nanoparticles for improved oral delivery of exemestane
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Poly(D,L-lactide-co-glycolide)/montmorillonite nanoparticles for improved oral delivery of exemestane

机译：聚（D，L-丙交酯-乙交酯）/蒙脱土纳米颗粒，用于改善依西美坦的口服给药

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The aim of this study was to develop poly(D,L-lactide-co-glycolide)/montmorillonite (PLGA/MMT) nanoparticles formulations for improved oral delivery of exemestane. Exemestane-loaded PLGA nanoparticles and PLGA/MMT nanoparticles were prepared by a modified solvent extraction/evaporation technology with vitamin E succinated polyethylene glycol 1000 (TPGS) as emulsifier. The content of MMT was estimated by thermal gravimetric analysis. The drug encapsulation efficiency and in vitro drug release kinetics were measured by high-performance liquid chromatography. The size, size distribution, surface charge and morphology of the exemestane-loaded nanoparticles were characterized using a Zetasizer Nano ZS and field emission scanning electron microscopy. The physical status of exemestane in the nanoparticles was characterized by differential scanning calorimetry. In vitro cellular uptake of coumarin-6-loaded nanoparticles was investigated by confocal laser scanning microscope, demonstrating that the fluorescence nanoparticles were internalized by Caco-2 cells (as an in vitro gastrointestinal model). The results of in vitro cytotoxicity experiment on MCF-7 cells (as a model of breast cancer cells) showed the exemestane-loaded nanoparticles resulted in lower cell viability versus the pure exemestane solution. The cytotoxicity against MCF-7 cells for exemestane-loaded nanoparticles and pure exemestane solution was dependent on the drug concentration and incubation time. In conclusion, this study indicates the capability of PLGA nanoparticles and PLGA/MMT nanoparticles in enhancing the oral delivery of exemestane.
机译：这项研究的目的是开发聚（D，L-丙交酯-乙交酯-乙交酯）/蒙脱石（PLGA / MMT）纳米颗粒制剂，以改善依西美坦的口服递送。通过改良的溶剂萃取/蒸发技术，以维生素E琥珀酸聚乙二醇1000（TPGS）作为乳化剂，制备了装载依西美坦的PLGA纳米颗粒和PLGA / MMT纳米颗粒。 MMT的含量通过热重量分析法估算。用高效液相色谱法测定药物的包封率和体外释药动力学。使用Zetasizer Nano ZS和场发射扫描电子显微镜表征了装载有依西美坦的纳米颗粒的尺寸，大小分布，表面电荷和形态。通过差示扫描量热法表征了依西美坦在纳米颗粒中的物理状态。通过共聚焦激光扫描显微镜研究了装载香豆素6的纳米颗粒在体外的细胞摄取，表明荧光纳米颗粒已被Caco-2细胞内化（作为体外胃肠道模型）。对MCF-7细胞（作为乳腺癌细胞的模型）进行体外细胞毒性实验的结果表明，与纯依西美坦溶液相比，载有依西美坦的纳米颗粒导致细胞活力较低。装载依西美坦的纳米颗粒和纯依西美坦溶液对MCF-7细胞的细胞毒性取决于药物浓度和孵育时间。总之，这项研究表明PLGA纳米颗粒和PLGA / MMT纳米颗粒具有增强依西美坦口服递送的能力。

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