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Paclitaxel-loaded polyester nanoparticles prepared by spray-drying technology: in vitro bioactivity evaluation

机译:通过喷雾干燥技术制备的载有紫杉醇的聚酯纳米粒子:体外生物活性评估

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摘要

Paclitaxel (PTX), an antimicrotubular agent used in the treatment of ovarian and breast cancer, was encapsulated in nanoparticles (NPs) of poly(lactide-co-glycolide) (PLGA) and poly(ε-caprolactone) (PCL) polymers using the spray-drying technique. Morphology, size distribution, drug encapsulation efficiency, thermal degradation and drug release were characterized. MCF7 cells were employed to evaluate the efficacy of the systems on cell cycle and cytotoxicity. The particle size was in the range 0.8-1 μm. The incorporation efficiency of PTX was more than 80% in all NPs obtained. In vitro drug release took place during 35 days, and drug release rates were in the order PCL > PLGA 50:50 > PLGA 75:25. Unloaded NPs showed to be cytocompatible at MCF7 cells. PTX-loaded NPs demonstrated the release of the drug block cells in the G2/M phase. All PTX-loaded formulations showed their efficacy in killing MCF7 cells, mainly PTX-loaded PLGA 50:50 and PLGA 75:25 that cause a decrease in cell viability lower than 20%.
机译:紫杉醇(PTX)是一种用于治疗卵巢癌和乳腺癌的抗微管药,使用喷雾干燥技术。表征了形态,尺寸分布,药物包封效率,热降解和药物释放。 MCF7细胞用于评估系统对细胞周期和细胞毒性的功效。粒度在0.8-1μm的范围内。在所有获得的NP中,PTX的掺入效率均超过80%。体外药物释放发生在35天之内,药物释放速率依次为PCL> PLGA 50:50> PLGA 75:25。卸载的NP在MCF7细胞上显示出细胞相容性。载有PTX的NPs在G2 / M期证明了药物阻断细胞的释放。所有装载PTX的制剂均显示出杀死MCF7细胞的功效,主要是装载PTX的PLGA 50:50和PLGA 75:25,它们会导致细胞活力降低低于20%。

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