用于骨化三醇递送的PLGA纳米颗粒

M. J. Ramalho, J. Loureiro, B. Gomes, Manuela F. Frasco, M. Coelho, M. C. Pereira
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引用次数: 15

摘要

骨化三醇是维生素D3的活性代谢物,是一种潜在的抗癌剂,但也有一些缺点。因此,必须开发新的治疗策略,如特定的药物输送系统,以克服这些限制。本研究的目的是制备聚丙交酯-乙醇酸酯纳米颗粒作为骨化三醇的载药载体。首先以胆骨化醇为药物模型,对维生素/聚合物比和超声时间两个配方参数进行了研究和探讨。然后,制备了具有可控尺寸和性能的骨化三醇负载的聚丙交酯纳米颗粒。纳米颗粒在储存条件下保持稳定数周,并使用冷冻保护剂成功冻干以延长其保质期。使用两种人类癌细胞系S2-013和A549进行的体外研究表明,裸PLGA NPs具有生物相容性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
PLGA nanoparticles for calcitriol delivery
Calcitriol, the active metabolite of Vitamin D3, is a potential anticancer agent but exhibits several drawbacks. Therefore, new therapeutic strategies, as specific drug delivery systems, must be developed in order to overcome those limitations. The aim of this work was to prepare poly(lactide-coglycolide) nanoparticles as drug delivery vehicles for calcitriol. Two formulation parameters, vitamin/polymer ratio and sonication time, were firstly studied and discussed using cholecalciferol as a drug model. Then, calcitriol-loaded poly(lactide-coglycolide) nanoparticles with controlled sizes and properties were prepared. The nanoparticles remained stable at storage conditions for several weeks and they were successfully lyophilized to increase their shelf-life using a crioprotectant. In vitro studies using two human cancer cell lines, S2-013 and A549, demonstrated that bare PLGA NPs are biocompatible.
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