Departamento de Materiales Radiactivos, Instituto Nacional de Investigaciones Nucleares, Ocoyoacac, Estado de Mexico, 52750. Mexico.
Departamento de Materiales Radiactivos, Instituto Nacional de Investigaciones Nucleares, Carretera Mexico-Toluca S/N., La Marquesa, Ocoyoacac, Estado de Mexico. Mexico.
Curr Pharm Des. 2017;23(23):3415-3422. doi: 10.2174/1381612823666170407143525.
Polymer-based nanoparticles as drug-delivery systems offer new therapeutic opportunities. Among them, ligand-mediated targeting, which increases selectivity and efficacy, allows controllable drug delivery. The aim of the this research was to prepare and characterize poly(methyl methacrylate) (PMMA) nanoparticles grafted with the -Arginine, Glycine, Aspartic Acid (RGD)- peptide sequence as a promising smart drug delivery system for Paclitaxel (PTX), directed at the sites of integrin receptor overexpression.
Nanoparticles were characterized by FT-IR and Raman spectroscopy, dynamic light scattering, zeta potential and transmission electron microscopy.
RGD-PMMA-PTX size distribution was 17.58 ± 7.45 nm with a zeta potential of -38.73 ± 5.62 mV. According to the boxLucas Model, PTX was incorporated into nanoparticles with an entrapment efficiency of 100% (evaluated by HPLC analysis). In vitro sustained release was determined, with the maximum release of 55% and 40% after 21 days at pH 5.3 and 7.4, respectively. The highest inhibition on cell proliferation was found with RGD-PMMA-PTX nanoparticles (90 %).
The obtained results showed that RGD-PMMA-PTX represents an attractive and suitable therapeutic approach for targeting overexpressed integrins in the cancer cells.
聚合物基纳米粒子作为药物传递系统提供了新的治疗机会。其中，配体介导的靶向作用提高了选择性和疗效，允许可控的药物传递。本研究的目的是制备和表征接枝有 -精氨酸、甘氨酸、天冬氨酸（RGD）-肽序列的聚甲基丙烯酸甲酯（PMMA）纳米粒子，作为一种有前途的智能药物传递系统，用于紫杉醇（PTX），针对整合素受体过表达的部位。
通过傅里叶变换红外光谱和拉曼光谱、动态光散射、Zeta 电位和透射电子显微镜对纳米粒子进行了表征。
RGD-PMMA-PTX 的粒径分布为 17.58 ± 7.45nm，Zeta 电位为-38.73 ± 5.62mV。根据 BoxLucas 模型，通过 HPLC 分析评估，PTX 以 100%的包封效率被纳入纳米粒子。在 pH 5.3 和 7.4 下分别测定了 21 天后的体外持续释放，最大释放率分别为 55%和 40%。RGD-PMMA-PTX 纳米粒子对细胞增殖的抑制作用最大（90%）。
研究结果表明，RGD-PMMA-PTX 是一种有吸引力和合适的治疗方法，可针对癌细胞中过度表达的整合素。
