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目的 制备靶向齐墩果酸纳米粒(OA@TPGS-PLLA NPs),研究其抗肿瘤效果。方法 将聚乙二醇1000维生素E琥珀酸酯与丙交酯通过开环反应合成靶向TPGS-PLLA嵌段共聚物，采用核磁共振氢谱(1H-NMR)、红外光谱(FT-IR)、X射线衍射法(XRD)和热重法表征嵌段共聚物的理化性质。以TPGS-PLLA作为载体材料，齐墩果酸(OA)作为药物，采用乳化-溶剂蒸发法制备OA@TPGS-PLLA NPs。对所制备的纳米粒粒径大小、表面电位以及稳定性进行考察，并对OA@TPGS-PLLA NPs抗肿瘤效果进行初步评价。结果 通过1H-NMR、FT-IR、XRD和热重的实验，证明TPGS-PLLA合成成功。所制备的OA@TPGS-PLLA NPs展现出了良好的性能，粒径大小为75.83nm, PDI为0.229,电位为-68.7mV,稳定性优异。此外，MTT实验结果表明，OA@TPGS-PLLA NPs与齐墩果酸原料药相比，其对胶质瘤C6细胞的增殖抑制效果更为显著。结论 OA@TPGS-PLLA NPs成功制备，具有较好的抗胶质瘤效果。
Abstract：Objective To prepare the targeted oleanolic acid nanoparticles(OA@TPGS-PLLA NPs),and evaluate their anti-tumor activity In Vivo.Methods The targeted TPGS-PLLA block copolymer was synthesized through a ring-opening reaction of D-α-tocopheryl polyethylene glycol 1000 succinate(TPGS) and lactide.The physicochemical properties of the block copolymer were characterized by protonnuclear magnetic resonance spectroscopy(1H-NMR),infrared spectroscopy(FT-IR),X-ray diffraction spectroscopy(XRD),and thermogravimetric analysis(TGA).OA@TPGS-PLLA NPs were prepared by the emulsion-solvent evaporation method by using TPGS-PLLA as the carrier material and oleanolic acid(OA) as the drug.The particle size, zeta potential, and stability of the prepared nanoparticles were investigated, and the antitumor effect of OA@TPGS-PLLA NPs was preliminarily evaluated.Results The successful synthesis of OA@TPGS-PLLA was confirmed by the experimental results of 1H-NMR,FT-IR,XRD and TGA.The prepared OA@TPGS-PLLA NPs exhibited excellent physicochemical, with a particle size of 75.83nm, a PDI of 0.229,a zeta potential of-68.7mV,and outstanding stability.In addition, the results of the MTT assay showed that OA@TPGS-PLLA NPs had a more significant inhibitory effect on the proliferation of glioma C6 cells, when compared with the raw oleanolic acid drug.Conclusion OA@TPGS-PLLA NPs can be successfully prepared and exhibits good anti-glioma effects.
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基本信息:
DOI：10.16751/j.cnki.2095-4646.2025022607
中图分类号:R943
引用信息:
[1]程丽媛,朱灵,彭小航等.载齐墩果酸纳米粒的制备及体外抗肿瘤效果初探[J].湖北科技学院学报(医学版),2025,39(04):289-293+272.DOI:10.16751/j.cnki.2095-4646.2025022607.
基金信息: