齐墩果酸与羟基喜树碱共组装纳米粒的制备及体外抗肿瘤评价

张廷恩; 杨文卓; 张林慧; 黄小超; 侯晓桐; 沈鹏宇; 左丽维; 皮佳鑫

doi:10.13748/j.cnki.issn1007-7693.20233588

齐墩果酸与羟基喜树碱共组装纳米粒的制备及体外抗肿瘤评价

Preparation and in Vitro Anti-tumor Evaluation of Oleanolic Acid and Hydroxycamptothecin Co-assembled Nanoparticles

摘要

摘要:
目的制备齐墩果酸-羟基喜树碱共组装纳米粒(oleanolic acid and hydroxycamptothecin co-assembled nanoparticles，OA-HCPT NPs)，优化其制备工艺，进行药剂学性质研究和体外抗肿瘤活性评价。
方法采用抗溶剂沉淀结合超声法制备OA-HCPT NPs；采用动态光散射法、扫描电子显微镜、傅里叶变换红外光谱等对OA-HCPT NPs的粒径、Zeta电位、形态、含量和稳定性进行研究；采用CCK-8法考察OA-HCPT NPs对结肠癌细胞HCT116及肺癌细胞A549的增殖抑制作用。
结果制备所得OA-HCPT NPs形态为类球形，粒径和电位分别为(245.1±16.4)nm、(−10.1±0.5)mV。傅里叶变换红外光谱结果表明OA-HCPT NPs较原料药及物理混合物特征峰发生明显变化。体外细胞毒性试验表明OA、HCPT对HCT116细胞及A549细胞均有抑制作用，且呈浓度依赖性，OA-HCPT NPs分别在20~100 μmol·L⁻¹和10~50 μmol·L⁻¹时对HCT116细胞及A549细胞的抑制作用显著增强(P<0.01或P<0.05)。
结论抗溶剂沉淀结合超声法制备OA-HCPT NPs方法可行，制剂平均粒径较小且分布均匀；OA-HCPT NPs对HCT116细胞及A549细胞的体外增殖抑制作用显著增强。

Abstract:
OBJECTIVE To construct oleanolic acid and hydroxycamptothecin co-assembled nanoparticles(OA-HCPT NPs), optimize their preparation, study their pharmaceutical properties and evaluate their anti-tumor efficacy in vitro.
METHODS The OA-HCPT NPs were prepared by anti-solvent precipitation combined with ultrasound. The particle size, Zeta potential, morphology, content and stability of OA-HCPT NPs were studied by the dynamic light scattering, scanning electron microscopy and Fourier transform infrared spectrometry. The inhibitory effect of OA-HCPT NPs on the proliferation of colon cancer HCT116 cells and lung cancer cell A549 was detected by CCK-8.
RESULTS The OA-HCPT NPs was spherical in appearance, and the particle size and Zeta potential were(245.1±16.4)nm and (−10.1±0.5)mV, respectively. Fourier transform infrared spectrum results showed that the characteristic peaks of OA-HCPT NPs were significantly different from that of raw materials and physical mixtures. In vitro cytotoxicity test showed that OA and HCPT inhibited both HCT116 cells and A549 cells in a concentration-dependent manner. OA-HCPT NPs significantly increased the inhibition of HCT116 cells and A549 cells at 20−100 μmol·L⁻¹ and 10−50 μmol·L⁻¹, respectively(P<0.01 or P<0.05).
CONCLUSION The OA-HCPT NPs can be obtained by a feasible anti-solvent precipitation combined with ultrasound method with small particle size and uniform size distribution. OA-HCPT NPs significantly enhance the inhibitory effects on HCT116 cell and A549 cell proliferation in vitro.

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