| 齐雪静,曹辉,赵宇,等.维生素 E聚乙二醇琥珀酸酯乳化 α-生育酚琥珀酸酯纳米乳的制备及体外抗肿瘤细胞活性评价[J].安徽医药,2024,28(2):240-245. |
| 维生素 E聚乙二醇琥珀酸酯乳化 α-生育酚琥珀酸酯纳米乳的制备及体外抗肿瘤细胞活性评价 |
| Preparation of α-tocopherol succinate nanoemulsion emulsified with TPGS and evaluation of its in vitro anticancer effect |
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| DOI：10.3969/j.issn.1009-6469.2024.02.007 |
| 中文关键词: α生育酚 纳米复合物 维生素 E聚乙二醇琥珀酸酯 纳米乳 体外抗肿瘤 |
| 英文关键词: Alpha-tocopherol Nanocomposites Tocopherol polyethylene glycol succinate (TPGS) Nanoemulsion In vitro anti. cancer |
| 基金项目:黑龙江省省属本科高校基本科研项目( 2019-KYYWF-1226) |
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| 中文摘要: |
| 目的探索以维生素 E聚乙二醇琥珀酸酯( TPGS)做乳化剂，制备 α-生育酚琥珀酸酯纳米乳(T-NE)，对纳米乳进行处方优化、制备方法以及制剂学性质考察，并且评价其体外抗肿瘤细胞活性。方法自 2022年 1―4月，先后通过水滴定法绘制伪三元相图，根据纳米乳区域确定最优处方，再采用乳化蒸发法制备，并对其进行了理化性质评价，包括类型确定、形态学考察、粒径大小和分布、 Zeta电位、载药量和稳定性，并通过细胞活力实验( MTT)进行体外抗肿瘤细胞活性评价。结果 T-NE的最优处方为 α-生育酚琥珀酸酯( α-TOS)、维生素 E、TPGS、聚乙二醇 400质量比 1∶1∶2∶1；所制得 T-NE为 O/W型，外观呈类球形且无粘连；载药量为( 20.15±1.91)g/L，粒径为( 258.8±3.48)nm，多分散指数( PDI)为 0.136±0.03，Zeta电位值为( .27.0± 0.46)mV；4℃和 25 ℃条件下放置稳定性良好，且适宜室温长期贮存；与游离的 α-TOS药物溶液相比， T-NE对人乳腺癌细胞系( MCF-7)及人卵巢癌细胞系( A2780)细胞具有更强的抑制作用， IC50值分别为 16.68 μmol/L和 7.50 μmol/L，且空白纳米乳基本无毒性作用。结论该实验制备的 T-NE外观均一呈类球形，粒径较小且分布均匀，载药量高稳定性好，同时表现出比游离 α-TOS更为优异的抗肿瘤细胞活性作用，具有良好的开发前景。 |
| 英文摘要: |
| Object To explore the preparation of α-tocopherol succinate nanoemulsion (T-NE) emulsified with tocopherol polyethyl.ene glycol succinate (TPGS), and investigate the formulation optimization, preparation method and pharmacological properties of nano.emulsion, and evaluate its antitumor cell activity in vitro.Methods From January to April 2022,The pseudo-ternary phase diagramswere drawn with water titration method, then the optimal prescription could be determined according to nanoemulsion region.T-NE was prepared by emulsion-evaporation method. The physicochemical properties were evaluated, including type determination, morphologi.cal investigation, particle size and distribution,Zeta potential, drug loading and stability, and antitumor cell activityin vitro was assayed by MTT assay.Results The optimal formula of T-NE was α-tocopherol succinate (α-TOS),Vitamin E, TPGS,polyethylene glycol 400 at the mass radio of 1∶1∶2∶1. T-NE prepared was O/W. The appearance was spherical and no adhesion. The average drug loading of α -TOS was (20.15±1.91)g/L.The average particle size of the nanoemulsion was (258.8±3.48)nm, the PDI was 0.136 ± 0.03, and the aver.age Zeta potential value was (.27.0±0.46)mV.T-NEhad excellent storage stability at 4 ℃ and 25 ℃,and was suitable for long-term stor. age at room temperature. Compared with free α-TOS solution, T-NE exhibited a stronger inhibitory effect on the activity of MCF-7 and A2780 cells,IC50 values were 16.68 μmol/L and 7.50 μmol/L, respectively.Meanwhile, blank accessories hardly did not affect the cell growth.Conclusions In this study, we have successfully developed T-NE with uniform and spherical appearance, small particle sizeand uniform distribution, high drug loading capacity and excellent stability.T-NE has a greater toxic effect than free α-TOS.Therefore, T-NE has good development prospects. |
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