新型棕榈酰谷氨酸-顺铂纳米粒的制备及其体外药效研究

发布时间：2018-06-11 10:56

本文选题：顺铂 + 棕榈酰谷氨酸　；参考：《沈阳药科大学学报》2016年12期

【摘要】：目的以棕榈酰谷氨酸为载体材料制备新型高载药顺铂纳米粒(palmoyl glutamic acid-cisplatin-nanoparticles,PG-CDDP-NPs),并对其体外抗肿瘤活性进行研究。方法采用肖顿-鲍曼缩合法合成棕榈酰谷氨酸两亲性材料,以所合成的材料为载体,利用其与顺铂的配位作用制备高载药新型顺铂纳米粒,并对所制备的PG-CDDP-NPs性质进行考察;以市售顺铂注射剂为对照,采用MTT法考察了PG-CDDP-NPs对人肝癌细胞HEPG2的体外抗肿瘤活性。结果合成了棕榈酰谷氨酸,并成功制备了高载药量的PG-CDDP-NPs,PG-CDDP-NPs粒径为(106.33±4.45)nm,粒度分布较均匀,包封率为(84.20±0.81)%,载药量质量分数高达(27.03±0.12)%。体外释放研究表明,PG-CDDP-NPs具有缓慢释药性质,24 h累积释放量质量分数仅为(28.74±1.37)%。体外药效学实验结果显示PG-CDDP-NPs和CDDP-S对高表达的人肝癌细胞HEPG2细胞的IC50值分别为3.54μmol·L-1和4.55μmol·L-1。结论以棕榈酰谷氨酸为载体材料可制备高载药量的顺铂纳米粒;PG-CDDP-NPs在体外对HEPG2细胞有杀伤作用,与顺铂注射剂相比,显示出较强的抑瘤效果,PG-CDDP-NPs是一种具有潜在应用价值的顺铂纳米制剂。
[Abstract]:Objective to prepare glutamic acid-cisplatin-nanoparticlesPG-CDDP-NPsN, a new type of high loaded cisplatin nanoparticles with palmoyl glutamic acid as carrier material, and to study its antitumor activity in vitro. Methods the amphiphilic materials of palmityl glutamic acid were synthesized by Shawton-Baumann method. The novel cisplatin nanoparticles were prepared by the coordination with cisplatin and the properties of PG-CDDP-NPs were investigated. The antitumor activity of PG-CDDP-NPs on human hepatoma cell line HEPG2 in vitro was investigated by MTT assay using Cisplatin injection as control. Results PG-CDDP-NPs with high drug loading were synthesized. The particle size of PG-CDDP-NPs was 106.33 卤4.45 nm, the particle size distribution was uniform, the entrapment efficiency was 84.20 卤0.81%, and the mass fraction of PG-CDDP-NPs was as high as 27.03 卤0.12. In vitro release studies showed that PG-CDDP-NPs had slow release properties and the mass fraction of cumulative release in 24 h was only 28.74 卤1.37%. The results of pharmacodynamics in vitro showed that the IC50 values of PG-CDDP-NPs and CDDP-S were 3.54 渭 mol L-1 and 4.55 渭 mol L-1, respectively. Conclusion PG-CDDP-NPs with high drug loading can be prepared by using palmityl glutamic acid as carrier material, which can kill HEPG2 cells in vitro, compared with cisplatin injection. PG-CDDP-NPs is a kind of potential application value of cisplatin nanopharmaceuticals.
【作者单位】：沈阳药科大学药学院;
【分类号】：R943;R96

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