目的 制备舒林酸纳米混悬剂，并考察其对肿瘤组织的抗肿瘤作用。方法 以油酸钠为稳定剂，通过反溶剂沉淀法制备舒林酸纳米混悬剂，考察其粒径大小、分散指数、电位及颗粒形状，采用MTT比色法使用乳腺癌细胞MCF-7、4T1进行体外抗肿瘤药效评价，采用4T1荷瘤小鼠进行体内抗肿瘤评价。结果 舒林酸纳米粒形状为球形，分散指数值小于0.3，平均粒径为（264.1±2.9）nm。相比较于游离药物，纳米粒显著提高了舒林酸对乳腺癌细胞的抑制作用，对MCF-7、4T1的IC₅₀值分别为（22.1±4.6）、（19.2±1.2）μg/mL，体内抑瘤率为（35.4±18.8）%。结论 将舒林酸制备成纳米粒后，拓宽了舒林酸的给药途径，显著增强其抗肿瘤作用。

Objective To prepare sulindac nanosuspensions, and study its anti-tumor effect. Methods Sulindac nanosuspensions were prepared with sodium oleate as stabilizer. The quality of nanosuspension was evaluated by particle size, dispersion index (PDI), potential and electron micrograph morphology. MTT colorimetric assay and MCF-7 cells and 4T1 were used for in vitro antitumor effect, and 4T1 tumor-bearing mice were used for anti-tumor effect in vivo. Results The shape of sulindac nanosuspensions was spherical, the PDI value was less than 0.3, and the particle size was (264.1±2.9) nm. The anti-tumor effect was significantly improved compared with the drug substance in vitro and the IC₅₀ values for MCF-7 and 4T1 were (22.1±4.6) and (19.2±1.2) μg/mL. Tumor inhibition rate in vivo was (35.4±18.8)%. Conclusion The preparation of sulindac into nanoparticles by nano preparation technology broadened the drug delivery pathway of sulindac and significantly enhanced the anti-tumor effect.

R285.5

国家自然基金-广东联合基金资助项目（U1401223）