目的 制備舒林酸納米混懸劑，并考察其對(duì)腫瘤組織的抗腫瘤作用。方法 以油酸鈉為穩(wěn)定劑，通過反溶劑沉淀法制備舒林酸納米混懸劑，考察其粒徑大小、分散指數(shù)、電位及顆粒形狀，采用MTT比色法使用乳腺癌細(xì)胞MCF-7、4T1進(jìn)行體外抗腫瘤藥效評(píng)價(jià)，采用4T1荷瘤小鼠進(jìn)行體內(nèi)抗腫瘤評(píng)價(jià)。結(jié)果 舒林酸納米粒形狀為球形，分散指數(shù)值小于0.3，平均粒徑為（264.1±2.9）nm。相比較于游離藥物，納米粒顯著提高了舒林酸對(duì)乳腺癌細(xì)胞的抑制作用，對(duì)MCF-7、4T1的IC₅₀值分別為（22.1±4.6）、（19.2±1.2）μg/mL，體內(nèi)抑瘤率為（35.4±18.8）%。結(jié)論 將舒林酸制備成納米粒后，拓寬了舒林酸的給藥途徑，顯著增強(qiáng)其抗腫瘤作用。

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

國(guó)家自然基金-廣東聯(lián)合基金資助項(xiàng)目（U1401223）