多西他赛脂质纳米粒的制剂学性质及其体外抗乳腺癌研究

Preparation Properties of Docetaxel Lipid Nanoparticles and Inhibition of Breast Cancer Cells in Vitro

目的研究多西他赛脂质纳米粒(LN/DTX)的理化性质及体外抑制乳腺癌细胞的效果。方法制备LN/DTX,超滤法测定包封率,透射电镜测定其粒径和形态,透析法测定体外释放行为,流式细胞术测定细胞摄取,MTT法测定其体外抗乳腺癌效果。结果最优处方制备的LN/DTX包封率为(93.43±2.1)%,外观为球形或类球形,粒径为120 nm;LN/DTX的体外释放在48 h内呈现缓慢释放效果,累计释放为(92.2±5.71)%;LN/DTX可显著增加肿瘤细胞摄取;MTT试验表明LN/DTX具有显著的抑制人乳腺癌细胞增殖的作用。结论 LN/DTX作为抗乳腺癌治疗药物的给药系统具有良好的应用前景。

OBJECTIVE To study the physicochemical properties of docetaxel lipid nanoparticles(LN/DTX) and inhibitory effect on breast cancer cells in vitro. METHODS LN/DTX was prepared.Ultrafiltration method was used to determine the envelope rate.Transmission electron microscope was used to determine the particle size and morphology.Dialysis method was used to determine the release behavior.Flow cytometry was used to detect cells uptake, and MTT method was used to determine the anti-breast cancer effect in vitro. RESULTS The encapsulation rate of LN/DTX prepared by the optimal prescription was(93.43±2.1)%. The appearance of LN/DTX was spherical or quasi-spherical, and the particle size was 120 nm.In vitro release of LN/DTX showed a slow release effect within 48 h, with a cumulative release of(92.2±5.71)%. MTT assay showed that LN/DTX had a significant inhibitory effect on human breast cancer cell proliferation. CONCLUSION LN/DTX has a good application prospect as an anti-breast cancer drug delivery system.