马兰;贾莉;孙俊平;
MA Lan;JIA Li;SUN Junping;Department of Pharmacy and Inspection,Heze Medical College;Outpatient Department of Heze University;

• 1:菏泽医学专科学校药学与检验系
• 2:菏泽学院门诊部

摘要(Abstract)：

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.

关键词(KeyWords)： 多西他赛;脂质纳米粒;抗乳腺癌
docetaxel;lipid nanoparticle ring;breast cancer

Abstract:

Keywords:

基金项目(Foundation): 山东省医药卫生科技发展计划项目(2018WS499)

作者(Authors): 马兰;贾莉;孙俊平;
MA Lan;JIA Li;SUN Junping;Department of Pharmacy and Inspection,Heze Medical College;Outpatient Department of Heze University;

参考文献(References)：

• [1] 曹莉，廖宁.2018年乳腺癌临床研究进展[J].循证医学，2019,19(1):10-13.
• [2] 郭童林，王翠，沈丽霞.固体脂质纳米粒的研究进展[J].神经药理学报，2017,7(6):15-21.
• [3] 白洁，英子伟，赵林，等.miR-21-5p对乳腺癌多西他赛耐药细胞株存活的影响及其机制研究[J].实用药物与临床，2019,22(5):476-480.
• [4] 陈莹，李岩，蔡爽.冬凌草甲素长循环固体脂质纳米粒的制备及对人胃癌SGC-7901细胞的抑制作用[J].中国医药导报，2013,10(17):13-15.
• [5] 何瑶，郭晓华.依托泊苷固体脂质纳米粒的制备与抗癌活性研究[J].中国药师，2018,21(5):792-796.
• [6] 简宇凡，卜伟，李韦韦，等.复乳法制备盐酸多柔比星固体脂质纳米粒及其体外稳定性研究[J].中国药师，2018,21(12):2096-2100.
• [7] 李亚男，田琳，徐月红.多西他赛他莫昔芬脂质体体外释放研究[J].今日药学，2020,30(4):249-251.
• [8] 于莲，杜妍，田丽华，等.叶酸修饰水飞蓟宾固体脂质纳米粒的制备及其对A549细胞抑制作用研究[J].中草药，2013,44(2):158-164.
• [9] 李慧，张志岳，孙萍.固体脂质纳米粒用于细胞毒性药物传递系统综述的研究进展[J].中国药房，2013,24(9):848-851.
• [10] 宋春晓，何书莲，曹春凤，等.固体脂质纳米粒和纳米结构脂质载体在药物传递中的研究进展[J].药学研究，2016,35(4):234-236.