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目的:优选乌索酸固体脂质纳米粒的处方工艺并考察其理化性质及体外抗肿瘤活性。方法:采用薄膜分散法制备乌索酸固体脂质纳米粒,以包封率为指标,通过正交试验优选处方工艺;利用透射电镜、激光粒度测定仪等考察纳米粒的理化性质,通过MMT法检测其体外抗肿瘤活性。结果:最佳处方工艺为乌索酸90 mg,卵磷脂30 mg,硬脂酸10 mg,磷酸盐缓冲液浓度10 mmol·L-1;制备的乌索酸固体脂质纳米粒在透射电镜下呈球形或椭圆球形,平均粒径(184.7±18.3)nm,包封率(82.6±0.6)%,载药量(11.9±0.5)%,48 h体外累积释放率达81.21%,30 d内粒径与包封率均无明显变化。在5,10,20,40,80μmol·L-1时,乌索酸对人肝癌细胞株SMMC-7721的抑制率分别为(9.0±1.2)%,(15.7±2.8)%,(42.3±4.6)%,(78.7±6.9)%,(79.3±7.2)%;乌索酸固体脂质纳米粒的抑制率则分别为(9.0±1.3)%,(23.6±2.2)%,(59.3±6.1)%,(84.7±8.3)%,(85.0±8.1)%。结论:薄膜法分散法制备的乌索酸固体脂质纳米粒粒径适中、体外释放和稳定性良好,具有优良的抗肿瘤活性。
Objective: To optimize the formulation process of ursolic acid solid lipid nanoparticles and study their physico-chemical properties and antitumor activity in vitro. Methods: Ursolic acid solid lipid nanoparticles were prepared by thin-film dispersion method. The encapsulation efficiency was taken as an index to optimize the formulation by orthogonal test. The physical and chemical properties of the nanoparticles were investigated by transmission electron microscopy and laser particle sizer. Test its antitumor activity in vitro. Results: The best prescription was ursolic acid 90 mg, lecithin 30 mg, stearic acid 10 mg and phosphate buffer concentration 10 mmol·L-1. The prepared ursolic acid solid lipid nanoparticles were characterized by transmission electron microscopy The average particle size was (184.7 ± 18.3) nm, encapsulation efficiency was (82.6 ± 0.6)%, drug load was (11.9 ± 0.5)%. The cumulative release rate in vitro was 81.21% Path and encapsulation efficiency were no significant changes. The inhibitory rates of ursolic acid on human hepatocellular carcinoma cell line SMMC-7721 were (9.0 ± 1.2)%, (15.7 ± 2.8)%, (42.3 ± 4.6) at 5,10,20,40,80μmol·L- ), (78.7 ± 6.9)% and (79.3 ± 7.2)% respectively. The inhibitory rates of ursolic acid solid lipid nanoparticles were (9.0 ± 1.3)%, (23.6 ± 2.2)% and %, (84.7 ± 8.3)%, (85.0 ± 8.1)%. CONCLUSION: The ursolic acid solid lipid nanoparticles prepared by thin-film dispersion method have moderate particle size, good release in vitro and good stability, and have excellent anti-tumor activity.