| 李娇娇，王茹静，马菁，雷以珵，石三军▲.藤黄酸脂质体的制备及抗肿瘤活性研究[J].中国医药科学,2023,(19):74-77 基金项目: |
| 藤黄酸脂质体的制备及抗肿瘤活性研究 |
| Study on the preparation and anti-tumor activity of liposomes of gambogic acid |
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| DOI： |
| 中文关键词: 藤黄酸；脂质体；薄膜分散法；抗肿瘤活性 |
| 英文关键词:Gambogic acid; Liposomes; Thin-film dispersion method; Anti-tumor activity |
| 作者 | 单位 | | 李娇娇，王茹静，马菁，雷以珵，石三军▲ | 成都中医药大学药学院，四川成都 611137 |
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| 中文摘要: |
| [摘要] 目的 制备藤黄酸脂质体（GA Lip），优化其处方并进行表征，考察GA Lip对4T1乳腺癌的抗肿瘤活性。 方法 采用薄膜分散法制备GA Lip，通过高效液相色谱（HPLC）法对藤黄酸（GA）含量测定进行方法学考察；以粒径和多分散系数为主要指标优化GA Lip的药脂比和投药量；测定GA Lip包封率；采用透射扫描电镜（TEM）观察其形貌；采用四甲基偶氮唑盐比色（MTT）法检测GA及GA Lip对4T1细胞的增殖抑制活性；建立4T1荷瘤小鼠模型，对比游离GA与GA Lip的体内抗肿瘤效果。 结果 优化后的GA Lip药脂比为1∶5，投药量为8 mg，包封率为（89.15±0.12）%，呈大小均一的椭圆形；GA及GA Lip对4T1细胞48 h的IC50分别为0.635 μmol/L和0.294 μmol/L；与游离GA组比较，GA Lip组小鼠肿瘤体积及重量更小。 结论 优化后的GA Lip稳定性较好，包封率高，与游离GA相比，GA Lip抗肿瘤活性更好，药效作用有所增强。 |
| 英文摘要: |
| [Abstract] Objective To prepare liposomes of gambogic acid (GA Lip), optimize its prescription and characterize it to investigate the anti-tumor activity of GA Lip against 4T1 breast cancer. Methods The GA Lip was prepared by the thin-film dispersion method. The methodological investigation was carried out by high-performance liquid chromatography (HPLC) for the determination of garcinolic acid (GA) content. The particle size and dispersion coefficient were used as the main indicators to optimize the drug-to-lipid ratio and dosage of GA Lip. The encapsulation rate of GA Lip was determined and the morphology was observed using a transmission electron microscope (TEM). The proliferation-inhibitory activity of GA and GA Lip on 4T1 cells was measured using the 3-(4,5)-dimethylthiahiazo (-z-y1)-3,5-di-phenytetrazoliumromide (MTT) method. A 4T1 tumor-bearing mouse model was established to compare the in-vivo anti-tumor effects of free GA with those of GA Lip. Results The optimized GA Lip had a lipid ratio of 1 : 5, a dosage of 8 mg and an encapsulation rate of (89.15±0.12)% in a uniformly sized oval shape. The IC50 of GA and GA Lip on 4T1 cells at 48 hours were 0.635 μmol/L and 0.294 μmol/L, respectively. Compared to the free GA group, the GA Lip group mice had smaller tumor volumes and weights. Conclusion The optimized GA Lip is more stable and has a high encapsulation rate. Compared to free GA, GA Lip has better anti-tumor activity and enhanced pharmacodynamic effects. |
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