人参皂苷Rg3负载PCL-PEG纳米系统在卵巢癌中的优化研究

Improvements on Ginsenoside Rg3 Nanopreparations Delivery Systems in Ovarian Cancer

摘要: 目的：为了提高人参皂苷Rg3的有效性和靶向性，研究人参皂苷Rg3脂质体、纳米粒及微乳的制备及其在小鼠体内组织分布的差异，比较各类纳米制剂的靶向特异性。方法：采用薄膜超声分散法、纳米沉淀法、微乳法分别制备人参皂苷Rg3脂质体及人参皂苷Rg3PLGA纳米粒，人参皂苷Rg3微乳粒，通过比较三种方案效果，制定优化方案。结果：1) 磷脂、胆固醇、人参皂苷Rg3制备的脂质体平均粒径为111.8 nm，Zeta电位为−38.67 mV，。2) PLGA浓度为10 mg∙mL⁻¹，人参皂苷Rg3浓度为3 mg∙mL⁻¹，有机相与水相体积比为1:3。制备的纳米粒平均粒径为186.1 nm，Zeta电位为−29.56 mV。3) 油酸乙酯、EL35、PEG400与水的最佳质量比为8.25:12:4.75:75，平均粒径为60.50 nm，Zeta电位为−15.63 mV。结论：三种人参皂苷Rg3纳米制剂的工艺方法均简便、稳定可行。微乳法分别制备人参皂苷Rg3脂质体分层结构最明显。

Abstract: Objective: To improve the effectiveness and targeting of ginsenoside Rg3, to study the preparation and distribution of ginsenoside Rg3 liposomes, nanoparticles and microemulsion in mice, and to compare the targeting specificity of various nano preparations. Methods: Ginsenoside Rg3 lipo-somes, ginsenoside Rg3 PLGA nanoparticles and ginsenoside Rg3 microemulsion granules were prepared by ultrasonic film dispersion method, nano precipitation method and microemulsion method respectively. The optimization scheme was developed by comparing the effect of the three schemes. Results: 1) Using chloroform-ethanol (1:1) as solvent, the mass ratio of phospholipid, cho-lesterol and ginsenoside Rg3 was 4:2:1, the average particle size of the liposome was 111.8 nm, the Zeta potential was −38.67 mV, and the encapsulation rate was 87.85%. 2) PLGA conase tcentration was 10 mg∙mL⁻¹, human ginseng saponin Rg3 concentration was 3 mg∙mL−1, organic pho water phase volume ratio was 1:3. The average particle size of the prepared nanoparticles was 186.1 nm, the Zeta potential was −29.56 mV, and the encapsulation rate was 87.29%. 3) The optimum mass ratio of ethyl oleate, EL35, PEG400 to water was 8.25:12:4.75:75, the average particle size was 60.50 nm, and the Zeta potential was −15.63 mV. There was no stratification after centrifugation at 4000 r∙min⁻¹ for 10 min. Conclusion: The three kinds of ginsenoside Rg3 nanopreparations are sim-ple, stable and feasible. The stratification structure of ginsenoside Rg3 liposomes prepared by mi-croemulsion method is the most obvious.