摘要
目的制备人参皂苷Rg3温敏纳米粒,对其体外释药特性和对肝癌细胞的抑制作用进行研究。方法两亲性温敏聚合物作为药物载体,滴制法制备载药温敏纳米粒。采用正交试验设计,以包封率为主要评价指标,温敏聚合物浓度、人参皂苷Rg3浓度和搅拌时间为考察因素,筛选纳米粒处方和工艺。体外释放曲线法研究37℃和42℃时温敏纳米粒的体外释放特征。MTT法(四氮唑盐微量酶反应比色法)考察温敏纳米粒对HepG2肝癌细胞增生的抑制作用。结果优选处方及制备工艺为温敏聚合物,浓度为0.20 mg/m L,人参皂苷Rg3浓度为0.03 mg/m L,搅拌时间为2 h;温敏纳米粒呈类球形,包封率为78.43%±1.76%,平均粒径为(147.0±2.3)nm,平均Zeta电位为-14.6 m V(n=3)。体外释放结果表明,37℃时,3 h药物累积释放度为36.1%,24 h累积释放度为44.6%;42℃时,3 h累积释放度达54.1%,24 h累积释放率为83.0%。体外抑制结果显示,随着温敏纳米粒浓度从20μg/m L增加至180μg/m L,HepG2肝癌细胞成活率由69.8%下降至37.7%。结论人参皂苷Rg3温敏纳米粒处方和工艺合理可行,能达到随温度变化对药物释放起调释作用,对HepG2肝癌细胞具有较好的体外抑制作用。
Objective To prepare ginsenoside Rg3 thermo-sensitive nanoparticles and to investigate the drug release behavior and the inhibiting effect on the hepatoma cells in vitro. Methods Thermo-sensitive nanoparticles were prepared using the solvent injective method with amphiphilic block copolymer. The encapsulation efficiency was used to evaluate the influence of different formulation and preparation factors; the formulation was optimized by orthogonal design,with mixing time,mass concentration of amphiphilic block copolymer and ginsenoside Rg3 as factors. The drug release properties were measured at 37 ℃ and 42 ℃ in vitro. MTT assay was used to determine the inhibiting effect of ginsenosides Rg3 thermo-sensitive nanoparticles on HepG2 cells. Results The mass concentration of amphiphilic block copolymer was 0. 20 mg/m L,the mass concentration of ginsenosides Rg3 was 0. 03 mg/m L and the mixing time was 2 h in the optimized formula and preparation process; the optimized nanoparticles had a spherical shape,the average diameter was（ 147. 0 ± 2. 3） nm（ n = 3）,the average Zeta potential was-14. 6 m V（ n = 3） and the encapsulation efficiency was 78. 43% ± 1. 76%（ n = 3）. The index of release showed that the accumulative release rates of the thermo-sensitive nanoparticles at the temperature of 37 ℃ and 42 ℃ were 36. 1% and 54. 1% within 3 h,and 44. 6% and 83. 0% within24 h,respectively. The test of inhibition showed the survival rate of HepG2 cells was decreased from 69. 8% to 37. 7%with the increase of the concentration of thermo-sensitive nanoparticles from 20 μg/m L to 180 μg/m L. Conclusion The results showthat both formulation and preparation of ginsenoside Rg3 thermo-sensitive nanoparticles are feasible and reasonable. The thermo-sensitive nanoparticles can well respond to the environmental temperature change and has a good inhibitory effect on HepG2 cells in vitro.
出处
《实用药物与临床》
CAS
2017年第11期1231-1235,共5页
Practical Pharmacy and Clinical Remedies
关键词
人参皂苷RG3
温敏纳米粒
正交设计
体外释放
Ginsenoside Rg3
Thermo-sensitive nanoparticles
Orghogonal experimental design
In vitro dissolution
