党参总皂苷纳米乳体外透皮性能及抗黑素瘤细胞研究

Percutaneous Permeability of Codonopsis pilosula Total Saponins Nanoemulsion in vitro and Anti-melanoma Cells

[目的]研究党参总皂苷纳米乳处方组成,考察其体外透皮性能及抗黑素瘤细胞作用。[方法]根据药物溶解性和伪三元相图筛选党参总皂苷纳米乳处方,粒度分析仪测定其粒径;以大鼠皮肤为模型,透皮扩散仪研究党参总皂苷纳米乳体外透皮性能;以黑素瘤B16细胞为靶细胞,MTT法和形态观察法研究党参总皂苷纳米乳对黑素瘤细胞的毒性作用。[结果]党参总皂苷纳米乳处方确定为Cremophor EL40/PEG400/橄榄油/蒸馏水(质量比为28.66∶14.33∶8.25∶48.76),党参总皂苷含量为44.75 mg/m L,粒径为60.67 nm;党参总皂苷纳米乳12 h累积渗透量和稳态渗透速率分别是党参总皂苷水溶液的2.73、2.47倍;党参总皂苷纳米乳能促使黑素瘤细胞数量减少,出现空泡和细胞碎片,并且100～800μg/m L党参总皂苷纳米乳对黑素瘤细胞增殖的抑制率大于相同浓度党参总皂苷水溶液。[结论]确定了党参总皂苷纳米乳处方组成,它能增强党参总皂苷透皮性能和抗黑素瘤作用,从而为纳米乳开发党参总皂苷透皮制剂提供参考。

[Objective]To study the formulation of Codonopsis pilosula total saponins nanoemulsion,and investigate its percutaneous permeability and anti-melanoma cells effect in vitro.[Method]The formulation of C.pilosula total saponins nanoemulsion was screened according to drug solubility and pseudo three phase diagram,and its particle size was determined by particle size analyzer.Its percutaneous permeability was studied using transdermal diffusivity analyzer with rat skin as the model.Using melanoma B16cells as target cells,the toxicity of C.pilosula total saponins nanoemulsion on melanoma cells was studied by MTT method and morphology.[Result]The screened formulation of C.pilosula total saponins nanoemulsion was as follows:Cremophor EL40/PEG400/olive oil/distilled water(the mass ratio was28.66∶14.33∶8.25∶48.76),the content of C.pilosula total saponins was44.75mg/mL,and its particle size was60.67nm.The cumulative permeation amount and steady state penetration rate of C.pilosula total saponins nanoemulsion treated for12h were2.73times and2.47times as many as that of C.pilosula total saponins solution,respectively.The number of melanoma cells treated with C.pilosula total saponins nanoemulsion reduced,and cell vacuoles and fragments appeared in the cells.The inhibition rate of100~800μg/mL C.pilosula total saponins nanoemulsion on the proliferation of melanoma cells was greater than that of C.pilosula total saponins solution under the same concentration.[Conclusion]The composition of C.pilosula total saponins nanoemulsion has been ascertained.It can enhance the percutaneous permeability and anti-melanoma cells effect of C.pilosula total saponins,which provides a reference for the development of nanoemulsion in transdermal preparation of C.pilosula total saponins.