环孢菌素A-纳米乳输液剂的制备及鉴定

Development and characterization of cyclosporine A nanoparticles emulsion

目的制备鉴定负载环孢菌素A(Cyclosporine A,CsA)的纳米乳(Cyclosporine A-nanopaticals e-mulsion,CsA-NP)并评估CsA-NP对体外干细胞增殖和分化的影响。方法采用乳化法制备油水(o/w)型CsA-NP。以蛋黄磷脂(Lipoid E 80)、泊洛沙姆188为水相,中链油(Lipoid MCT)为油相,采用高压均质法制备而成。高效液相色谱法(HPLC)评估产品的载药率,乳径的粒径经激光粒度分析仪测定。CsA-NP对干细胞增殖和分化影响采用细胞直接计数和MTT检测。结果本研究制备的CsA-NP工艺稳定性好,粒径均匀,50%的乳滴微粒直径在162 nm以内。CsA-NP浓度在(0.01～1 mg/mL)之间1～3 d对细胞增殖有明显促进作用(P<0.01);其中又以0.5 mg/mL的CsA-NP浓度组为最佳。结论CsA-NP是一种稳定性良好的静脉注射用纳米乳。

Objective To make and evaluate the ability of cyclosporine incorporated into nanoparticles emulsion（CsA-NP）,as well as the effects of CsA-NP on stem cells proliferation in vitro.Methods An oil-in-water（o/w）emulsification-diffusion method was used to prepare cyclosporin A-loaded nanoparticles（CsA-NP）intravenous emulsion.CsA-NP emulsion was prepared by the high pressure homogenization method,using Lipoid E 80 and poloxamer 188 as emulsifiers,Lipoid MCT as the oil phase.The products were evaluated by measuring drug loading with high performance liquid chromatography（HPLC）,particle sizing by dynamic light scattering（DLS）.The proliferation and differentiation of CsA-NP on stem cells were measured by direct cell counting and MTT assay,respectively.Results The prepared with the optimized formulation was stable with uniform particle size distribution and the dimension of 50% emulsion droplets was less than 162 nm.The proliferation of stem cells were stimulated by 0.01~1 mg/mL CsA-NP for 1~3 d（P0.01）;and the best proliferative effect was observed at concentration of 0.5 mg/mL.Conclusion Intravenous CsA-NP emulsion is stable as a new type of drug delivery system.