左旋多巴和姜黄素共递送protocells纳米粒的制备及体外评价  

Preparation and in vitro evaluation of levodopa and curcumin co-loaded protocells nanoparticles

作　　者：刘畅[1] 周文凯[1] 李桂玲[1] LIU Chang;ZHOU Wen-kai;LI Gui-ling(Formulation Laboratory,Institute of Medicinal Biotechnology,Chinese Academy of Medical Sciences&Peking Union Medical College,100050 Beijing,China)

机构地区：[1]中国医学科学院北京协和医学院医药生物技术研究所制剂室

出　　处：《中国医药生物技术》2020年第1期5-12,共8页Chinese Medicinal Biotechnology

基　　金：国家自然科学基金（81603062）

摘　　要：目的制备共载左旋多巴和姜黄素protocells纳米粒并进行体外评价。方法以介孔二氧化硅为内核,脂质双分子层为外膜,制备共载左旋多巴和姜黄素protocells纳米粒。使用激光粒度分析仪和透射电子显微镜对所制备纳米粒的形貌、粒径、多分散系数(PDI)和Zeta电势进行表征;采用高效液相色谱法对所制备纳米粒的载药量和包封率进行测定;采用透析袋法对所制备纳米粒的体外释放特性进行考察;应用粒径、Zeta电势、载药量等指标对所制备纳米粒的室温贮存稳定性进行评价。结果制备的载左旋多巴和姜黄素protocells纳米粒粒径分布均一性好、粒子表面呈电负性、平均粒径为(210.9±2.8)nm、PDI为(0.201±0.011)。其中左旋多巴的载药量为(20.28±0.43)%、包封率为(10.14±0.22)%;姜黄素的载药量为(1.97±0.01)%、包封率为(98.32±0.01)%。体外释放结果表明该纳米粒48 h姜黄素累计释放率为59.2%,且可有效阻止左旋多巴的泄漏,降低其在循环系统中的暴露量。稳定性结果表明左旋多巴和姜黄素在protocells纳米粒中稳定性良好。结论载左旋多巴和姜黄素的protocells纳米粒制备工艺简单,具有良好的理化性质、稳定性及所预期的释放性能。Objective We aim to prepare and evaluate the levodopa and curcumin co-loaded protocells nanoparticles in vitro.Methods Levodopa and curcumin co-loaded protocells nanoparticles were prepared with mesoporous silica nanoparticles(MSNs)as core and lipid bilayer as outer membrane.The morphology,particle size,polydispersion index(PDI)and Zeta potential of the nanoparticles were characterized by laser particle size analyzer and transmission electron microscope(TEM).The drug loading capacity(DLC)and entrapment efficiency(EE)of the nanoparticles were determined by HPLC.The in vitro release characteristics of the nanoparticles were investigated by dialysis bag method.The storage stability of the nanoparticles at room temperature was evaluated by particle size,Zeta potential and so on.Results The particle size distribution of levodopa and curcumin co-loaded protocells nanoparticles was uniform with the average particle size of(210.9±2.8)nm and PDI of(0.201±0.011),and the surface of the particles was electronegative.The DLC and EE of levodopa were(20.28±0.43)%and(10.14±0.22)%,respectively.The DLC and EE of curcumin were(1.97±0.01)%and(98.32±0.01)%,respectively.The results of in vitro release showed that the cumulative release rate of curcumin was 59.2%in 48 h,and the exposure amount of levodopa was significantly reduced in the circulatory system.The results of stability showed that levodopa and curcumin were stable in the nanoparticles.Conclusion The preparation process of levodopa and curcumin co-loaded protocells nanoparticles is simple,which have good physicochemical properties,stability and expected release properties.

关 键 词：左旋多巴 姜黄素 PROTOCELLS 纳米粒 体外评价 

分 类 号：TQ460.4[化学工程—制药化工] TB383.1[一般工业技术—材料科学与工程]