共载阿霉素-碳点@磷酸钙脂质纳米粒的制备与评价

Preparation and evaluation of Doxorubicin and carbon dots loaded lipid coated calcium phosphate nanoparticles

目的制备共载阿霉素-碳点@磷酸钙脂质纳米粒(Doxorubicin-carbon dots@lipid coated calcium,DOX-CDs@LCP NPs),并对其载药性能及体外释药行为进行评价。方法采用反相微乳法制备DOX-CDs@LCP NPs,考察钙/磷比值,内水相pH值及搅拌速度对纳米粒外观的影响;并对阿霉素和碳点浓度对制剂载药量的影响进行考察。通过激光散射粒径测定仪测定粒径和电位,采用透射电镜表征纳米粒形态。同时以不含碳点的纳米粒(DOX@LCP NPs)作为对照。比较两种制剂在体外释药行为上的差异。结果DOX-CDs@LCP NPs带有磷酸钙内核,外层有磷脂包裹,平均粒径为133.9 nm,zeta电位为-20 mV,包封率和载药量质量分数分别为(64.38±2.4)%、(12.22±0.53)%;在生理条件下,DOX-CDs@LCP能够延缓药物释放达29.9%;在酸性环境下,药物释放加速,累积释放量可达78%。结论DOX-CDs@LCP NPs具有较高的载药量和体外释药性能。

Objective To fabricate Doxorubicin-carbon dots@lipid coated calcium phosphate(DOX-CDs@LCP)nanoparticles and evaluate its drug loading capacity and in vitro drug release behavior.Methods Reverse microemulison method was used to prepare DOX-CDs@LCP nanoparticles.Single factor test was performed to optimize the formulation with the entrapment efficiency,drug loading capacity,particle size and size distribution as the indexes.The morphology,diameter and Zeta-potential of the nanoparticles were characterized by dynamic light scattering and transmission electron microscopy,respectively.The in vitro drug release behavior of DOX-CDs@LCP NPs was also performed.Results The encapsulation efficiency and loading capacity of DOX-CDs@LCP nanoparticles according to the optimal conditions were(64.38±2.4)%and(12.22±0.53)%,respectively.The nanoparticles was globular-like in shape and the size was 138 nm with a narrow distribution.The Zeta potential of the nanoparticles was-20 mV.In virto release results illustrated that drug-loading nanoparticles had a pH sensitivity,that is,more fast release rate at a lower pH value.Conclusion DOX-CDs@LCP NPs have a high drug loading capacity and in vitro drug release profiles.