大黄素-聚乳酸-羟基乙酸共聚物纳米粒的制备

目的 制备大黄素-聚乳酸-羟基乙酸( emodin-polylactic-co-glycolic acid,EMD-PLGA NPs)共聚物纳米粒,观察其电镜形态、稳定性,测定粒径、包封率、载药量.方法 采用乳化-溶剂挥发法( emulsion solvent evaporation method)按照正交设计制备EMD-PLGA NPs并优化处方,透射电镜下观察纳米粒的外观形态,激光粒度仪检测纳米粒的大小、分布及zeta电位,沉降法观察稳定性,用紫外分光光度计测定大黄素纳米粒的吸光度以计算包封率、载药量.结果 得到最佳优化处方工艺条件,在最佳条件下制得大黄素纳米粒呈圆球状或椭圆状;粒径约( 100±50 )nm;分散体系的颗粒由上而下呈逐渐变淡的弥散分布,无明显的沉积物;包封率为(24.5±1.9)％,载药量为(18.5±3.7)％.结论 采用乳化-溶剂挥发法制备大黄素-PLGA纳米粒,该方法材料简单,便于操作,优于以往的固体脂质纳米粒法;制备的大黄素纳米粒粒径小、分布均匀、载药率较高,药物吸光度及稳定性等均符合要求,为进一步制备组织靶向药物的研究奠定了基础.

Preparation of edomin-polylactic-co-glycolic acid nanoparticles

Objective To prepare edomin-polylactic-co-glycolic acid nanoparticles(EMD-PLGA NPs),and to observe its diameter,electronic speculum,stability,encapsulation efficiency and drugloading rate of the NPs.Methods EMD-PLGA NPs were made with emulsion solvent evaporand method and orthogonal design.Firstly the appearance was observed under trasmission electron microscope and we detected the diameter,distribution and zeta potential of the nanoparticles.The stability of laser particles was measured by sedimentation method,and the light absorption,the encapsulation efficiency,and drugloading were calculated.Results The best preparation condition was obtained.the end product of the drug under the best condition was globle or elliptic;the diameter of the particles was about(100±50) nm.The disperse system of nanoparticles in water scattered from the top to the bottom without sedimentation;the encapsulation efficiency was about(24.5±1.9)%;and the drugloading was about(18.5±3.7) %.Conclusion The method is superior to the previous solid lipid nanoparticle method,and the EMD-PLGA NPs have many advantages such as mini-size,better distribution and higher drugloading rate.Both the light absorbance and the stability meet the standard of demand.The method has laid a foundation for clinical target drugs.