负载戊唑醇的聚乙二醇-聚己内酯胶束的制备与性能研究

Preparation and performances of poly(ethyleneglycol)-polycaprolactone micelles loaded with tebuconazole

通过开环聚合法合成了聚乙二醇-聚己内酯嵌段共聚物(PEG-b-PCL),以PEG-b-PCL为囊壁、以戊唑醇为囊芯,采用自组装的方法制备了载药胶束。分别利用动态光散射仪(DLS)和透射电镜(TEM)对其粒径进行了表征,通过紫外分光光度计和高效液相色谱仪测定了其载药量、包覆率和体外释药性能,用滤纸片法测试了载药胶束对木霉Trichoderma viride的抑菌性能。结果表明:PEG-b-PCL载戊唑醇胶束平均粒径为250 nm,均匀度良好,载药量为26.4%,包覆率为18.0%,体外释放192 h的释药率为83.35%,其对木霉的抑菌效果明显高于同浓度下的戊唑醇乙酸乙酯溶液。

The poly（ethylene glycol）-polycaprolactone（PEG-b-PCL） block copolymer was synthesized by ring-opening polymerization method,and the self-assembled PEG-b-PCL micelles was applied as carrier to load tebuconazole by self-assembly method.The diameter of the tebuconazole loaded micelles was characterised by dynamic light scattering（DLS） and transmission electron microscope（TEM）.The drug loading efficiency,encapsulation rate and release characteristics in vitro were measured by ultraviolet specrophotometer and high performance liquid chromatography（HPLC）.The mould inhibition properties of tebuconazole-loaded micelles to Trichoderma viride was evaluated by filter paper method.Results showed that tebuconazole loaded PEG-b-PCL micelles were spherical and uniform,with a mean particle diameter of 250 nm.The drug loading efficiency and encapsulation rate were 26.4% and 18% respectively.Tebuconazole-loaded PEG-b-PCL micelles showed good slow-release characteristics.After 192 h,the drug release percentage of tebuconazole-loaded PEG-b-PCL micelles was 83.35%.Tebuconazole-loaded PEG-b-PCL micelles also exhibited more efficient mould inhibitions to T.viride than that of tebuconazole-ethyl acetate solution.