多柔比星聚合物胶束制备、表征及其体外释药研究

Preparation, characterization and drug release property of doxorubicin-loaded polymeric micelles

目的制备多柔比星的soluplus聚合物胶束,并对其进行体外评价。方法采用薄膜分散法-p H诱导法相结合制备多柔比星聚合物胶束;采用粒径测定仪、透射电镜、X-射线衍射(XRD)、差示扫描量热法(DSC)及红外光谱(FTIR)对其进行表征;采用HPLC法测定胶束的包封率和载药量;采用动态膜透析法考察载药胶束的体外释药特性。结果本研究制备的胶束呈球形或类球形,平均粒径为(67.57±2.9)nm,平均包封率为(77.81±4.03)%,平均载药量(10.15±1.56)%;XRD和DSC结果表明多柔比星以无定型状态或分子状态包载在聚合物胶束中;FTIR结果表明多柔比星分子中羟基和聚合物的羰基之间形成了氢键;体外释放结果表明多柔比星的soluplus聚合物胶束具有缓释作用。结论该胶束制备工艺简单,其粒径、包封率、载药量可控,具有缓释作用。

Objective To prepare doxorubicin-loaded soluplus polymeric micelles （ADM-PMs） and evaluate their quality. Methods The ADM-PMs were prepared by film dispersion method using an amphiphilic copolymer soluplus. The ADM-PMs were characterized by dynamic light scattering, transmission electron microscopy （TEM）, X-ray diffraction （XRD）, differential scanning calorimetry （DSC）, and fourier transform-infrared spectra （FTIR）. The release curve was determined by dialysis. Entrapment efficiency and drug loading were determined by HPLC. Results The ADM-PMs observed by TEM were spherical with a mean particle size of （67.57±2.9）nm, the encapsulation efficiency and drug loading of ADM-PMs were （77.81±4.03）% and （10.15±1.56）%. XRD and DSC determined that doxorubicin was in an amorphous or molecular form within the PMs. FTIR indicate that hydrogen bonds were formed between doxorubicin and polymer. Conclusion The ADM-PMs prepared had exhibited sustained release in vitro, and the particle size, encapsulation efficiency, and drug loading are controllable.