甲氨蝶呤磷脂复合物纳米粒的制备及表征

Preparation and Characterization of MTX-PC Complex-Nanoparticles

研究甲氨蝶呤磷脂复合物纳米粒的制备方法并进行表征。以卵磷脂(PC)为材料,甲氨蝶呤(MTX)为模型药物,采用共溶剂法制备MTX-PC复合物,用薄膜分散法将MTX-PC复合物自组装成纳米粒,并对其进行质量评价与体外释药试验。MTX-PC复合物纳米粒为类似脂质体的球形结构,粒径均匀,分散性好,平均粒径为(152. 5±3. 2) nm、多分散系数为0. 162±0. 015、电位为-(20. 3±2. 1) m V、载药量为(20. 7±2. 4)%;且MTX以非晶型状态均匀分布在纳米粒中。其在3种p H值条件下的体外释放随着p H值的下降而上升,在模拟肿瘤弱酸性环境的p H 5. 0下,48 h药物累积释放量高达90%。MTX-PC复合物纳米粒具有缓释的特点,且在肿瘤环境中利于药物的释放,有肿瘤治疗的潜力。

To prepare MTX-PC complex-nanoparticles and charactorize it. In this study,the MTX-PC complex was prepared by co-solvent method with PC and MTX,followed by self-assembly to form MTX-PC complex-nanoparticles by film dispersion method. Its quality was evaluated and in vitro drug release experiments were carried out. It was proposed that MTX-PC complex-nanoparticles exhibited a liposome-like globular shape,fairly uniform size and well dispersed. The average particle diameter was( 152.5 ± 3.2) nm,polydispersity was 0. 162 ± 0. 015,Zeta potential was-( 20.3 ± 2.1) m V and drug-loading was( 20.7 ± 2.4) %. MTX uniformly distributed in the nanoparticles with an amorphous state. Their release behavior in vitro showed sustained releasing. The lower the PH value,the faster the release of MTX from the nanparticles,and in simulated weak acidic tumor environment with p H 5. 0,48 h drug cumulative release was up to 90%. The prepared MTX-PC complex-nanoparticles with sustained release and good release in the tumor environment,showed a promising potential for treatment of tumor.