负载表阿霉素乙酰普鲁兰纳米粒的制备及细胞摄取

Preparation of epirubicin-loaded pullulan acetate nanoparticles and uptake by KB cells

①目的探讨疏水性乙酰普鲁兰作为纳米药物载体负载表阿霉素的可行性。②方法采用溶剂扩散法制备负载表阿霉素的PA纳米粒,并对其形态、粒径、包封率、载药量、体外释药特征和细胞摄取进行研究。③结果载药PA纳米粒为球形,载药量随乙酰基取代度的增大而增加,药物体外累积释放量随乙酰基取代度增高及释放介质pH降低而加快;与KB细胞(口腔上皮癌细胞株)温育2h,纳米粒中药物主要位于细胞浆,而游离药物主要位于胞核。④结论溶剂扩散法制备负载表阿霉素的PA纳米粒包封率和载药量高,体外释药具有缓释制剂特征,并可被肿瘤内吞入细胞。

Objective To investigate the feasibility of pullulan acetate （PA） was prepared epirubicin - loaded PA nanoparticles. Methods The solvent diffusion method was used to prepare EPI - loaded PA nanoparticles. The nanoparticles were characterized in terms of morphology, particle size, drug loading, drug release profile and intracellular uptake. Results The drug - loaded PA nanoparticles were spherical. The drug entrapment and drug content increased as the degree of acetyl substitution increasing. The size of EPI - loaded PA nanoparticles increased with the increasing of EPI - loading content. The EPI release rate was controlled by the degree of substitution and pH of release medium. After 2h incubation, nanoparticle loading EPI mainly localized in the cytoplasm, whereas free EPI accumulated in nuclear. Conclusion The EPI - loaded PA nanoparticles have high entrapment efficiency and drug loading, and can retard drug release in vitro. The nanoparticles can be internalized by KB tumor cells.