透明质酸修饰阿霉素脂质体的制备及抑制肿瘤细胞生长活性

制备了一种透明质酸修饰的脂质体作为疏水性抗肿瘤药物阿霉素（Doxorubicin，DOX）的载体，以增强其受体介导的细胞内吞，提高其抗肿瘤效果。以透明质酸为原料，通过酰胺键和十八烷胺制备透明质酸-十八烷基（Hyaluronic acid-Octodecane，HOA）聚合物，以DOX为模型药物，脂质体为药物载体，通过薄膜分散法和后插入法，制备得到HOA修饰的DOX靶向脂质体（DOX/LP/HOA），测定其平均粒径为（50.17±0.60） nm，电位为（-7.61±0.43） mV，包封率为（98.85±0.40）%。体外释放和细胞毒性结果表明，所得到DOX/LP/HOA脂质体可控制药物缓慢释放，抑制肿瘤细胞生长，活性良好，具有潜在应用价值。
Doxorubicin（DOX）-loaded hyaluronic acid（HA） modified Liposomes（DOX/LP/ HOA） were prepared to enhance receptor mediated endocytosis and improve anti-tumor effect. Octadecyl was chosen to conjugate HA backbone by amide bond to prepare hyaluronic acid-octodecane（HOA） polymers. DOX，as a model drug，was encapsulated into HOA modified liposomes by the film dispersion method and post-insertion method. The average particle size，zeta potential and encapsulation of DOX/LP/HOA were（50.17±0.60） nm，（-7.61±0.43） mV and（98.85±0.40）%，respectively. In vitro release and cytotoxicity results showed that DOX/LP/HOA could release DOX slowly and improve tumor targeting ability. DOX/LP/HOA with excellent anti-tumor activity can be used as the potential carrier for delivery of anti-tumor drugs