双敏感杂合脂质体体外释放度的研究

Study on in Vitro Release of Hybrid Liposomes with Dual Sensitivity

目的:制备载索拉非尼的核壳结构杂合脂质体(HA-Sf-CL),考察其理化性质和pH/酶敏感性。方法:采用薄膜分散法制备装载Sf的阳离子脂质体内核(Sf-CL),再将阴离子材料外壳透明质酸(HA)静电吸附到内核上,得到杂合脂质体HA-Sf-CL,对其包封率、载药量、粒径、多分散系数、Zeta电位、形态及体外释药特性进行考察。结果:内核包封率86.61%±0.73%,平均载药量为4.98%±0.049%,平均粒径221.7±10.1 nm,PDI为0.182±0.032,Zeta电位为43.8±2.9 mV;最优处方HA-Sf-CL平均粒径236.1±5.8 nm,PDI为0.151±0.020,Zeta电位为-40.9±0.7 mV,外观圆整。HA-Sf-CL再当前条件下稳定性良好,体外释放呈现pH和酶双敏感的特征。结论:成功制备了pH/酶双敏感杂合脂质体,为进一步研究和体内抗肿瘤能力提供基础。

Objective:To prepare sorafenib loaded core-shell hybrid nanoparticles(HA-Sf-CL)and investigate the physicochemical properties and pH/enzyme sensitivity.Method:The Sf-loaded cationic liposomal core(Sf-CL)was prepared by thin film dispersion method,and then hyaluronic acid(HA)was electrostatic adsorbed onto the core to obtain hybrid liposome(HA-Sf-CL).The encapsulation efficiency,drug loading capacity,particle size,multi-dispersion coefficient,zeta potential,morphology and drug release characteristics of HA-Sf-CL was investigated.Result:The encapsulation efficiency of the core was 86.61%±0.73%,the drug loading efficiency was 4.98%±0.049%,the mean particle size was 221.7±10.1 nm,PDI was 0.182±0.032,and zeta potential was 43.8±2.9 mV.The average particle size of HA-Sf-CL of the optimal prescription was 236.1±5.8 nm,PDI was 0.151±0.020,Zeta potential was-40.9±0.7 mV,and the appearance was round.HA-Sf-CL had good stability under the current conditions and showed pH/enzyme double sensitivity in vitro release.Conclusion:pH/enzyme double sensitive hybrid liposomes were successfully prepared,which would provide the basis for further study and in vivo anti-tumor ability.