响应面法优化大黄和厚朴脂质体制备工艺及其结肠靶向性研究OA

Objective To optimize the formulation process of honokiol/rhein dual-loaded oral liposomes modified with chitosan(CS)and sodium alginate(SA)for colon targeting(HNK/RH-CS-SA Lip)and investigate their colon-targeting properties.Methods HNK/RH-CS-SA Lip were prepared using the thin-film dispersion method.With the phospholipid-to-cholesterol ratio,drug-to-lipid ratio,and ultrasonic power as evaluation indices,single-factor experiments and Box-Behnken response surface methodology were employed to screen the optimal preparation conditions.The morphological characteristics,particle size,and in vitro release behavior in different media of HNK/RH-CS-SA Lip were evaluated.The colon-targeting property in vivo was assessed through tissue distribution experiments in mice.Results The optimal preparation conditions for HNK/RH-CS-SA Lip were as follows:phospholipid-to-cholesterol mass ratio of 4.44:1,drug-to-phospholipid mass ratio of 1:9.77,ultrasonic power of 600 W,hydration medium of PBS,and hydration volume of 6 mL.Under the optimized conditions,the average encapsulation efficiency of HNK/RH-CS-SA Lip was 92.98%±0.74%,and the aver-age particle size was(340.78±2.01)nm.The liposomes exhibited sustained-release behavior and colon-targeted release characteris-tics.Conclusion The prepared HNK/RH-CS-SA Lip demonstrate good stability,uniform particle size distribution,high encapsulation efficiency,and colon-targeting properties.