抗肿瘤活性化合物胡桃醌脂质体的构建与评价OA

Objective To prepare juglone liposomes to enhance the stability and water solubility of juglone.Methods Juglone liposomes were prepared using the thin-film dispersion method.A relatively optimal formulation was preliminarily screened through single-factor experiments,followed by an orthogonal test design.With the entrapment efficiency(EE)as the evaluation index,the effects of membrane material ratio(soybean phospholipid:cholesterol),lipid-to-drug ratio(membrane materials:juglone),organic solvent volume,and ultrasonic temperature on the entrapment efficiency were investigated to determine the optimal preparation process for juglone liposomes.A high-performance liquid chromatography(HPLC)method was established for the determination of juglone content,and its entrapment efficiency and drug loading(DL)were calculated.Quality evaluation was performed on the optimized juglone liposomes.Results The optimal formulation of juglone liposomes was lipid to cholesterol ratio of 5∶1,lipid material to juglone ratio of 10∶1,40 mL organic solvent volume,and ultrasound temperature of 4℃.The prepared juglone liposomes were brownish-yellow liquid with good fluidity,an average particle size of 327.6 nm,a polydispersity index(PDI)of 0.016,and an average Zeta potential of-48.4 mV.The average encapsulation efficiency of juglone was 96.91%,with an RSD of 0.05%,and the average drug loading was 6.317%,with an RSD of 0.02%.The leakage rate of juglone liposomes after being placed at 4℃for 30 days was 4.72%.Conclusion This study established a stable preparation process for juglone liposomes,enhancing both the stability and solubility of juglone.