OBJECTIVE: To optimize the formulation and technology of Lappaconitine liposome, to prepare Lappaconitine liposome gel and investigate the characteristics of its drug release in vitro. METHODS: Thin film dispersion method was used to prepare Lappaconitine liposome. L9(34) orthogonal test was designed to optimize the formulation technology of Lappaconitine liposome using encapsulation rate as evaluation index, the mass ratio of lecithin to cholesterol, the mass ratio of drug to lipid and hydration temperature as factors. Validation test was also conducted. Lappaconitine liposome was prepared by optimal technology. The morphology, particle size distribution and Zeta potential were observed. Using 1.0% carbomer 940 as gel matrix, Lappaconitine liposome gel was prepared and dialysis bag release test was used to investigate the characteristics of its drug release in vitro, and compared with Lappaconitine gel. RESULTS: The optimal formulation technology of Lappaconitine liposome was that mass ratio of lecithin to cholesterol was 8 ∶ 1; mass ratio of drug to lipid was 1 ∶ 10; hydration temperature was 55 ℃. The optimal formulation of lappaconitine liposome with a spherical appearance and complete structure, the average particle size was (379.6±0.71) nm (RSD=0.18%, n=3); PDI was (0.171±0.003) (RSD=1.58%,n=3); Zeta potential was (-23.1±0.02) mV (RSD=0.85%,n=3); encapsulation rate was (63.84±0.36)% (RSD=0.57%,n=3). Prepared liposome gel was sticky milky white semisolid. In vitro release experiments showed that the drug release of Lappaconitine gel and Lappaconitine liposome gel reached balance at 9 h and 15 h, and the accumulative release rate were 70.2% and 63.9%, both drugs release were in line with Higuchi equation. CONCLUSIONS: Use the optimized formulation and technology of Lappaconitine liposome to prepared Lappaconitine liposome gel with good quality and can effectively delay the release.
关键词
高乌甲素脂质体凝胶薄膜分散法正交试验处方工艺制备体外释药
Keywords
Lappaconitine liposome gelFhin film dispersion methodOrthogonal testFormulation and technologyPrepareDrug release in vitro