The preparation of silybin liposome by ethanol injection method and its quality evaluation
Jun Jia
Abstract
Jun Jia
Abstract
Objective To prepare silybin liposome, optimize the formulation and preparation technology, and evaluate its properties. Method Silybin liposome was prepared by ethanol injection method. HPLC and ultrafiltration methods were used to determine silybin entrapment efficiency in the liposome. Factors influencing the encapsulation efficiency of silybin in the liposome was investigated, and formulation and process parameters were optimized with orthogonal design. Result The optimized condition was as follows: the total phospholipid concentration 0.006 mg·mL-1, the ratio of phospholipid to cholesterol 10:1(m:m), the ratio of drug to total lipid 1:60 (m:m), pH=7.30, the lipid solution was prepared by dissolving phospholipid, cholesterol and drug together in ethanol of 35 ℃ for 25 min. Encapsulation efficiency of silybin in liposome reached (92.44±0.98) % after optimization, with the mean size of (151±21) nm and the Zeta potential of (-34.6±1.2) mV. The prepared liposome caused no hemolysis. Conclusion It is feasible to prepare silybin liposome by ethanol injection method. The obtained silybin liposome has high encapsulation efficiency, low particle size without hemolysis.
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Objective To prepare silybin liposome, optimize the formulation and preparation technology, and evaluate its properties. Method Silybin liposome was prepared by ethanol injection method. HPLC and ultrafiltration methods were used to determine silybin entrapment efficiency in the liposome. Factors influencing the encapsulation efficiency of silybin in the liposome was investigated, and formulation and process parameters were optimized with orthogonal design. Result The optimized condition was as follows: the total phospholipid concentration 0.006 mg·mL-1, the ratio of phospholipid to cholesterol 10:1(m:m), the ratio of drug to total lipid 1:60 (m:m), pH=7.30, the lipid solution was prepared by dissolving phospholipid, cholesterol and drug together in ethanol of 35 ℃ for 25 min. Encapsulation efficiency of silybin in liposome reached (92.44±0.98) % after optimization, with the mean size of (151±21) nm and the Zeta potential of (-34.6±1.2) mV. The prepared liposome caused no hemolysis. Conclusion It is feasible to prepare silybin liposome by ethanol injection method. The obtained silybin liposome has high encapsulation efficiency, low particle size without hemolysis.
Key concepts: Liposome, Chromatography, Chemistry, Phospholipid, Zeta potential, Ethanol, Particle size, Dissolution