Preparation and Preliminary Pharmacodynamic Evaluation of Anionic Liposomes Loaded with Limonene
Limonene-loaded dipalmitoyl phosphatidylglycerol(DPPG)anionic long cycle liposomes were constructed by ethanol injection,and the formulation of the liposomes were optimized with particle size and PDI as the evaluation indexes.The results showed that the optimal liposomes were prepared in a 46.5∶10∶38.5∶5 molar ratio of hydrogenated soybean phospholipid,DPPG,N-(carbonyl-methoxypolyethylene glycol 2000)-1,2-distearoyl-sn-glycerol-3-phosphoethanolamine sodium and cholesterol.The particle size and PDI of the optimized liposomes were(62.84±2.36)nm and 0.241±0.012,respectively.Moreover,the products appeared spherical with relatively uniform distribution and obvious phospholipid bilayer structure in the TEM images.The serum stability and blood compatibility of the drug-loaded anionic liposomes were good and could be stably stored at 4 ℃ for 4 d.The cumulative release rate within the first 12 h in PBS was about 50％,and was about 80％at 48 h,showing a slow release characteristics.Pharmacodynamic studies in mouse models showed that the limonene anionic liposomes could improve the enlargement of gallbladder size,bile turbidity and gallstones in cholesterolosis mice,and also inhibit the inflammation in liver and gallbladder sites.
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