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OBJECTIVE To prepare cepharanthine(CEP) polymer micelles and characterize them. METHODS The CEP polymer micelles were prepared by solvent evaporation method. Based on the single factor investigation, the preparation process was optimized by Box-Behnken response surface method with the entrapment efficiency and drug loading as indicators, and the particle size distribution, potential and in vitro release of the micelles were characterized. RESULTS The optimum process of CEP polymer micelle was as follows: 50 mg of MA-PEG-PLGA and 17.82 mg of CEP were dissolved in 0.25 mL of acetone, added dropwise into 14 mL of PBS solution at 60 ℃ and stirred on a magnetic stirrer at a speed of 1 000 r·min-1 for 4 hours to obtain a clear CEP polymer micelle. The optimized CEP polymer micelles are spherical, with an average particle size of (111.37±3.51) nm, a PDI of (0.21±0.01) and a Zeta potential of (-9.78±2.15) mV. In vitro release results showed that CEP was released rapidly within 10 h, and its micelles released (79.99±4.96)% and (71.66±2.62)% respectively within 72 h, indicating that CEP could be released slowly after being made into micelles. The results of freeze-drying agent investigation showed that 0.5% poloxamer 188 had the smallest change in complex particle size after freeze-drying. The results of hemolysis test showed that the hemolysis rate was obviously reduced after CEP was made into micelles. CONCLUSION The optimized formulation and technology in this study can be used for the preparation of CEP-MA-PEG-PLGA polymer micelles, which lays a foundation for the subsequent development of CEP targeted preparations.
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| 科 Family | 属数 Number of genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) | 属 Genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) |
|---|---|---|---|---|---|---|
| 鹅膏菌科Amanitaceae | 2 | 11 | 5.26 | 鹅膏菌属 Amanita | 10 | 4.78 |
| 小菇科 Mycenaceae | 2 | 12 | 5.74 | 丝盖伞属 Inocybe | 5 | 2.39 |
| 多孔菌科 Polyporaceae | 8 | 14 | 6.70 | 蜡蘑属 Laccaria | 5 | 2.39 |
| 红菇科 Russulaceae | 3 | 23 | 11.00 | 小皮伞属 Marasmius | 6 | 2.87 |
| 小菇属 Mycena | 11 | 5.26 | ||||
| 光柄菇属 Pluteus | 5 | 2.39 | ||||
| 红菇属 Russula | 17 | 8.13 | ||||
| 栓菌属 Trametes | 5 | 2.39 |
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