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OBJECTIVE To prepare polymyxin B sulfate multivesicular liposomes (PMB-MVLs), optimize their formulation, and their quality, stability, release and investigate their antibacterial activity in vitro. METHODS The PMB-MVLs were prepared by the double-emulsion method. The response surface method of Box-Behnken design was used to optimize the initial prescription. High performance liquid chromatography method was established to quantitatively analyze PMB in PMB-MVLs. The physicochemical properties, the in vitro drug release behavior, in vitro antimicrobial activity and formulation safety of PMB-MVLs were investigated. RESULTS The appearance of PMB-MVLs prepared by optimal prescription were non-concentric spherical vesicles with uniform size. The encapsulation efficiency of PMB-MVLs were (69.521±1.531)%. The average particle size was (5.84±1.42) μm, and the average Zeta potential was (-26.77±0.55)mV. The PMB-MVLs showed good stability when stored at 4 ℃ for one month. The results showed that PMB-MVLs were released continuously for 72 h in vitro, and there was no sudden release effect. The in vitro antibacterial activities of PMB-MVLs on E.coli and P.aeruginosa were significantly stronger than those of the free PMB. And PMB-MVLs has no risk of hemolysis within its range of antimicrobial activity. CONCLUSION The slow-release PMB-MVLs are successfully prepared with uniform particle size, high encapsulation efficiency, and enhanced antibacterial activity.
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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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