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目的:考察N-三甲基壳聚糖(TMC)包覆司帕沙星(SL)纳米脂质体的离体角膜渗透性及体外抗菌性。方法:采用Franz扩散池,以兔离体角膜为屏障,分别考察TMC包覆SL纳米脂质体、SL纳米脂质体及SL滴眼液的角膜渗透性,并计算角膜渗透参数。以大肠埃希菌、金黄色葡萄球菌、铜绿假单胞菌和枯草芽孢杆菌为菌种,分别考察以上3种SL制剂的体外抑菌性,得到最小抑菌浓度(MIC)、最低杀菌浓度(MBC)及抑菌率与时间的关系。结果:3种SL制剂的稳态渗透速率J、角膜渗透系数P及角膜滞留率大小顺序为:TMC包覆SL纳米脂质体>SL纳米脂质体>SL滴眼液。时滞τ及角膜扩散系数D的大小顺序为:SL纳米脂质体>SL滴眼液>TMC包覆SL纳米脂质体。对4种细菌的抑菌活性大小顺序为:TMC包覆SL纳米脂质体>SL纳米脂质体>SL滴眼液。结论:脂质体可增强SL的角膜渗透作用及储库作用,体外抑菌活性也较滴眼液增强,而TMC包覆后效果更佳,且作用迅速,值得进一步研究。
Objective: To investigate the in vitro corneal permeability and in vitro antibacterial activity of sparing-wall nanocapsules coated with N-trimethyl chitosan (TMC). Methods: The corneal permeability of TMC-coated SL nanosomes, SL nanoliposomes and SL eye drops were investigated by using Franz diffusion cells and rabbit cornea as a barrier. The corneal permeability parameters were calculated. Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa and Bacillus subtilis as the strains, respectively, in vitro antibacterial activity of the above three kinds of SL formulations to obtain the minimum inhibitory concentration (MIC), the minimum bactericidal concentration ( MBC) and the relationship between antibacterial activity and time. Results: The steady-state permeation rate J, corneal permeability coefficient P and corneal retention rate of three kinds of SL preparations were as follows: TMC coated SL nanoliposomes> SL nanoliposomes> SL eye drops. The order of delay τ and corneal diffusion coefficient D are: SL nanoliposomes> SL eye drops> TMC coated SL nanoliposomes. The order of antibacterial activity to four kinds of bacteria was as follows: TMC coated SL nanoliposomes> SL nanoliposomes> SL eye drops. CONCLUSION: Liposomes can enhance the corneal osmotic effect and depot function of SL, and enhance the antibacterial activity in vitro compared with the ophthalmic solution. However, the effect of TMC coating is better and the effect is rapid, which deserves further study.