Studies On Solubilization Of Cyclosporine A Nanoparticle And The Preparation Of Cyclosporine A Eye Drops

OBJECTIVE: To study the prescription and preparation technology of cyclosporin A, evaluate its quality and observe the irritant effect of cyclosporin A eye drops on rabbit eyes.METHODS: Mixed micelles and nanoparticle colloids of cyclosporin A were preparated using sodium cholate/lecithin and polylactec-acid as carriers respectively, one of them was chosen to optimize the prescription of cyclosporin A eye drops through evaluating degree of solubilization of cyclosporin A and preparation technology by testing cyclosporin A contents, encapsulation efficiency, diameters and pH of them respectively. Meanwhile, its irritant effect on rabbit eyes was evaluated by counting rabbit nictation times, short-time multiple eye drops irritation (once per 15 minute for continuously 2 hours) and long-time eye drops irritation ( 5 times per day for continuously 4 weeks).RESULTS: Results showed that cyclosporin A mixed micelles was better than nanoparticle colloids on higher drug contents, higher encapsulation efficiency, narrower diameters and perfect pH fit for eye. There was no significant difference on rabbit nictation times between cyclosporin A eye drops preparated with mixed micelles and excipient. However, light irritation was observed in short-time multiple regular irritation and long-time multiple regular irritation on tested rabbit eyes.CONCLUSION: The solubilization of cyclosporin A in water could be improved significantly by sodium cholate/lecithin system. Cyclosporin A eye drops could be made through solubilization effect of the sodium cholate/lecithin on cyclosporin A .