一种长眼表停留和高角膜渗透载药纳米胶束制备方法,利用眼表具有带负黏蛋白层的性质,通过在纳米胶束表面嫁接多肽,由于多肽具有两性解离的性质,通过多肽设计,使其在泪液环境中呈现带正电的性质,从而增加纳米粒子与眼表组织的相互作用,增加药物的眼表停留及角膜穿透,该药物载体能够包载不同疏水性药物后,用于不用眼表和眼内疾病的治疗。

The sealed anatomical features of the eye and its physiological activity that rapidly removes drugs are called anatomical and physiological barriers, which are the cause of more than 90% of drug loss. This aspect remains a critical issue in eye surface medication. Thus, promoting tissue permeability of drugs as well as prolonging their retention on the eye surface can improve their bioavailability and enhance their therapeutic effects. Thanks to the existence of a negatively charged mucin layer on the eye surface, several peptide-decorated polymeric micelles were prepared to enhance the interaction between the micelle and eye surface, thus prolonging the drug retention on the eye surface and promoting its tissue permeability. Our results showed that the positively charged nanomicelles could significantly prolong FK506 retention on the eye surface and enhance its corneal permeability in ex vivo and in vivo conditions. our results suggested that these positively charged nanomicelles might be a good drug delivery system for ocular surface medication.