提高角膜滞留性的策略：黏附材料及递药系统的应用进展

Strategies for Improving Corneal Retention:Progress in the Application of Adhesive Materials and Drug Delivery Systems

关键词:  角膜滞留性  黏膜黏附材料  新型递药系统  眼部给药

Key words:  corneal retention  bioadhesive materials  novel ophthalmic preparation  ophthalmic drug delivery

摘要:

由于眼睛复杂的解剖结构和特殊的保护屏障使得眼部给药存在很多挑战。传统的眼用制剂普遍存在剂量损失大、停留时间短等亟待解决的关键问题。通过改善药物在眼部的滞留性能，可以提高药物的眼内生物利用度。一方面是使用黏膜黏附聚合物，如壳聚糖及其季铵衍生物、聚乙二醇、透明质酸和卡波姆等，增强制剂与角膜的黏附作用；另一方面利用纳米递药体系及原位凝胶系统与眼部黏膜的相互作用，延长药物在眼部的停留时间。因此，本文基于改善药物角膜滞留性，对新型眼部递药体系及可修饰制剂性能的生物黏附性材料进行综述，并结合二者优势，旨在为新材料和新制剂用于眼部疾病的治疗提供有效参考。

Abstract:

There are a large number of challenges in ophthalmic drug delivery because of the complex anatomical structures and the special protective barriers of the eyes. However, there is no doubt that the traditional ophthalmic preparation generally meet key problems with large dose loss and short residence time. The intraocular bioavailability of the drugs can be promoted by improving the retention performance of the drugs in the eyes. On the one hand, there are a great of mucosal adhesion polymers to modify the preparation, such as chitosan and its quaternary ammonium derivatives, polyethylene glycol, hyaluronic acid and carbomer and so on, which can enhance the adhesion between the preparation and cornea. On the other hand, researchers can utilize the interaction between nanodrug delivery system and in situ gel system and ocular mucosa, which is extremely good to lengthen the residence time of the drugs on the surface of the eyes. Therefore, in this paper, based on the improvement of corneal retention performance of drugs, the novel ocular drug delivery systems and bioadhesive materials that can modify the performance of preparations are reviewed for the purpose of providing effective reference for the treatment of ocular diseases with new materials and new preparations.