穿透促进剂提高滴眼液眼内通透性的研究进展

滴眼液是常用的眼药剂型，但许多药物的眼内通透性差，使其应用受到限制。研究发现，穿透促进剂可以提高药物的角膜通透性，主要通过扩大细胞间途径和增加细胞内转运两种途径实现。近年来国内外学者应用穿透促进剂研制配方提高滴眼液的角膜透性。证明氮酮等可提高亲水性药物的眼内透性，而苯扎氯胺等可提高亲脂性药物的眼内透性。研究者采用各种途径来提高肽类和蛋白类药物滴眼液的生物利用度，其中最有效的则是穿透促进剂的应用。

Current studies on penetration enhancers improving the penetrability of ophthalmic solution

Topical route of administration is wi d ely used for the treatment of ocular diseases.One of the principal problems in d rug delivery of eye is relatively low permeability of drugs across ocular tissue s.Recently, it has been found that penetration enhancers can improve corneal dru g transportation by two approaches.The first way is expanding intercellular path way, and the second one is to enhance transcellular transportation.Some reports have demonstrated that Azone has promoting effects on hydrophilic drug penetrati ng cornea,and Benzalkonium chloride can increased the ocular absorption of lipop hilic drugs.Over the years, some attempts have been made to improve ocular bioav ailability of peptides and proteins, most effective delivery method is to use pe netration enhancers.