Although topical drug delivery is a convenient route of administration to treat various eye diseases, it has serious limitations due to rapid clearance of the formulation from the surface of the eye. In this study, we engineered microparticles for both sustained drug delivery and prolonged residence time on the extraocular surface. Microparticles were fabricated by emulsification using poly(lactic-co-glycolic acid) (PLG) and poly(ethylene glycol) (PEG) as the core material and mucoadhesion promoter, respectively. The particle size was controlled to be less than 10 microm to avoid eye irritation and for eventual clearance through the lacrimal canals. In vitro mucoadhesion tests showed that PLG microparticles with PEG adhered better to the mucous membrane under the conditions employed in this study compared to the microparticles without PEG. When an aqueous suspension of microparticles with PEG was administered topically to the rabbit eye in vivo, microparticles were seen for up to 30 min on the ocular surface in the cul-de-sac, which was a dramatic increase in residence time as compared to conventional eye drop formulations. We conclude that mucoadhesive microparticles are promising vehicles for ophthalmic drug delivery.

中文翻译：

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用于眼科药物递送的粘膜粘附微粒

尽管局部给药是治疗各种眼病的便捷给药途径，但由于制剂从眼表面快速清除，因此具有严重的局限性。在这项研究中，我们设计了微粒以实现持续的药物递送和延长在眼外表面的停留时间。分别使用聚（乳酸-乙醇酸共聚物）（PLG）和聚（乙二醇）（PEG）作为核心材料和黏膜粘附促进剂，通过乳化制备微粒。粒径被控制为小于 10 微米，以避免眼睛刺激和最终通过泪道清除。体外粘膜粘附试验表明，与不含 PEG 的微粒相比，在本研究采用的条件下，含有 PEG 的 PLG 微粒更好地粘附到粘膜上。当将含有 PEG 的微粒的水性悬浮液在体内局部给药于兔眼时，微粒在眼底尽头的眼表上可观察到长达 30 分钟，与常规方法相比，停留时间显着增加。滴眼液配方。我们得出结论，粘膜粘附微粒是用于眼科药物递送的有前途的载体。