Dry eye syndrome (DES) is characterized by a chronic lack of lubrication on the surface of the eye, with consequences ranging from mild irritation to extensive ocular surface inflammation. Eye drop formulations such as Restasis(R) (a 0.05% suspension of cyclosporine A, CsA) require frequent dosing at high drug concentrations due to rapid clearance from the ocular surface. We developed a mucoadhesive nanoparticle eye drop delivery platform to prolong the ocular surface retention of topical drugs and studied both its effect on surface retention on the rabbit cornea and its efficacy in treating experimentally-induced dry eye in mice by delivering CsA bound to this delivery system. The indocyanine green (ICG) encapsulated NPs were clearly visible on the ocular surface of rabbits for up to 24 hrs after the administration. Following one month of treatment of experimental dry eye in mice, the once-a-week administration of NP-CsA 0.005-0.01% demonstrated elimination of obvious inflammation and total ocular surface recovery, whereas the administration of Restasis(R) or NP-CsA 0.025% only showed elimination of inflammatory signs, without recovery of the ocular surface tissues. The mucoadhesive nanoparticle eye-drop platform demonstrated prolonged ocular surface retention of ICG in rabbits, and effective treatment of dry eye conditions in mice with up to 50 to 100 fold reduction in overall dosage of CsA compared to Restasis(R), which may significantly reduce side effects and by extending the inter-dosing interval, improve patient compliance.

中文翻译：

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环孢霉素A负载粘膜粘附性纳米颗粒滴眼液配方可使用每周给药方案增强对小鼠实验性干眼症的治疗。

干眼症候群（DES）的特征是眼表长期缺乏润滑，其后果从轻度刺激到广泛的眼表发炎不等。眼药水制剂如Restasis（0.05％的环孢素A，CsA悬浮液）由于从眼表快速清除而需要在高药物浓度下频繁给药。我们开发了粘膜黏着剂纳米颗粒滴眼剂递送平台，以延长局部用药的眼表滞留性，并研究了其对兔角膜表面滞留的影响以及通过递送与该递送系统结合的CsA来治疗小鼠实验性干眼症的功效。 。给药后长达24小时，吲哚菁绿（ICG）封装的NP在兔眼表面清晰可见。在小鼠实验性干眼症治疗一个月后，每周一次0.005-0.01％的NP-CsA给药可消除明显的炎症和总眼表恢复，而Restasis（R）或NP-CsA给药0.025％仅显示出炎症迹象的消除，而未恢复眼表组织。粘膜粘附性纳米颗粒滴眼剂平台可延长兔ICG的眼表滞留时间，并能有效治疗小鼠干眼症，与Restasis（R）相比，CsA的总剂量可降低多达50到100倍，可显着降低副作用，并通过延长给药间隔，提高患者依从性。01％证明消除了明显的炎症和总的眼表恢复，而0.025％的Restass或NP-CsA的施用仅显示了炎性体征的消除，而没有眼表组织的恢复。粘膜粘附性纳米颗粒滴眼剂平台可延长兔ICG的眼表滞留时间，并能有效治疗小鼠干眼症，与Restasis（R）相比，CsA的总剂量可降低多达50到100倍，可显着降低副作用，并通过延长给药间隔，提高患者依从性。01％证明消除了明显的炎症和总的眼表恢复，而施用Restasis或NP-CsA为0.025％仅显示了炎症迹象的消除，而没有眼表组织的恢复。粘膜粘附性纳米颗粒滴眼剂平台可延长兔ICG的眼表滞留时间，并能有效治疗小鼠干眼症，与Restasis（R）相比，CsA的总剂量减少多达50到100倍，这可能会显着降低副作用，并通过延长给药间隔，提高患者依从性。