Ocular drug delivery remains a significant challenge that is limited by poor corneal retention and permeation, resulting in low ocular bioavailability (< 5%). Worse still, the most convenient and safe route of ocular drug administration, topical administration results in a drug bioavailability of less than 1%. iRGD modified drug delivery strategies have been developed for cancer therapy, however active targeting iRGD platforms for ocular drug delivery have yet to be explored. Herein, an iRGD modified liposomes was developed for ocular drug delivery via topical administration. The results indicated that iRGD modified liposomes could prolong the corneal retention time and enhance corneal permeability in an iRGD receptor mediated manner. These findings provided a novel strategy for topical ocular drug delivery for the treatment of posterior ocular diseases.

眼部药物传递仍然是一项重大挑战，但由于角膜保留和渗透性差，导致眼部生物利用度低（<5％）而受到限制。更糟糕的是，眼内给药的最方便，最安全的途径是局部给药导致药物生物利用度低于1％。已经开发了用于癌症治疗的iRGD修饰的药物递送策略，但是尚未探索用于眼部药物递送的主动靶向iRGD平台。本文中，开发了iRGD修饰的脂质体，用于通过局部给药进行眼内药物递送。结果表明，iRGD修饰的脂质体可以通过iRGD受体介导的方式延长角膜保留时间并增强角膜通透性。