iRGD decorated liposomes: A novel actively penetrating topical ocular drug delivery strategy
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iRGD decorated liposomes: A novel actively penetrating topical ocular drug delivery strategy Hai Huang1,§, Xiaorong Yang1,§, Huili Li1, Hansi Lu1, James Oswald2, Yongmei Liu1, Jun Zeng1, Chaohui Jin1, Xingchen Peng1, Jiyan Liu1, and Xiangrong Song1 () 1
Outpatient Department, Department of Critical Care Medicine, National Clinical Research Center for Geriatrics, State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, Chengdu 610041, China 2 School of Nanotechnology Engineering, University of Waterloo, Waterloo, ON N2L 3G1, Canada § Hai Huang and Xiaorong Yang contributed equally to this work. © Tsinghua University Press and Springer-Verlag GmbH Germany, part of Springer Nature 2020 Received: 19 January 2020 / Revised: 9 July 2020 / Accepted: 10 July 2020
ABSTRACT 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.
KEYWORDS ocular drug delivery, iRGD decorated liposomes, active corneal permeability, topical drops
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Introduction
Compared with drug delivery to other parts of the body, ocular drug delivery remains a significant challenge [1]. The inherently complex anatomy and physiological properties of the eye present an array of biological barriers that must be overcome for effective ocular drug delivery. These barriers include the surface epithelial barrier, aqueous vitreous, blood aqueous barrier, and blood retinal barrier, which limit the entry of drugs into the eye [2]. As a result, only about 5% of drugs reach intraocular tissues [3]. The eye is roughly divided into the anterior and posterior segment [4]. About 55% of ocular diseases occur in posterior segments. Additionally, the number of patients with posterior ocular diseases is increasing at an alarming rate [5]. Many different ocular drug delivery methods have been used for the treatment of posterior ocular diseases including topical administration, systemic delivery, and intravitreal injection [6]. Topical drops are the most convenient, safe, immediately active, patient compliant, non-invasive and widely recommended route of ocular drug administration [4]. Due to the challenges facing topical drug administration, less than 1% of the administered drug is available with current topical drops administration method
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