Eyedrop-based Macromolecular Ophthalmic Drug Delivery for Ocular Fundus Disease Treatment

Overview

Journal Sci Adv

Specialties Biology
Science

Date 2023 Jan 27

PMID 36706184

Authors

Jingjing Shen

HuiQin Gao

Linfu Chen

Yutong Jiang

Shu Li

Yu Chao

Nanhui Liu

Yufei Wang

Ting Wei

Yan Liu

Jipeng Li

Muchao Chen

Jiafei Zhu

Juan Liang

Xiaoyu Zhou

Xiaofeng Zhang

Ping Gu

Qian Chen

Zhuang Liu

Affiliations

Soon will be listed here.

Abstract

Therapeutic antibodies are extensively used to treat fundus diseases by intravitreal injection, as eyedrop formulation has been rather challenging due to the presence of ocular barriers. Here, an innovative penetrating carrier was developed for antibody delivery in eyedrop formulations. We found that fluorocarbon-modified chitosan (FCS) would self-assemble with proteins to form nanocomplexes, which could effectively pass across the complicated ocular structure to reach the posterior eye segments in both mice and rabbits. In a choroidal melanoma-bearing mouse model, eyedrops containing FCS/anti-PDL1 could induce stronger antitumor immune responses than those triggered by intravenous injection of anti-PDL1. Moreover, in choroidal neovascularization-bearing mouse and rabbit models, FCS/anti-VEGFA eyedrops effectively inhibited vascular proliferation, achieving comparable therapeutic responses to those observed with intravitreal injection of anti-VEGFA. Our work presents an effective delivery carrier to treat fundus diseases using eyedrop of therapeutic proteins, which may enable at-home treatment of many eye diseases with great patient compliance.

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