A dual-path nano-preparation targeting sclera, and a preparation method and application thereof

By using a dual-pathway nano-formulation targeting the sclera, HIF-1α siRNA is loaded onto a ketethiol-fluorinated polyethyleneimine (TK-F-PEI) carrier and coupled with a CCL2 nucleic acid aptamer on the surface, the problems of poor targeting and systemic side effects in existing technologies are solved, achieving highly efficient treatment of myopic sclera.

CN122321160APending Publication Date: 2026-07-03EYE & ENT HOSPITAL SHANGHAI MEDICAL SCHOOL FUDAN UNIV
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Patent Information

Application Number
CN202610601107.4
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2026-05-01
Publication Date
2026-07-03

AI Technical Summary

Technical Problem

Existing technologies are difficult to effectively target the sclera in myopia. Traditional intervention methods have problems such as difficulty in penetrating the intraocular barrier, poor targeting, low drug utilization, and systemic side effects. There is an urgent need to develop a drug delivery system that can simultaneously target the CCL2 and HIF-1α pathways.

Method used

Using ketethiol-fluorinated polyethyleneimine (TK-F-PEI) as a carrier, hypoxia-inducible factor-1α small interfering RNA (HIF-1α siRNA) is loaded and coupled with a nucleic acid aptamer targeting the chemokine CCL2 on the surface to form a dual-pathway nano-formulation targeting the sclera, achieving synergistic intervention on both CCL2 and HIF-1α targets.

Benefits of technology

It achieves highly efficient targeted delivery to the sclera of myopia, significantly reduces inflammation and activation of cellular hypoxia pathways, reverses scleral remodeling, and slows down axial elongation, demonstrating good biocompatibility and promising clinical application prospects.

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Abstract

This invention discloses a dual-pathway nanoformulation targeting the sclera, its preparation method, and its applications. The nanoformulation uses ketithial-modified fluorinated polyethyleneimine (TK-F-PEI) as a carrier, with a core loaded with hypoxia-inducible factor-1α small interfering RNA (HIF-1α siRNA) and a surface-coupled chemokine CCL2 nucleic acid aptamer. After local ocular administration, this formulation can efficiently target scleral lesions in myopic eyes, neutralizing CCL2 through the aptamer to improve the scleral inflammatory microenvironment, while simultaneously releasing siRNA to silence HIF-1α to inhibit the intracellular hypoxia pathway, synergistically reversing pathological scleral remodeling and delaying axial elongation. This invention's formulation exhibits strong targeting, good safety, and significant efficacy, providing a novel combined targeted drug delivery strategy for the clinical treatment of myopia, especially high myopia.
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