Topical Ophthalmic Peptide Formulation for Posterior Segment Delivery
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Solution Overview
Problem
Current treatments for posterior segment eye diseases, such as diabetic retinopathy and age-related macular degeneration, face challenges with systemic administration due to limited penetration across the hemato-retinal barrier, discomfort, and secondary effects from invasive local administration methods, while topical ocular routes have been ineffective in delivering therapeutic concentrations to the eye.
Innovation Solution
A topical ophthalmic composition in the form of eye drops or ointments containing somatostatin or its analogues, formulated to reach therapeutically effective concentrations in the posterior segment of the eye, utilizing a peptide concentration between 1 µg/mL and 10 mg/mL, with pH adjustment and incorporation into carriers like liposomes or nanoparticles to enhance permeability and stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If systemic parenteral administration is used, then therapeutic concentrations can be achieved in the body, but penetration across the hemato-retinal barrier is limited and the effect is not local
Solution Approach 1:
The invention extracts the active substance (somatostatin or analogue) from systemic circulation and delivers it directly to the target site (posterior segment of the eye) through topical ocular administration, bypassing the hemato-retinal barrier and achieving local therapeutic concentrations without systemic distribution
Solution Approach 2:
The invention uses topical ocular formulation as an intermediary delivery system that facilitates transport of the active substance across the hemato-retinal barrier through the ocular surface and aqueous humor, enabling localized delivery to the posterior segment
2Reliability
If intraocular or periocular injections are used, then local therapeutic effect is achieved, but patient comfort deteriorates and secondary effects increase
Solution Approach 1:
The invention replaces the mechanical injection system (needles, syringes, surgical intervention) with a topical ocular formulation system that delivers the active substance through eye drops or ointments, eliminating physical trauma and improving patient comfort while maintaining local therapeutic efficacy
Solution Approach 2:
The invention changes the administration route from invasive injection to non-invasive topical application, fundamentally altering the delivery parameters while achieving the same local therapeutic effect without the associated discomfort and secondary effects
3Ease of operation
If topical ocular administration is used, then patient comfort is improved, but therapeutic concentrations in the posterior segment are insufficient
Solution Approach 1:
The invention optimizes formulation parameters including pH adjustment (3-8), concentration (1 µg/mL to 10 mg/mL), and uses of permeation enhancers to increase the bioavailability and penetration of the active substance through the ocular surface and into the posterior segment, achieving therapeutic concentrations while maintaining patient comfort
Solution Approach 2:
The invention employs composite formulation systems combining the active substance with excipients, permeation enhancers, and stabilizing agents that work synergistically to improve penetration across ocular barriers and achieve effective concentrations in the posterior segment
Data Source
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AI summary
Topical ophthalmic formulation of peptides and their use for the treatment and/or local prevention of ocular diseases, preferably posterior segment eye diseases.