Dry Eye Peptide Composition for Tear Film Stability
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Solution Overview
Problem
Dry eye (DE) is a common condition characterized by inadequate tear production or rapid tear evaporation, leading to symptoms such as dryness, irritation, and blurred vision, with existing treatments often inadequate in addressing the underlying stability and biological activity of peptides used for tear stimulation.
Innovation Solution
Development of novel peptides with specific amino acid compositions and identities, formulated into ophthalmic solutions, contact lens care products, and methods for administering these peptides to stimulate tear production and stabilize the tear film.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing peptide treatments are used for dry eye, then tear production may be stimulated, but peptide stability and biological activity are insufficient
Solution Approach 1:
The patent modifies peptide sequences by changing amino acid parameters - specifically incorporating hydrophobic amino acids (I, V, L, F, C, M, A) in Y sequences and hydrophilic amino acids (R, K, N, D, Q, E, H) in X sequences. This parameter change optimizes both stability and biological activity by creating peptides with specific hydropathic characteristics that enhance tear film stability while maintaining tear production stimulation capability
Solution Approach 2:
The invention creates composite peptide structures combining different amino acid types in specific patterns - hydrophobic Y sequences (10-50 amino acids) paired with hydrophilic X sequences (40-65 amino acids). This composite structure allows the peptide to simultaneously achieve stability through hydrophobic interactions and biological activity through hydrophilic interactions, resolving the contradiction between stability and productivity
2Stability of the object's composition
If peptide sequences are modified to improve stability, then shelf-life increases, but biological activity may be reduced
Solution Approach 1:
The patent applies local quality by assigning different hydrophobicity characteristics to different regions of the peptide sequence. The Y sequence (10-50 amino acids) is designed with hydrophobic amino acids to provide stability and membrane interaction capability, while the X sequence (40-65 amino acids) uses hydrophilic amino acids to maintain biological activity and solubility. This localized functional differentiation allows each region to optimize its specific property without compromising the other
Solution Approach 2:
The peptide is segmented into two functional domains: X sequences containing hydrophilic amino acids responsible for biological activity and solubility, and Y sequences containing hydrophobic amino acids responsible for stability and membrane interaction. This segmentation allows independent optimization of stability and biological activity through separate sequence design, then integrates both functions in the complete peptide structure
3Ease of operation
If hydrophobic amino acids are increased to improve membrane interaction, then cell membrane translocation improves, but peptide aggregation may occur
Solution Approach 1:
The patent precisely controls the parameter of hydrophobic amino acid content by limiting Y sequences to 10-50 amino acids with at least 50% hydrophobic residues, while balancing this with X sequences of 40-65 amino acids with hydrophilic residues. This parameter optimization ensures sufficient membrane interaction capability through the hydrophobic Y region while the hydrophilic X region prevents aggregation by providing solubility and preventing excessive hydrophobic clustering
Data Source
AI summary
The present disclosure provides a novel polypeptide. Also provided is an ophthalmic composition for treating or preventing dry eye (DE) or DE associated disorders. Also provided is a method for treating or preventing DE or DE associated disorders, stimulating tears, stabilizing tear film or any combination thereof in a subject in need thereof, comprising administering to the subject an effective amount of the novel peptides. Also provided is a contact lenses care product comprising the novel peptides and the preparation method thereof.