Low Molecular Polypeptide H-RN Ocular Barrier Penetration
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Solution Overview
Problem
Current treatments for uveitis, such as non-steroidal anti-inflammatory drugs and biological agents, face challenges including side effects, limited drug penetration due to ocular barriers, low bioavailability, and complex preparation processes, which hinder effective suppression of inflammatory reactions.
Innovation Solution
Development of a small molecule polypeptide, H-RN, with a specific amino acid sequence that can penetrate ocular tissue barriers, exhibit high solubility, and inhibit inflammation, formulated into pharmaceutical compositions for topical or systemic administration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If large molecular weight biological agents are used to inhibit ocular inflammation, then anti-inflammatory activity is improved, but penetration through ocular barriers is worsened
Solution Approach 1:
The patent segments large molecular weight biological agents into smaller peptide molecules (1-10 kDa) that retain anti-inflammatory activity while improving ocular barrier penetration. The H-RN peptide (11 amino acids) is a segmented version of larger anti-inflammatory proteins, enabling it to cross the blood-ocular barrier effectively.
Solution Approach 2:
The patent changes the molecular weight parameter from large biological agents (>76.5 kDa) to small peptides (1-10 kDa), specifically designing the H-RN peptide with 11 amino acids to optimize both penetration capability and biological activity. This parameter transformation resolves the contradiction between size and function.
2Quantity of substance
If high concentration of drugs is administered to improve bioavailability, then drug effectiveness is improved, but toxicity is worsened
Solution Approach 1:
The patent changes the molecular size parameter to enable effective drug delivery at lower concentrations. The small H-RN peptide achieves high bioavailability and sufficient tissue concentration at low doses due to its excellent penetration properties, avoiding the toxicity associated with high-concentration administration of larger molecules.
3Reliability
If complex biological agents are used to treat inflammation, then therapeutic effect is improved, but preparation complexity is worsened
Solution Approach 1:
The patent segments complex biological agents into simpler peptide structures that are easier to produce. The H-RN peptide with 11 amino acids can be synthesized using standard peptide synthesis methods, avoiding the complex recombinant expression and purification processes required for large biological agents, while maintaining therapeutic effectiveness.
Solution Approach 2:
The patent employs small peptides that can be produced through relatively simple and cost-effective chemical synthesis methods compared to complex biological agents. The H-RN peptide can be synthesized on demand without requiring complex living cell systems, reducing preparation complexity and cost.
Data Source
AI summary
Disclosed are a low molecular polypeptide for preventing and treating inflammation, a preparation method and the use thereof and a pharmaceutical composition containing the polypeptide, wherein the polypeptide can penetrate the eye tissue barrier, can maintain a high concentration in neutral tears, aqueous humour and vitreous humour, and can be used to treat inflammation.