Boric Acid-Buffered PEDF-Derived Peptide Formulations for Stress Stability

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Solution Overview

Problem

Existing formulations of PEDF-derived short peptides (PDSPs) lack long-term stability, particularly under stress conditions such as chemical and physical stress during storage.

Innovation Solution

Formulations of PDSPs are developed using boric acid buffers with non-ionic tonicity agents like glycerin, sucrose, or sorbitol, and pH values between 5 and 9, specifically around 6.5 to 7.5, to enhance stability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional formulations of PDSPs are used, then the peptides can be administered, but they lack long-term stability under stress conditions

Engineering Contradiction:

Improvelong-term stabilityVSAvoidpeptide stability under stress

Core Design Contradiction:

ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent changes the buffer system from conventional options to boric acid buffer at pH 7.0, and optimizes the concentration of non-ionic tonicity agents (glycerin, sucrose, or sorbitol) to specific ranges. These parameter changes in the formulation composition resolve the contradiction by providing a chemical environment that maintains peptide stability while allowing administration.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent introduces non-ionic tonicity agents (glycerin, sucrose, or sorbitol) as intermediary substances that mediate between the peptide and the buffer environment. These intermediaries protect the peptide from stress conditions while maintaining physiological compatibility, thus resolving the stability contradiction.

Inventive Principle:

Principle #24Intermediary (Mediator)

2Ease of operation

If ionic tonicity agents like NaCl are used, then tonicity is adjusted, but peptide stability decreases under shearing forces

Engineering Contradiction:

Improvetonicity adjustmentVSAvoidpeptide stability under shearing force

Core Design Contradiction:

Ease of operationVSStability of the object's composition

Solution Approach 1:

The patent replaces expensive and unstable ionic tonicity agents with cheaper, more stable non-ionic alternatives (glycerin, sucrose, or sorbitol). These non-ionic agents provide the same tonicity adjustment function without the harmful effects on peptide stability under shearing forces, effectively resolving the contradiction.

Inventive Principle:

Principle #27Cheap short-living objects (Disposable)

Solution Approach 2:

The patent changes the type of tonicity agent from ionic to non-ionic, and optimizes their concentration to achieve both tonicity adjustment and enhanced stability. This parameter change resolves the contradiction by finding a substance that satisfies both requirements simultaneously.

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentEP4281099B1Compositions comprising PEDF-derived short peptides (PDSP) and uses thereof

Publication Date: 2025.10.01 BRIM BIOTECH INC

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AI summary

An aqueous formulation includes a PEDF-derived short peptide (PDSP) having the sequence of one of SEQ ID NO: 1, 2, 3, 5, 6, 8, or 9; boric acid at a concentration of 0.01 mM – 923 mM; and a non-ionic tonicity agent. The pH value is around 5.5–8.4. The non-ionic tonicity agent is glycerin, sucrose, mannitol, or sorbitol. A concentration of the PDSP is 0.01% - 1% w/v.