PEDF-Derived Peptide Formulation Stabilization via Copolymer and pH Control

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Solution Overview

Problem

Formulations of PEDF-derived short peptides (PDSP) lack long-term stability, which is a critical issue for their effectiveness as therapeutic agents in treating various diseases.

Innovation Solution

A composition comprising PEDF-derived short peptides, a stabilizer (copolymer of vinylpyrrolidone and vinyl acetate), and a buffer system (citric acid, phosphate, boric acid, or histidine buffer system) is developed, with a pH range of 4-9, to enhance stability and bioavailability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If PEDF-derived short peptides are formulated as therapeutic agents, then therapeutic efficacy is improved, but long-term stability deteriorates

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidlong-term stability
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent introduces a stabilizer as an intermediary substance that mediates between the PEDF-derived short peptide and the formulation environment. This stabilizer acts as a protective intermediary that prevents direct interaction between the peptide and destabilizing factors, thereby maintaining peptide stability while preserving therapeutic activity.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent employs parameter changes by adjusting pH to a specific range (4-9) and controlling temperature conditions to optimize peptide stability. By modifying these physical and chemical parameters, the formulation maintains the peptide's structural integrity and therapeutic efficacy over extended periods.

Inventive Principle:
Principle #35Parameter changes

2Stability of the object's composition

If peptide formulation stability is improved, then long-term storage is enhanced, but bioavailability may be compromised

Engineering Contradiction:
Improveformulation stabilityVSAvoidbioavailability
Core Design Contradiction:
Stability of the object's compositionVSReliability

Solution Approach 1:

The patent optimizes pH parameters within the range of 4-9 to achieve a balance between stability and bioavailability. This parameter optimization ensures that the peptide maintains structural stability while remaining sufficiently soluble and absorbable for effective bioavailability.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite formulation system combining the PEDF-derived short peptide with stabilizing agents and buffer systems. This composite approach allows the formulation to simultaneously achieve both stability through the stabilizer and bioavailability through the optimized pH environment.

Inventive Principle:
Principle #40Composite materials

Data Source

PatentUS20240261379A1Composition comprising PEDF-derived short peptide, preparation method thereof, and use thereof
Publication Date: 2024.08.08 GRAND PHARMA (CHINA) CO LTD

AI summary

The present invention relates to a composition, a preparation method therefor, and a use thereof. The composition comprises a PEDF-derived short peptide (PDSP), a stabilizer, and a buffer agent. The pH of the composition ranges from 4 to 9. The stabilizer is a copolymer of vinyl pyrrolidone and vinyl acetate. The buffer agent is selected from a citric acid buffer system, a phosphoric acid buffer system, a boric acid buffer system, a histidine buffer system, or a combination thereof. The composition has improved stability, small irritation to eyes, and/or high bioavailability.