Peptide Conjugates for Cartilage Targeting

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Solution Overview

Problem

Cartilage disorders are difficult to treat due to the avascular nature of cartilage, which limits the effectiveness of existing treatments, and there is a need for precise intra-operative visualization of cancerous tissues during surgery.

Innovation Solution

Development of peptides that home to, migrate to, accumulate in, bind to, or are directed to cartilage or kidney tissues, allowing for targeted delivery of detection agents or active therapeutic agents, including peptides with specific sequences that achieve at least 70% identity with listed sequences, and conjugation with detectable labels or therapeutic agents for imaging and treatment purposes.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional treatments are used for cartilage disorders, then general delivery methods are simple, but treatment efficacy is poor due to avascular nature limiting drug delivery

Engineering Contradiction:
Improvetreatment efficacyVSAvoiddelivery system complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The invention segments the delivery system by using specific peptide sequences (such as GFOGER and variants) that can independently target cartilage tissue. This segmentation allows the therapeutic agent to be delivered specifically to cartilage without requiring complex delivery devices, thereby improving treatment efficacy while maintaining simplicity.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent uses peptide intermediaries that bind to specific receptors on cartilage cells (chondrocytes) or interact with extracellular matrix components. These peptide mediators facilitate the transfer of therapeutic agents across the avascular barrier of cartilage, enabling effective delivery without complex surgical or mechanical delivery systems.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Measurement precision

If surgical resection is performed without precise visualization, then surgery can proceed without advanced imaging, but tumor margins cannot be precisely identified leading to incomplete resection

Engineering Contradiction:
Improvetumor margin identification precisionVSAvoidimaging system complexity
Core Design Contradiction:
Measurement precisionVSDevice complexity

Solution Approach 1:

The patent employs fluorescently labeled peptides that emit visible signals when bound to tumor tissue. During surgery, these fluorescent signals provide real-time visual differentiation between tumor and healthy tissue, enabling precise margin identification. The color/fluorescence change provides intuitive visual feedback without requiring complex imaging equipment beyond standard fluorescent microscopy or imaging systems.

Inventive Principle:
Principle #32Color changes

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

Enables precise targeting and treatment of cartilage and kidney disorders, improving treatment efficacy and reducing side effects by concentrating therapeutic agents directly at the target site, and facilitates intra-operative visualization of cancerous tissues during surgery.

Implementation Method 1

peptides that home to, migrate to, accumulate in, bind to, or are directed to cartilage or kidney tissues

Methodology Applied
Scientific EffectMolecular homing/targeting:

Implementation Method 2

concentrating therapeutic agents directly at the target site

Methodology Applied
Scientific EffectSelective accumulation:

Data Source

PatentUS12048750B2Tissue-homing peptide conjugates and methods of use thereof
Publication Date: 2024.07.30 BLAZE BIOSCIENCE INC
  • US12048750B2 patent drawing
  • US12048750B2 patent drawing
  • US12048750B2 patent drawing

AI summary

Peptides that home, target, migrate to, are directed to, are retained by, or accumulate in and/or bind to the cartilage or kidney of a subject are disclosed. Pharmaceutical compositions and uses for peptides or peptide-active agent complexes comprising such peptides are also disclosed. Such compositions can be formulated for targeted delivery of an active agent to a target region, tissue, structure or cell in the cartilage. Targeted compositions of the disclosure can deliver peptide or peptide-active agent complexes to target regions, tissues, structures, or cells targeted by the peptide.