Multivalent Peptide-Cellulose Conjugates for Prolonged Tumor Retention

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Solution Overview

Problem

Current cancer treatments using immunotherapeutic peptides face challenges such as rapid clearance from tumor sites due to the circulatory and lymphatic system, leading to frequent dosing requirements and systemic side effects, which can be mitigated by increasing the intra-tumoral residence time of drugs.

Innovation Solution

Development of a conjugate comprising a biologically active polypeptide linked to a biocompatible cellulose polymer via an organic linker, enhancing the intra-tumoral half-life and reducing systemic exposure.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If immunotherapeutic peptides are administered systemically to treat cancer, then the drug can reach the tumor site, but the circulatory and lymphatic system rapidly clear the drug from the tumor site, requiring frequent dosing and causing systemic side effects

Engineering Contradiction:
Improvedrug concentration at tumor siteVSAvoidintra-tumoral residence time
Core Design Contradiction:
Quantity of substanceVSDuration of action of stationary object

Solution Approach 1:

The patent creates a composite material by conjugating the immunotherapeutic peptide (active agent) with a biocompatible polymer carrier. This composite structure allows the peptide to be delivered to the tumor site while the polymer component provides prolonged retention at the injection site, reducing clearance by the circulatory and lymphatic systems. The composite enables sustained local release of the peptide without requiring frequent systemic re-dosing.

Inventive Principle:
Principle #40Composite materials

2Reliability

If potent drugs are administered systemically to maintain therapeutic dose at tumor site, then therapeutic effect is achieved, but dangerous side effects occur elsewhere in the body

Engineering Contradiction:
Improvetherapeutic effectVSAvoidsystemic side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by modifying the drug delivery system to concentrate the therapeutic agent specifically at the tumor site through intra-tumoral injection of the polymer-conjugated peptide. The biocompatible polymer provides localized retention at the injection site, creating a high concentration gradient at the tumor while minimizing systemic circulation. This localized delivery approach maintains therapeutic efficacy at the target site while reducing exposure and side effects in healthy tissues.

Inventive Principle:
Principle #3Local quality

3Quantity of substance

If intra-tumoral injection is used to deliver potent drugs directly into the tumor, then the dose required is lower, but the injection requires professional administration and is more burdensome and costly

Engineering Contradiction:
Improvedrug doseVSAvoidadministration complexity
Core Design Contradiction:
Quantity of substanceVSEase of operation

Solution Approach 1:

The biocompatible polymer acts as an intermediary carrier that facilitates intra-tumoral drug delivery. The polymer-conjugated peptide formulation provides sustained release at the injection site, which extends the therapeutic effect and reduces the frequency of administrations required. This intermediary system maintains lower drug doses while reducing overall treatment burden by decreasing the number of professional administrations needed compared to frequent systemic dosing.

Inventive Principle:
Principle #24Intermediary (Mediator)

4Manufacturing precision

If drugs are administered directly to the tumor site, then local efficacy is improved, but the circulatory and lymphatic system rapidly clear the drugs from the injection site into the bloodstream

Engineering Contradiction:
Improvelocal drug deliveryVSAvoiddrug clearance from tumor site
Core Design Contradiction:
Manufacturing precisionVSLoss of substance

Solution Approach 1:

The patent implements continuity of useful action through the biocompatible polymer carrier, which provides sustained release of the immunotherapeutic peptide at the tumor site. The polymer matrix maintains a continuous reservoir of the active agent, releasing it gradually over time rather than allowing rapid clearance. This continuous local supply overcomes the rapid clearance by circulatory and lymphatic systems, maintaining therapeutic concentrations at the tumor site without requiring frequent re-administration.

Inventive Principle:
Principle #20Continuity of useful action

Data Source

PatentUS20250213704A1Method of treating a cancer with a multivalent peptide conjugate
Publication Date: 2025.07.03 VALITOR INC
  • US20250213704A1 patent drawing
  • US20250213704A1 patent drawing
  • US20250213704A1 patent drawing

AI summary

The present disclosure is directed to peptide-polymer conjugates, and their use in treating cancers, such as solid tumors.