Poly(I:C) Compositions With Polyalkyleneimine for Stable Delivery

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Solution Overview

Problem

Existing formulations of polyinosinic-polycytidylic acid (poly(I:C)) molecules face challenges with stability, homogeneity, unpredictable pharmacokinetics, and limited anti-tumoral effects, necessitating frequent administration and compliance with regulatory requirements for clinical use.

Innovation Solution

A composition comprising particles with a complex of polyinosinic-polycytidylic acid and polyalkyleneimine, specifically polyethyleneimine, having controlled size, zeta potential, and concentration, optimized for pharmaceutical manufacturing, with a mono-modal diameter distribution and specific pH and osmolality, allowing stable and uniform delivery.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If naked poly(I:C) molecules are used, then therapeutic effects are observed, but stability and homogeneity are poor

Engineering Contradiction:

Improvetherapeutic effectVSAvoidstability

Core Design Contradiction:

ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent introduces polyalkyleneimine as an intermediary carrier molecule that binds to poly(I:C) molecules, forming a stable complex. This intermediary carrier protects the poly(I:C) from degradation by cytosolic RNases and improves its stability in biological systems, while still allowing the therapeutic effects to manifest.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent creates a composite formulation combining poly(I:C) molecules with polyalkyleneimine and other excipients to form a stable, homogeneous composition. This composite approach improves the overall stability and homogeneity of the therapeutic agent while preserving its anti-tumoral activity.

Inventive Principle:

Principle #40Composite materials

2Reliability

If naked poly(I:C) molecules are used, then therapeutic effects are observed, but pharmacokinetics are unpredictable

Engineering Contradiction:

Improvetherapeutic effectVSAvoidpharmacokinetics

Core Design Contradiction:

ReliabilityVSDifficulty of detecting and measuring

Solution Approach 1:

Polyalkyleneimine serves as a carrier that mediates the interaction between poly(I:C) and the biological system. This carrier system provides more predictable pharmacokinetics by controlling the release and distribution of poly(I:C), making the therapeutic effects more consistent and measurable.

Inventive Principle:

Principle #24Intermediary (Mediator)

3Reliability

If naked poly(I:C) molecules are used, then therapeutic effects are observed, but cellular uptake is poor

Engineering Contradiction:

Improvetherapeutic effectVSAvoidcellular uptake

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

Polyalkyleneimine acts as a facilitating intermediary that enhances cellular uptake of poly(I:C). The positive charge of polyalkyleneimine promotes interaction with cell membranes and endocytosis, improving the delivery of poly(I:C) into cancer cells while maintaining therapeutic efficacy.

Inventive Principle:

Principle #24Intermediary (Mediator)

4Reliability

If naked poly(I:C) molecules are used, then therapeutic effects are observed, but degradation by cytosolic RNases occurs

Engineering Contradiction:

Improvetherapeutic effectVSAvoiddegradation by cytosolic RNases

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

Polyalkyleneimine serves as a protective intermediary that shields poly(I:C) from degradation by cytosolic RNases. The complex formation between polyalkyleneimine and poly(I:C) prevents direct contact with degrading enzymes, maintaining the integrity and therapeutic activity of the poly(I:C) molecules.

Inventive Principle:

Principle #24Intermediary (Mediator)

5Reliability

If poly(I:C) is administered frequently, then therapeutic effect is maintained, but compliance and practicality are reduced

Engineering Contradiction:

Improvetherapeutic effectVSAvoidfrequency of administration

Core Design Contradiction:

ReliabilityVSLoss of time

Solution Approach 1:

The patent formulates poly(I:C) with polyalkyleneimine and excipients to create a stable composition that maintains therapeutic activity over extended periods. This continuous stable formulation reduces the frequency of administration needed to maintain therapeutic effects, improving patient compliance and practicality.

Inventive Principle:

Principle #20Continuity of useful action

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

The composition achieves stable, uniform, and effective delivery of poly(I:C), selectively inducing apoptosis in cancer cells while maintaining normal cell viability, with improved clinical applicability and reduced frequency of administration.

Implementation Method 1

a complex of polyinosinic-polycytidylic acid and polyalkyleneimine

Methodology Applied

Scientific EffectElectrostatic interaction: Electrostatics

Implementation Method 2

with controlled size, zeta potential, and concentration

Methodology Applied

Scientific EffectZeta potential: Electrostatics

Data Source

PatentUS20250332191A1Novel polyinosinic- polycytidylic acid compositions

Publication Date: 2025.10.30 BIONCOTECH THERAPEUTICS SL

AI summary

The present invention relates to compositions comprising polyinosinic (poly(I))-polycytidylic acid (poly(C)) molecules, or a salt and/or solvate thereof, comprising double-stranded polyribonucleotides. The present invention further relates to compositions wherein the disclosed respective poly(I) and poly(C) single-stranded molecules are annealed to thereby form double-stranded poly(I:C) molecules.