Poly(I:C)-Polyal-kyleneimine Particles for Stable Cancer Delivery

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Solution Overview

Problem

Existing formulations of poly(I:C) molecules for cancer treatment face challenges such as low stability, poor homogeneity, unpredictable pharmacokinetics, and limited antitumoral effects, necessitating frequent administration and compliance with regulatory requirements for reproducibility and uniformity.

Innovation Solution

A composition comprising particles formed by a complex of double-stranded polyribonucleotides, such as polyinosinic-polycytidylic acid, with polyalkyleneimine, with specific size, zeta potential, and molecular weight ratios, ensuring uniformity and stability for effective cancer treatment.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If naked poly(I:C) molecules are used for cancer treatment, then immune system activation against tumors is achieved, but stability is low and pharmacokinetics are unpredictable

Engineering Contradiction:
ImprovestabilityVSAvoidformulation complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent uses polyalkyleneimine as an intermediary carrier molecule that binds to poly(I:C) molecules, forming a complex that improves stability and pharmacokinetics. The polyalkyleneimine acts as a mediator between the poly(I:C) and the biological system, protecting it from degradation while maintaining therapeutic activity.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention creates a composite formulation combining poly(I:C) molecules with polyalkyleneimine polymers. This composite structure integrates the therapeutic properties of poly(I:C) with the stabilizing and pharmacokinetic benefits of the polyalkyleneimine carrier, resulting in a formulation with improved reliability.

Inventive Principle:
Principle #40Composite materials

2Reliability

If poly(I:C) molecules are administered frequently to achieve effective therapeutic effect, then antitumoral activity is improved, but loss of time and patient compliance are worsened

Engineering Contradiction:
Improveantitumoral effectVSAvoidadministration frequency
Core Design Contradiction:
ReliabilityVSLoss of time

Solution Approach 1:

The patent modifies the pharmacokinetic parameters of poly(I:C) by forming a complex with polyalkyleneimine. This parameter change extends the half-life and improves the pharmacokinetic profile, allowing for less frequent administration while maintaining effective antitumoral activity.

Inventive Principle:
Principle #35Parameter changes

3Productivity

If poly(I:C) molecules are formulated at high concentration to reduce administration frequency, then productivity is improved, but manufacturing precision and homogeneity become more difficult to achieve

Engineering Contradiction:
Improveadministration frequencyVSAvoidhomogeneity
Core Design Contradiction:
ProductivityVSManufacturing precision

Solution Approach 1:

The formation of the poly(I:C)-polyalkyleneimine complex changes the physical and chemical parameters of the formulation, enabling stable high-concentration formulations that maintain homogeneity and manufacturing precision even at elevated concentrations.

Inventive Principle:
Principle #35Parameter 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

The composition achieves stable, homogeneous, and reproducible delivery of poly(I:C) molecules, enhancing therapeutic efficacy and compliance with regulatory standards, demonstrating selective cancer cell killing with minimal impact on normal cells.

Implementation Method 1

a complex of double-stranded polyribonucleotides, such as polyinosinic-polycytidylic acid, with polyalkyleneimine

Methodology Applied
Scientific EffectElectrostatic interaction: Electrostatics

Implementation Method 2

demonstrating selective cancer cell killing with minimal impact on normal cells

Methodology Applied
Scientific EffectCellular uptake:

Data Source

PatentUS20250352665A1Polyinosinic- polycytidylic acid compositions and methods of making same
Publication Date: 2025.11.20 HIGHLIGHT THERAPEUTICS SL
  • US20250352665A1 patent drawing
  • US20250352665A1 patent drawing
  • US20250352665A1 patent drawing

AI summary

The present invention relates to compositions comprising particles, each of said particles comprising a complex of at least one double-stranded polyribonucleotide, such as polyinosinic-polycytidylic acid [poly(IC)], and at least one linear polyal-kyleneimine. The particles are also characterized by their monomodal diameter distribution and z-average diameter within specific ranges. The present invention additionally relates to the use of said compositions as medicaments, in particular for the treatment of a cell growth disorder characterized by abnormal growth of human or animal cells, as well as to processes for the preparation of said compositions.