Anionic Polymer Microspheres for Targeted Cancer Drug Delivery

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Solution Overview

Problem

Current treatments for liver cancer, such as transarterial chemoembolization, face challenges with drug delivery due to phase separation of emulsions, leading to unsustained antitumor effects and systemic side effects, and drug-eluting beads have limitations in complete drug release and tissue necrosis risks, necessitating the development of biocompatible and efficient drug delivery methods.

Innovation Solution

The development of microspheres composed of anionic polymers like carboxymethyl cellulose and dextran sulfate, combined with trivalent metal compounds and cationic drugs, which are reduced to a nano level using homogenization techniques, to enhance water phase stability and targeted drug delivery to microvessels.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If emulsion is used for drug delivery in TACE, then drug can be delivered to liver cancer, but phase separation occurs leading to unsustained antitumor effects and systemic side effects

Engineering Contradiction:

Improvesustained antitumor effectVSAvoidemulsion stability

Core Design Contradiction:

Duration of action of moving objectVSStability of the object's composition

Solution Approach 1:

The patent changes the physical-chemical parameters of the drug delivery system by transitioning from an emulsion formulation to a nanoparticle formulation. The nanoparticles have controlled size (10-100 nm), specific surface charge (zeta potential), and composition ratios that prevent phase separation while enabling sustained drug release. This parameter transformation resolves the contradiction between emulsion stability and sustained antitumor effect.

Inventive Principle:

Principle #35Parameter changes

2Duration of action of moving object

If drug-eluting beads are used for embolization, then drug release is extended, but complete drug release is not achieved and tissue necrosis risks increase

Engineering Contradiction:

Improvedrug release durationVSAvoidtissue necrosis risk

Core Design Contradiction:

Duration of action of moving objectVSObject-affected harmful factors

Solution Approach 1:

The patent transforms the drug delivery system from macro-scale beads (40-900 μm) to nano-scale particles (10-100 nm). This size reduction enables complete drug release while preventing tissue necrosis through enhanced penetration and distribution. The nanoparticle formulation achieves near-complete drug release without the harmful effects associated with larger bead formulations.

Inventive Principle:

Principle #35Parameter changes

3Quantity of substance

If large particle size is used for embolization, then drug delivery to cancer tissue is enhanced, but penetration into microvessels is limited

Engineering Contradiction:

Improvedrug concentration in cancer tissueVSAvoidparticle size

Core Design Contradiction:

Quantity of substanceVSLength of moving object

Solution Approach 1:

The patent applies a dramatic size reduction from micrometer-scale beads to nanometer-scale particles. This parameter change enables the drug carrier to penetrate microvessels effectively while maintaining high drug concentration in the target cancer tissue. The nanoparticle size optimizes both penetration capability and drug delivery efficiency.

Inventive Principle:

Principle #35Parameter changes

4Reliability

If repeated TACE procedures are performed, then treatment efficacy is improved, but hepatotoxicity and postembolization syndrome increase

Engineering Contradiction:

Improvetreatment efficacyVSAvoidhepatotoxicity

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent transforms the formulation from emulsion to nanoparticle system with optimized composition ratios and physical properties. This parameter transformation enables repeated treatments by reducing hepatotoxicity and postembolization syndrome while maintaining treatment efficacy. The nanoparticle formulation provides safer pharmacokinetics that allow multiple treatment sessions.

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 microspheres provide a biocompatible and efficient delivery system for cancer treatment, ensuring sustained drug release and reduced systemic exposure, thereby improving treatment efficacy and minimizing side effects.

Implementation Method 1

nanoparticles including an anionic polymer and a trivalent metal compound salt

Methodology Applied

Scientific EffectIonic crosslinking: Chemical Bonding

Implementation Method 2

reduced to a nano level using homogenization techniques

Methodology Applied

Scientific EffectHomogenization: Mechanical Force

Implementation Method 3

targeted drug delivery to microvessels

Methodology Applied

Scientific EffectTargeted drug delivery: Diffusion

Data Source

PatentUS20240024532A1Novel microspheres using anionic polymer, preparation method and composition thereof

Publication Date: 2024.01.25 IMGT

AI summary

The present invention relates to novel microspheres using an anionic polymer, a preparation method thereof, a composition, and the like, and the present invention is used for a method for performing a vascular embolization and/or necrosing cancer cells by blocking major blood vessels that supply nutrients to cancer cells to induce an embolic effect, and thus may be used for the treatment of patients with cancer.