Biodegradable Microbead Composition for Controlled Drug Release

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Solution Overview

Problem

Current transarterial chemoembolization methods face challenges in controlling drug release rates and biodegradability, leading to inadequate anticancer effects and side effects due to non-degradable microbeads spreading beyond the target site.

Innovation Solution

A composition of biodegradable microbeads made from albumin cross-linked with dextran sulfate and glycosaminoglycan-based polymers, allowing for controlled drug release through electrostatic attraction, with adjustable mixing ratios to optimize drug delivery for transarterial chemoembolization.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If doxorubicin is dissolved in aqueous phase and mixed with oily lipiodol, then the drug can be administered through hepatic artery, but the drug promptly leaks into body blood and fails to accumulate in liver cancer site

Engineering Contradiction:
Improvedrug accumulation in tumorVSAvoiddrug delivery stability
Core Design Contradiction:
Quantity of substanceVSReliability

Solution Approach 1:

The patent uses microbeads with a core-shell structure where a hydrophobic core contains the dissolved doxorubicin-lipiodol complex, surrounded by a hydrophilic shell that provides stability. This shell structure prevents the microbeads from disintegrating in blood while maintaining drug encapsulation, thereby preventing drug leakage into body blood and ensuring sustained accumulation at the tumor site.

Inventive Principle:
Principle #30Flexible shells and thin films

Solution Approach 2:

The patent employs composite microbeads combining hydrophobic materials (for drug loading) and hydrophilic materials (for stability and biocompatibility). This composite structure allows the microbeads to maintain structural integrity in aqueous physiological environments while retaining the ability to deliver the hydrophobic anticancer drug, resolving the contradiction between drug accumulation and delivery stability.

Inventive Principle:
Principle #40Composite materials

2Duration of action of moving object

If polyvinylalcohol microbeads are used for embolization and drug delivery, then sustained release and embolization effect are achieved, but the microbeads do not degrade and cause inflammation or spread to other organs

Engineering Contradiction:
Improvesustained drug releaseVSAvoidinflammation and organ damage
Core Design Contradiction:
Duration of action of moving objectVSObject-affected harmful factors

Solution Approach 1:

The patent changes the material composition parameters of the microbeads by incorporating biodegradable polymers instead of non-degradable polyvinylalcohol. This parameter change maintains the sustained release capability through controlled degradation kinetics while eliminating the harmful effects of permanent foreign bodies, as the biodegradable materials are metabolized and excreted by the body after fulfilling their therapeutic function.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent adopts biodegradable microbeads that are designed to be temporary and disposable in the physiological sense - they perform their embolization and drug delivery function, then naturally degrade and are eliminated by the body. This approach eliminates the long-term harmful effects of non-degradable PVA beads while maintaining the sustained release benefit through controlled degradation.

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

3Quantity of substance

If anticancer drug is administered to hepatic artery for TACE, then tumor necrosis is achieved, but normal liver tissues may be harmed due to non-selective drug distribution

Engineering Contradiction:
Improvedrug concentration in tumorVSAvoiddamage to normal liver tissue
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by creating microbeads with specific physical and chemical properties tailored for tumor-targeted delivery. The microbeads are designed to be retained in the tumor vasculature through size-dependent embolization and to release drug locally through controlled degradation, thereby concentrating the therapeutic effect in the tumor while minimizing exposure of normal liver tissues to the anticancer drug.

Inventive Principle:
Principle #3Local quality

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 effectively controls the release rate of anticancer drugs, reducing side effects by ensuring targeted delivery and biodegradability, enhancing treatment efficacy for cancers like liver cancer.

Implementation Method 1

allowing an anticancer drug to be adsorbed onto a surface of the microbeads through an electrostatic attraction of the anionic polymers contained in the microbeads

Methodology Applied
Scientific EffectElectrostatic attraction: Electrostatics

Data Source

PatentUS10485763B2Composition for transarterial chemoembolization, comprising first and second biodegradable microbeads, and preparation method therefor
Publication Date: 2019.11.26 UTAH INHA DDS & ADVANCED THERAPEUTICS RES CENT
  • US10485763B2 patent drawing
  • US10485763B2 patent drawing
  • US10485763B2 patent drawing

AI summary

The present invention provides: a composition for transarterial chemoembolization, comprising two types of biodegradable microbeads having different anticancer drug release characteristics; and a preparation method therefor. According to the present invention, a composition for transarterial chemoembolization exhibiting a desired anticancer drug release characteristic can be effectively prepared by controlling the mixing ratio of first and second biodegradable microbeads. Therefore, the present invention can be usefully applied to the transarterial chemoembolization of liver cancer.