Iodine-Labeled Chemoembolization Microspheres for Controlled Tumor Therapy

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Solution Overview

Problem

Existing chemoembolization and radioembolization treatments for tumors suffer from short embolization times, burst drug release, systemic toxicity, and radiation damage to non-tumor areas, limiting therapeutic efficacy and causing side effects.

Innovation Solution

A multifunctional microsphere preparation made of polyvinyl alcohol derivative and N-acryl amino acid monomer, capable of encapsulating chemotherapy drugs and labeling radionuclide iodine, providing stable embolization, slow drug release, and enabling real-time imaging through emission computed tomography or single photon emission computed tomography.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If lipiodol is used as embolization agent, then chemoembolization treatment can be performed, but embolization time is short and burst release of chemotherapeutic drugs occurs causing toxic reactions in normal tissues

Engineering Contradiction:
Improveembolization efficacyVSAvoidtoxic reactions in normal tissues
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the physical state parameter of the embolization agent from liquid (lipiodol) to solid (microspheres with 50-200 μm diameter), which fundamentally alters the embolization mechanism from transient occlusion to permanent blockage, thereby extending embolization time and enabling controlled drug release

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite microsphere system comprising polyvinyl alcohol derivative skeleton, encapsulated chemotherapeutic drugs, and labeled radionuclide iodine. This composite structure integrates embolization, chemotherapy, and radiotherapy functions while controlling drug release kinetics to avoid burst release and reduce systemic toxicity

Inventive Principle:
Principle #40Composite materials

2Productivity

If 131I labeled lipiodol is used for internal irradiation radiotherapy, then therapeutic effect is achieved, but deposition in lung causes side effects such as lung injury

Engineering Contradiction:
Improveradiotherapy efficacyVSAvoidlung injury
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the physical form of the radioembolization carrier from liquid lipiodol to solid microspheres, enabling precise control of particle size (50-200 μm) that matches tumor vasculature dimensions. This ensures selective embolization of tumor blood vessels while preventing pulmonary deposition, thereby maintaining radiotherapy efficacy while reducing lung injury

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent achieves localized delivery of radionuclide iodine-131 to tumor sites through microsphere embolization. The microspheres with controlled size and surface properties selectively accumulate in tumor vasculature, concentrating the therapeutic radiation dose at the target site while minimizing exposure to normal lung tissue

Inventive Principle:
Principle #3Local quality

3Productivity

If external irradiation is combined with chemoembolization, then survival time is prolonged, but radiation damage to non-tumor areas causes great side effects

Engineering Contradiction:
Improvesurvival timeVSAvoidradiation damage to non-tumor areas
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent extracts the radiation source from external beam radiotherapy and incorporates it directly into the embolization microspheres via radionuclide iodine-131 labeling. This transforms external irradiation into internal irradiation, where the radioactive source is delivered directly to the tumor site through the embolized blood vessels, eliminating radiation exposure to non-tumor areas while maintaining therapeutic efficacy

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent merges embolization therapy, chemotherapy, and internal radiotherapy into a single integrated microsphere preparation. The microspheres simultaneously provide mechanical embolization, encapsulated chemotherapeutic drugs, and labeled radionuclide iodine-131 for internal irradiation, achieving synergistic therapeutic effect while reducing the need for external irradiation and its associated side effects

Inventive Principle:
Principle #5Merging (Combining)

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 achieve synergistic tumor treatment with reduced drug and nuclide doses, enhancing therapeutic effect while minimizing side effects and allowing precise monitoring, with a median survival time improvement in treated rats.

Implementation Method 1

Therapeutic radionuclide 131I has a decay half-life of 8 days and emits β ray. The maximum energy of the β ray is 0.81 MeV. The maximum penetration depth is 2 mm, which is an ideal internal irradiation nuclide.

Methodology Applied
Scientific EffectBeta radiation: Radioactive Decay

Implementation Method 2

It also emits γ ray. The maximum energy of ray is 364 keV, which can be used for emission computed tomography imaging or single photon emission computed tomography imaging.

Methodology Applied
Scientific EffectGamma radiation: Radioactive Decay

Implementation Method 3

design and prepare new microsphere preparations to achieve stable labeling of radionuclide iodine

Methodology Applied
Scientific EffectRadionuclide labeling: Chemical Bonding

Implementation Method 4

stable encapsulation of chemotherapy drugs, and permanent embolization of tumor blood vessels

Methodology Applied
Scientific EffectDrug encapsulation: Adsorption

Data Source

PatentUS12551442B2Multifunctional microsphere preparation for chemoembolization therapy and imaging of tumors, and preparation method therefor
Publication Date: 2026.02.17 FUDAN UNIVERSITY
  • US12551442B2 patent drawing
  • US12551442B2 patent drawing
  • US12551442B2 patent drawing

AI summary

In the microsphere preparation for chemoembolization therapy and nuclear medicine imaging of tumor, and a preparation method thereof, the microsphere is formed by means of using a polyvinyl alcohol derivative as a framework material and polymerizing, crosslinking and curing same with an N-acryl amino acid monomer. The microsphere can label radionuclide iodine and can also absorb load chemotherapeutic drugs.