Theranostic Nanoparticles for Prostate Cancer Targeting

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Solution Overview

Problem

Current methods for diagnosing and treating prostate cancer are inadequate due to the small size of the prostate gland, low metabolic rate, and proximity to the bladder, leading to ineffective treatments with severe side effects, and a need for targeted molecular theranostic regimes that can deliver imaging and therapeutic agents to prostate cancer cells effectively.

Innovation Solution

Development of nanoparticles conjugated with targeting ligands, such as polyglutamated folate derivatives, that specifically bind to prostate-specific membrane antigen (PSMA) on cancer cells, allowing for the simultaneous delivery of therapeutic agents and imaging compounds to prostate cancer cells.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Measurement precision

If traditional PET imaging using small molecule radionucleotides is used, then imaging capability is provided, but detection precision is poor due to bladder interference and low metabolic rate of PCa

Engineering Contradiction:
Improvedetection precisionVSAvoiddifficulty of detecting PCa
Core Design Contradiction:
Measurement precisionVSDifficulty of detecting and measuring

Solution Approach 1:

The patent uses polyglutamated folate derivatives as intermediary targeting ligands that specifically bind to PSMA on prostate cancer cells, serving as a mediator between the imaging agent and the tumor cells. This intermediary mechanism enables specific accumulation of the radiotracer in PCa cells, overcoming the bladder interference and low metabolic rate problems of traditional FDG imaging.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the targeting parameter from non-specific FDG uptake to specific PSMA-binding folate derivatives. By altering the molecular target parameter from general metabolic activity to specific membrane antigen binding, the imaging system achieves superior detection precision for prostate cancer while eliminating bladder interference issues.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If current treatment options such as surgery, chemotherapy and radiation therapy are used, then treatment capability is provided, but harmful factors increase due to severe side effects

Engineering Contradiction:
Improvetreatment efficacyVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by delivering therapeutic agents specifically to prostate cancer cells through PSMA-targeting nanoparticles, rather than systemically distributing chemotherapy. The folate-PSMA binding mechanism ensures that the therapeutic payload is concentrated at the tumor site, improving treatment efficacy while minimizing harmful side effects to normal tissues.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The nanoparticle serves as an intermediary carrier that delivers therapeutic agents to cancer cells through PSMA binding. This intermediary delivery system replaces direct systemic chemotherapy, enabling targeted treatment that maintains efficacy while reducing the harmful side effects associated with conventional chemotherapy and radiation.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Measurement precision

If targeted molecular theranostic regimes are developed, then treatment precision is improved, but device complexity increases due to nanoparticle conjugation requirements

Engineering Contradiction:
Improvetreatment precisionVSAvoidnanoparticle conjugation complexity
Core Design Contradiction:
Measurement precisionVSDevice complexity

Solution Approach 1:

The patent applies universality by designing a multi-functional nanoparticle platform where polyglutamated folate derivatives serve dual purposes: as targeting ligands for PSMA binding and as carriers for both diagnostic (radionucleotide) and therapeutic (chemotherapy) agents. This multi-functional design achieves targeted theranostic capability while managing complexity through a unified nanoparticle system rather than separate diagnostic and therapeutic components.

Inventive Principle:
Principle #6Universality (Multi-functionality)

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 nanoparticles effectively target and deliver therapeutic agents to prostate cancer cells, reducing systemic exposure and enabling in vivo imaging, thereby improving treatment efficacy and reducing side effects while enhancing diagnostic capabilities.

Implementation Method 1

nanoparticles conjugated with targeting ligands, such as polyglutamated folate derivatives, that specifically bind to prostate-specific membrane antigen (PSMA) on cancer cells

Methodology Applied
Scientific EffectMolecular recognition:

Implementation Method 2

the nanoparticle further comprises an imaging compound and has a therapeutic agent encapsulated in the hydrophobic interior of the nanoparticle

Methodology Applied
Scientific EffectEncapsulation: Physical Containment

Data Source

PatentUS12097264B2Methods and compositions for theranostic nanoparticles
Publication Date: 2024.09.24 UNIVERSITY OF CENTRAL FLORIDA RESEARCH FOUNDATION INC
  • US12097264B2 patent drawing
  • US12097264B2 patent drawing
  • US12097264B2 patent drawing

AI summary

Provided herein is a nanoparticle for drug delivery, wherein the nanoparticle comprises a hyperbranched polyester (HBPE) nanoparticle having a hydrophobic interior, polyglutamate folate ligands conjugated to the nanoparticle, and one or more PET detectable isotopes. Also provided herein are methods of using thereof.