NTS-polyplex Nanoparticles for Targeted Gene Delivery

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Solution Overview

Problem

Current gene therapy methods for breast cancer and pleural mesothelioma are either risky due to viral vectors or inefficient with nonviral methods, lacking specificity and often affecting healthy cells, which limits their effectiveness in treating invasive and metastatic stages of these cancers.

Innovation Solution

The development of a targeted gene delivery system using NTS-polyplex nanoparticles that specifically target cells expressing the neurotensin receptor (NTSR1), carrying therapeutic or suicide genes to induce apoptosis in cancer cells, thereby reducing tumor progression and metastasis without harming healthy cells.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If viral vectors are used for gene delivery, then transfection efficiency is improved, but safety and reliability deteriorate due to risks to patients

Engineering Contradiction:
Improvetransfection efficiencyVSAvoidsafety
Core Design Contradiction:
ProductivityVSReliability

Solution Approach 1:

The patent employs non-viral polymeric vectors (such as polyethylenimine, polylysine, or dendrimers) that are safer, biodegradable, and do not integrate into the host genome, eliminating the risks associated with viral vectors while maintaining effective gene delivery through transient expression

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

2Reliability

If nonviral methods are used for gene delivery, then safety is improved, but transfection efficiency and specificity deteriorate

Engineering Contradiction:
ImprovesafetyVSAvoidtransfection efficiency
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The patent incorporates targeting moieties (such as antibodies, peptides, or aptamers) conjugated to the polymeric vector that specifically bind to receptors expressed on the surface of cancer cells, enabling selective delivery and transfection of tumor cells while sparing healthy tissues

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent uses composite polymeric structures combining cationic polymers with targeting moieties and gene payloads, creating multifunctional vectors that simultaneously ensure safety, specific targeting, and efficient gene delivery to cancer cells

Inventive Principle:
Principle #40Composite materials

3Productivity

If conventional chemotherapy is used, then tumor growth is reduced, but harmful effects on healthy cells increase

Engineering Contradiction:
Improvetumor growth reductionVSAvoidharmful effects on healthy cells
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent delivers therapeutic genes specifically to cancer cells through receptor-mediated endocytosis, enabling localized treatment that spares healthy cells from the cytotoxic effects while maintaining effective tumor growth inhibition

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 NTS-polyplex system demonstrates high specificity and efficiency in transfecting breast cancer and mesothelioma cells, effectively reducing tumor growth and metastasis through targeted gene delivery, offering a safer and more effective alternative to conventional chemotherapy.

Implementation Method 1

The strategy is based on the natural cell process of receptor-mediated endocytosis by which the transfer of genetic material is specifically targeted to the cell of interest (target cell) where the binding of a ligand to its receptor occurs on the cell surface producing endocytosis

Methodology Applied
Scientific EffectReceptor-mediated endocytosis:

Implementation Method 2

a fusogenic peptide (as hemagglutinin HA2) and a charyophillic peptide (as Vp1 of SV40) can be coupled thereto

Methodology Applied
Scientific EffectMembrane fusion:

Data Source

PatentEP2673001B1NTS-polyplex nanoparticles system for gene therapy of cancer
Publication Date: 2016.12.21 CENTRO DE INVESTIGACION Y DE ESTUDIOS AVANZADOS DEL IPN (CINVESTAV)
  • EP2673001B1 patent drawingFigure 1A~2
  • EP2673001B1 patent drawingFigure 4
  • EP2673001B1 patent drawingFigure 5~6

AI summary

The present invention describes a system of gene carrier nanoparticles capable of specifically internalize into cancer cells, eg, cancer cells involved in breast cancer, in vitro and in vivo. The system described allows the introduction of therapeutic genes specifically into target cells through NSTR1 receptor-mediated endocytosis of said system, making it possible to provide treatment for this type of conditions, for example by systemic, intravenous, or in situ administration.