Cholesterol-Containing rHDL Nanoparticles for BBB Transport and Tumor Efflux

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Solution Overview

Problem

Current treatments for glioblastoma and pancreatic cancer are limited by the blood-brain barrier's permeability, and there is a need for targeted delivery systems that can effectively cross the BBB to deliver therapeutic agents, while also addressing cholesterol dysregulation in cancer cells.

Innovation Solution

Development of reconstituted high-density lipoprotein (rHDL) nanoparticles comprising cholesterol, phospholipids, and apolipoprotein E, which can target LDLR and induce cholesterol efflux, thereby killing cancer cells and crossing the BBB.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional chemotherapeutic agents are used to treat glioblastoma, then treatment can be administered systemically, but the blood-brain barrier limits effective delivery to the tumor site

Engineering Contradiction:

Improvetreatment effectivenessVSAvoidblood-brain barrier permeability

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent uses HDL nanoparticles as intermediary carriers that can cross the blood-brain barrier. These nanoparticles mediate the delivery of therapeutic agents (such as oxysterols or other cancer-fighting drugs) from the bloodstream into the brain tissue, overcoming the BBB permeability limitation while maintaining systematic administration capability

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent modifies the physical and chemical parameters of the drug delivery system by formulating drugs within HDL nanoparticle structures. This changes the size, surface properties, and transport characteristics of the therapeutic agents, enabling them to penetrate the blood-brain barrier while maintaining their biological activity

Inventive Principle:

Principle #35Parameter changes

2Productivity

If cholesterol is increased in cancer cells to support tumor growth, then cancer cell proliferation is promoted, but cholesterol efflux mechanisms can be activated to eliminate excess cholesterol and induce cell death

Engineering Contradiction:

Improvecancer cell proliferationVSAvoidintracellular cholesterol accumulation

Core Design Contradiction:

ProductivityVSObject-generated harmful factors

Solution Approach 1:

The patent exploits the harmful effect of intracellular cholesterol accumulation in cancer cells by introducing HDL nanoparticles that deliver cholesterol efflux inducers. The cancer cells' own cholesterol metabolism is turned against them - the nanoparticles trigger the cells to actively efflux their excess cholesterol through ABCA1 and ABCG1 transporters, depleting the cholesterol needed for tumor growth and inducing cell death

Inventive Principle:

Principle #22Blessing in disguise (Convert harm into benefit)

Solution Approach 2:

The patent changes the intracellular cholesterol metabolism parameters by modulating the expression and activity of cholesterol transport proteins (ABCA1, ABCG1). Through HDL nanoparticle delivery of activators, the patent shifts the cholesterol metabolism balance from accumulation to efflux, fundamentally altering the cellular cholesterol homeostasis to achieve anti-cancer effects

Inventive Principle:

Principle #35Parameter changes

3Reliability

If targeted delivery systems are developed to cross the blood-brain barrier, then therapeutic delivery to glioblastoma is improved, but the complexity of the delivery system increases

Engineering Contradiction:

Improvetherapeutic delivery efficiencyVSAvoiddelivery system complexity

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The HDL nanoparticle platform provides multi-functionality: it serves as a vehicle for crossing the blood-brain barrier, a delivery system for various therapeutic agents (oxysterols, chemotherapeutics, genes), and a mechanism for inducing cholesterol efflux. This universal platform reduces overall system complexity by consolidating multiple functions into a single nanoparticle system rather than requiring separate systems for each function

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 rHDL nanoparticles effectively induce cholesterol efflux and kill cancer cells, including glioblastoma and pancreatic cancer cells, while being non-toxic to BBB constituent cells, and can also be used to treat Alzheimer's disease.

Implementation Method 1

the rHDL nanoparticles effectively induce cholesterol efflux and kill cancer cells

Methodology Applied

Scientific EffectCholesterol efflux:

Implementation Method 2

there is a need for targeted delivery systems that can effectively cross the BBB to deliver therapeutic agents

Methodology Applied

Scientific EffectBlood-brain barrier permeability: Permeation

Data Source

PatentUS20260053747A1Reconstituted high-density lipoprotein nanoparticles comprising cholesterol

Publication Date: 2026.02.26 MEPSGEN CO LTD

AI summary

The present invention relates to: reconstituted high-density lipoprotein nanoparticles comprising cholesterol; and a composition for preventing or treating Alzheimer's disease and cancer, the composition comprising the nanoparticles. Specifically, the reconstituted high-density lipoprotein nanoparticles comprising cholesterol according to the present invention have an excellent cell influx rate and promote cholesterol efflux from cells, thus having a cancer cell killing effect, and can therefore be used for preventing or treating cancer.