Engineered Adipocytes for Targeted Anti-Cancer Prodrug Delivery

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Solution Overview

Problem

Current cancer therapies face challenges in effectively targeting the adipocyte microenvironment, which supports tumor growth by providing energy to cancer cells through lipolysis, and in achieving sustained release of anti-cancer therapeutics within the tumor tissue.

Innovation Solution

Engineered adipocytes are developed to encapsulate anti-cancer prodrugs, such as doxorubicin prodrug, conjugated with fatty acids like rumenic acid, using environmentally responsive linkers, and equipped with fatty-acid binding protein 4 (FABP4) for targeted delivery and sustained release within the tumor microenvironment.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional cancer therapies are used, then anti-cancer agents can be delivered to tumor tissue, but the therapies cannot effectively target the adipocyte microenvironment or achieve sustained release within the tumor

Engineering Contradiction:
Improvetargeting effectivenessVSAvoiddelivery system complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The engineered adipocytes utilize the tumor microenvironment's own lipolytic activity and fatty acid metabolism pathways to trigger therapeutic release. The system self-activates through endogenous enzymes and metabolic processes, eliminating the need for external triggers or complex control mechanisms while achieving targeted delivery to the adipocyte microenvironment

Inventive Principle:
Principle #25Self-service

Solution Approach 2:

The patent employs environmentally responsive linkers that change their chemical state in response to specific parameters in the tumor microenvironment, such as pH changes, enzymatic activity, or redox conditions. This allows the delivery system to remain stable during circulation but automatically activate and release the therapeutic payload when encountering the unique biochemical parameters of the tumor adipocyte microenvironment

Inventive Principle:
Principle #35Parameter changes

2Reliability

If anti-cancer agents are delivered systemically, then broad coverage is achieved, but side effects increase and sustained release at the tumor site is not achieved

Engineering Contradiction:
Improvesustained release capabilityVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The engineered adipocytes act as intermediary carriers that transport the therapeutic payload from the bloodstream to the tumor adipocyte microenvironment. These living cells serve as a bridge between systemic administration and localized delivery, protecting the therapeutic during circulation and releasing it only at the target site through interactions with tumor-associated macrophages and lipolytic enzymes

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent extracts and utilizes specific components of the tumor microenvironment, such as lipolytic enzymes and fatty acid metabolism pathways, to trigger therapeutic release. By harnessing these endogenous tumor-specific processes, the system achieves localized sustained release without requiring systemic administration, thereby minimizing exposure of healthy tissues to the therapeutic agent

Inventive Principle:
Principle #2Taking out (Extraction)

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 engineered adipocytes effectively inhibit cancer cell growth, suppress tumor-promoting adipokines, and enhance immune cell infiltration, leading to significant tumor growth inhibition and reduced recurrence, while minimizing side effects through targeted and sustained delivery of anti-cancer agents.

Implementation Method 1

the prodrug can be conjugated to the conjugated fatty acid via an environmentally reactive linker (such as, for example, a pH sensitive, enzymatic, and/or reactive oxygen species responsive linker)

Methodology Applied
Scientific EffectpH-sensitive bond cleavage: Hydrolysis

Implementation Method 2

the prodrug can be conjugated to the conjugated fatty acid via an environmentally reactive linker (such as, for example, a pH sensitive, enzymatic, and/or reactive oxygen species responsive linker)

Methodology Applied
Scientific EffectEnzymatic reaction: Enzyme

Implementation Method 3

adipocytes further comprising a lipid transport protein (such as, for example) fatty-acid binding protein 4 (FABP4)

Methodology Applied
Scientific EffectFatty acid binding: Absorption (physical)

Data Source

PatentEP3873504B1Adipocyte mediated delivery of anticancer therapeutics
Publication Date: 2023.12.13 NORTH CAROLINA STATE UNIV
  • EP3873504B1 patent drawingFigure 1A~1K
  • EP3873504B1 patent drawingFigure 2A~2L
  • EP3873504B1 patent drawingFigure 3A~3F

AI summary

Disclosed are compositions and methods related to the use of adipocytes for sustained release of anti-cancer therapeutics and treatment of cancer.