Propolis-Cyclodextrin Inclusion Complex for Gastrointestinal Cancer Therapy

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Solution Overview

Problem

Current treatments for gastrointestinal cancers, such as colorectal, gastric, and throat cancers, are limited in effectiveness, with chemotherapy and radiotherapy often causing significant side effects and resistance issues, necessitating the development of more effective prevention and treatment compositions.

Innovation Solution

A composition comprising an inclusion complex of propolis and gamma-cyclodextrin, which can inhibit gastrointestinal tumour formation, growth, and metastasis, induce apoptosis in neoplastic cells, and enhance the responsiveness of cancer cells to therapy, thereby addressing resistance and improving treatment outcomes.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If chemotherapy and radiotherapy are used to treat gastrointestinal cancers, then cancer treatment is provided, but significant side effects and resistance issues occur

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidside effects and resistance
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent uses cyclodextrin as an intermediary substance that forms inclusion complexes with propolis compounds. This complex acts as a mediator to deliver anti-cancer agents more effectively to cancer cells while reducing harmful side effects. The cyclodextrin-propolis complex enhances the bioavailability and targeted delivery of active compounds like caffeic acid phenethyl ester (CAPE), thereby improving treatment reliability while mitigating harmful effects.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent creates a composite material system combining cyclodextrin and propolis extracts. This composite formulation integrates the beneficial properties of both substances: cyclodextrin provides enhanced solubility and delivery capabilities, while propolis contributes multiple anti-cancer active compounds. The composite structure enables synergistic effects that improve treatment effectiveness and reduce resistance development compared to conventional single-agent chemotherapy.

Inventive Principle:
Principle #40Composite materials

2Reliability

If conventional chemotherapies are used, then cancer cells are treated, but treatment resistance develops

Engineering Contradiction:
Improveanti-cancer activityVSAvoidtherapy responsiveness
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent modifies key parameters of propolis extraction and formulation by using cyclodextrin inclusion complexes. This changes the physical and chemical parameters of the active compounds, improving their bioavailability and cellular uptake. The complexed form of CAPE and other propolis compounds enters cancer cells more effectively, reversing or preventing treatment resistance and restoring therapy responsiveness.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The cyclodextrin-propolis composite system provides multi-functional anti-cancer activity that can address multiple resistance mechanisms simultaneously. The formulation contains multiple active compounds from propolis that work together to inhibit cancer cell proliferation, induce apoptosis, and reverse resistance to conventional chemotherapies. This universal approach makes the treatment effective across different cancer types and resistance profiles.

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 propolis-cyclodextrin composition demonstrates enhanced anti-gastrointestinal cancer activity, including increased sensitivity to therapy and prolonged maintenance of anti-cancer effects, potentially leading to improved treatment efficacy and reduced side effects.

Implementation Method 1

A composition comprising an inclusion complex of propolis and cyclodextrin

Methodology Applied
Scientific EffectInclusion complex formation:

Data Source

PatentEP2983681B1Therapeutic compositions and uses thereof
Publication Date: 2020.07.15 MANUKA HEALTH NEW ZEALAND LIMITED
  • EP2983681B1 patent drawingFigure 1A~1B
  • EP2983681B1 patent drawingFigure 2~3
  • EP2983681B1 patent drawing

AI summary

The invention provides pharmaceutical compositions, including anti-gastrointestinal cancer compositions, containing propolis and cyclodextrin. Methods of using such compositions, in particular in the treatment or prevention of gastrointestinal cancers, and in the resenitisation of gastrointestinal cancers to therapy, are also provided.