Cannabinoid-Chemotherapy Complex for Blood-Brain Barrier Penetration

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Solution Overview

Problem

Current chemotherapy drugs for brain cancers face significant challenges in crossing the blood-brain barrier, leading to ineffective delivery and debilitating side effects, as most are too large to penetrate the barrier and are not designed to target central nervous system tumors effectively.

Innovation Solution

Chemically linking cannabinoids such as THC, CBD, or THCV with chemotherapy agents like Carmustine or Dacarbazine to create complexes that can cross the blood-brain barrier, where the cannabinoid assists in transport and subsequent release to bind with brain receptors, while the chemotherapy agent attacks cancer cells.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If chemotherapy agents are used to treat brain cancer, then therapeutic effect is improved, but the ability to cross the blood-brain barrier deteriorates because most chemotherapy drugs are too large to penetrate the barrier

Engineering Contradiction:
Improvetherapeutic effectVSAvoidblood-brain barrier penetration
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent uses cannabinoids as intermediary molecules to transport chemotherapy agents across the blood-brain barrier. The cannabinoid-chemotherapy complex allows the chemotherapy drug to hitchhike through the barrier by binding to the cannabinoid carrier, which has the ability to penetrate the barrier. This resolves the contradiction by introducing a mediator that bridges the gap between the chemotherapy agent and the barrier penetration requirement.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent creates composite molecules by chemically linking cannabinoids with chemotherapy agents. This composite structure combines the barrier-penetrating properties of cannabinoids with the therapeutic properties of chemotherapy drugs, allowing the resulting complex to both cross the blood-brain barrier and exert anti-cancer effects.

Inventive Principle:
Principle #40Composite materials

2Object-affected harmful factors

If small lipid-soluble molecules are used to cross the blood-brain barrier by diffusion, then barrier penetration is improved, but the molecular size and lipid solubility requirements limit the choice of effective chemotherapy agents

Engineering Contradiction:
Improveblood-brain barrier penetrationVSAvoiddrug selection flexibility
Core Design Contradiction:
Object-affected harmful factorsVSAdaptability or versatility

Solution Approach 1:

Cannabinoids serve as intermediary carriers that enable large, water-soluble chemotherapy agents to cross the blood-brain barrier without needing to meet the restrictive size and lipid solubility requirements. The cannabinoid mediator handles the barrier penetration function, freeing the chemotherapy agent from these constraints and expanding drug selection flexibility.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The cannabinoid carrier provides a universal mechanism for transporting various chemotherapy agents across the blood-brain barrier. By using the same cannabinoid carrier system with different chemotherapy drugs, the patent achieves multi-functionality and broad applicability, resolving the limitation of drug selection flexibility.

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

3Object-affected harmful factors

If highly lipid-soluble compounds are used to increase transport across the blood-brain barrier, then barrier penetration is improved, but the amount of compound reaching the target brain tissue decreases due to sequestration by the capillary bed and peripheral tissues

Engineering Contradiction:
Improveblood-brain barrier penetrationVSAvoiddrug concentration at target
Core Design Contradiction:
Object-affected harmful factorsVSQuantity of substance

Solution Approach 1:

The cannabinoid-chemotherapy complex acts as a targeted delivery system where the cannabinoid mediator guides the chemotherapy agent specifically to the brain tissue. This targeted approach prevents non-specific sequestration by peripheral tissues and capillary beds, ensuring that the chemotherapy agent reaches the brain target in sufficient concentrations.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent employs local quality by using the cannabinoid carrier to deliver the chemotherapy agent specifically to the brain region where it is needed. The complex exhibits different behavior in different locations: it penetrates the blood-brain barrier efficiently and releases the chemotherapy agent specifically in the brain tissue, rather than being distributed systemically and sequestered elsewhere.

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

This approach enables the delivery of chemotherapy agents across the blood-brain barrier, providing therapeutic effects for brain cancer while alleviating chemotherapy-induced side effects like nausea and pain, by leveraging the natural ability of cannabinoids to penetrate the brain and bind with cannabinoid receptors.

Implementation Method 1

passage through the BBB does not ensure that a compound will be pharmacologically effective. After passing through the monolayer of endothelial cells forming the BBB

Methodology Applied
Scientific EffectPassive diffusion: Diffusion

Implementation Method 2

Once across the BBB, the cannabinoid will attach to cannabinoid receptors in the brain (thereby alleviating nausea and pain, and increasing appetite) and the chemotherapy agent will be released to attack cancer cells

Methodology Applied
Scientific EffectMetabolic cleavage: Decomposition (biological)

Data Source

PatentUS11298425B2Delivery of a chemotherapy agent across the blood-brain barrier
Publication Date: 2022.04.12 ROWLESBIOMED LLC
  • US11298425B2 patent drawing
  • US11298425B2 patent drawing
  • US11298425B2 patent drawing

AI summary

A therapeutic method and composition which includes a cannabinoid chemically linked to a chemotherapy agent. The therapeutic composition is capable of crossing the blood-brain barrier, and delivery of the composition across the blood-brain barrier provides both chemotherapy for the treatment of brain cancer and alleviation of side effects caused by the chemotherapy agent. Once across the blood-brain barrier, the chemotherapy agent will be released to attack cancer cells, and the cannabinoid will be free to bind to cannabinoid receptors in the brain to alleviate side effects of chemotherapy such as nausea/vomiting, pain and decreased appetite.