Topical Cannabinoid Composition with Penetration Enhancers

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Solution Overview

Problem

Current pain management therapies for musculoskeletal disorders, such as rheumatoid arthritis and osteoarthritis, have limited efficacy and are associated with significant side effects, and there is a need for improved topical formulations that can deliver active ingredients directly to deep tissues with reduced gastrointestinal, central nervous system, and cardiovascular side effects.

Innovation Solution

A topical cannabinoid composition comprising a cannabinoid (0.01-10% w/w), a humectant (0.01-10% w/w), a penetration enhancer (1-5% w/w), and water, with a glycol ether content of less than 10% w/w, which penetrates deep into the skin, enhancing the absorption of cannabinoids into the dermis and hypodermis layers, thereby providing therapeutic effects while minimizing systemic side effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional painkillers (NSAIDs, opiates) are administered to alleviate pain, then pain relief is achieved, but gastrointestinal damage, liver damage, tolerance, and addiction occur

Engineering Contradiction:
Improvepain relief efficacyVSAvoidgastrointestinal and liver damage, tolerance, addiction
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent uses topical cannabinoid compositions as an intermediary treatment approach. Instead of systemic administration of conventional painkillers that affect the entire body, the cannabinoids are applied topically to the affected area, acting as a localized mediator that provides pain relief through cannabinoid receptors in the skin and underlying tissues without causing systemic gastrointestinal or liver damage.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent extracts and isolates the pain-relieving properties of cannabinoids from the whole cannabis plant, creating purified topical formulations containing specific cannabinoids (CBD, THC, CBG, CBN) along with penetration enhancers and humectants. This extraction allows for targeted pain relief without the psychoactive effects or systemic side effects associated with oral cannabis use.

Inventive Principle:
Principle #2Taking out (Extraction)

2Object-affected harmful factors

If topical formulations are used to deliver active ingredients to deep tissues, then side effects are reduced, but penetration depth and absorption efficiency become limited

Engineering Contradiction:
Improvesystemic side effectsVSAvoidpenetration depth and absorption efficiency
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

The patent incorporates penetration enhancers (glycols, fatty acids, surfactants) as intermediary substances that facilitate the transfer of cannabinoids through the skin barrier. These enhancers temporarily modify the skin structure or interact with cannabinoid molecules to increase their permeability, allowing deeper penetration without increasing systemic absorption and associated side effects.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent modifies key parameters of the topical formulation including pH (adjusted to 3.5-7.5 to optimize skin penetration), viscosity (adjusted to 10-10,000 cP for proper application and retention), and composition (specific ratios of cannabinoids, humectants, and penetration enhancers). These parameter changes enhance penetration depth while maintaining safety and efficacy.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If high concentrations of penetration enhancers are used to improve cannabinoid absorption, then penetration depth increases, but formulation stability and safety may be compromised

Engineering Contradiction:
Improvepenetration depthVSAvoidformulation stability and safety
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent optimizes the concentration of penetration enhancers within specific ranges (glycols at 1-10%, fatty acids at 0.1-5%, surfactants at 0.1-5%) to achieve effective penetration while maintaining formulation stability. The pH is adjusted to 3.5-7.5 and viscosity to 10-10,000 cP, creating optimal conditions for both penetration and stability.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates composite topical formulations that combine multiple components (cannabinoids, humectants like glycerin and propylene glycol, penetration enhancers, emulsifiers, and preservatives) in specific ratios. This composite approach allows the formulation to achieve enhanced penetration through synergistic interactions while maintaining stability through balanced composition.

Inventive Principle:
Principle #40Composite materials

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 topical composition effectively delivers cannabinoids to deep tissues, reducing the frequency and severity of side effects associated with oral and systemic administration, providing effective pain relief for musculoskeletal disorders with improved stability and viscosity.

Implementation Method 1

a penetration enhancer (1-5% w/w), and water, with a glycol ether content of less than 10% w/w, which penetrates deep into the skin, enhancing the absorption of cannabinoids into the dermis and hypodermis layers

Methodology Applied
Scientific EffectTransdermal penetration: Permeation

Implementation Method 2

a humectant (0.01-10% w/w)

Methodology Applied
Scientific EffectHumectant action: Absorption (physical)

Data Source

PatentUS12064461B2Deep penetrating topical cannabinoid compositions and methods for treating musculoskeletal inflammation and pain
Publication Date: 2024.08.20 AVICANNA INC
  • US12064461B2 patent drawing
  • US12064461B2 patent drawing
  • US12064461B2 patent drawing

AI summary

Topical compositions comprising cannabinoids in combination with one or more humectants and one or more penetration enhancers are provided. Also provided are methods comprising applying a topical cannabinoid composition provided herein to the skin areas of a subject affected by inflammation and/or pain associated with musculoskeletal disease or condition and uses of a topical cannabinoid formulation provided herein for the treatment of inflammation and/or pain associated with musculoskeletal disease or condition in a subject.