Cannabinoid Encapsulation with Alginate and Permeation Enhancer

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Solution Overview

Problem

Current cannabinoid therapies face challenges such as low oral bioavailability, high volatility, and instability, which limit their effectiveness and cost-effectiveness for treating neurological conditions, particularly due to the lipophilic nature of CBD and its sensitivity to light and degradation in the duodenum.

Innovation Solution

A composition comprising encapsulated cannabinoids and a permeation enhancer, such as deoxycholic acid, combined with an alginate polymer, which enhances brain uptake and stability, forming encapsulated particles that protect against degradation and improve delivery across the blood-brain barrier.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If CBD is administered orally, then it can be used for treatment, but its oral bioavailability is extremely low due to degradation in the duodenum

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidoral bioavailability
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The invention segments the delivery system by using multiple encapsulation layers (outer shell and inner core) to protect CBD at different stages of digestion. The outer shell contains enzymes like lipase and protease that prevent CBD degradation in the duodenum, while the inner core maintains CBD stability, enabling effective oral administration despite digestive breakdown

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention introduces enzymatic intermediaries (lipase and protease) within the encapsulation structure that actively prevent CBD degradation. These enzymes serve as mediators between the harsh duodenal environment and the sensitive CBD compound, protecting it from breakdown while allowing controlled release

Inventive Principle:
Principle #24Intermediary (Mediator)

2Adaptability or versatility

If CBD is used therapeutically, then neurological conditions can be treated, but its high volatility and instability limit research and clinical adaptation

Engineering Contradiction:
Improveclinical adaptabilityVSAvoidcompound stability
Core Design Contradiction:
Adaptability or versatilityVSStability of the object's composition

Solution Approach 1:

The invention provides beforehand cushioning by pre-encapsulating CBD in a protective structure containing stabilizing enzymes and antioxidants before exposure to degrading conditions. This prior protection prevents volatility and instability issues during storage, handling, and administration, enabling reliable clinical and research use

Inventive Principle:
Principle #11Beforehand cushioning (Prior cushioning)

Solution Approach 2:

The invention uses composite materials combining CBD with stabilizing enzymes (lipase, protease), antioxidants, and encapsulation polymers in a multi-layer structure. This composite approach enhances CBD stability while maintaining therapeutic activity, overcoming the limitations of pure CBD formulations

Inventive Principle:
Principle #40Composite materials

3Reliability

If high doses of CBD are administered to overcome low bioavailability, then treatment effectiveness may improve, but the cost becomes prohibitive

Engineering Contradiction:
Improvetreatment effectivenessVSAvoiddosage cost
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The invention changes the delivery parameters by modifying how CBD is presented to the digestive system through encapsulation. This transforms the bioavailability parameter from extremely low to significantly improved, allowing effective treatment at lower, more affordable doses rather than requiring high costly doses

Inventive Principle:
Principle #35Parameter changes

4Ease of operation

If CBD is exposed to light and air during storage and administration, then it can be easily stored and administered, but it degrades and loses efficacy

Engineering Contradiction:
Improvestorage convenienceVSAvoidcompound stability
Core Design Contradiction:
Ease of operationVSStability of the object's composition

Solution Approach 1:

The invention uses flexible encapsulation shells and thin film barriers that protect CBD from light and air exposure during storage and administration. These protective layers maintain compound stability while allowing the product to remain in convenient storage forms, balancing protection with ease of use

Inventive Principle:
Principle #30Flexible shells and thin films

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 encapsulated composition significantly enhances cannabinoid uptake and retention in the brain, providing a more stable and effective treatment option for neurological conditions, with increased bioavailability and prolonged retention, as demonstrated by enhanced pharmacokinetic parameters in animal studies.

Implementation Method 1

mixing an aqueous solution of the one or more cannabinoids and the alginate polymer to form an emulsion, then casting the emulsion into an aqueous solution of a multivalent salt to form an encapsulated cannabinoid particle

Methodology Applied
Scientific EffectEncapsulation:

Implementation Method 2

mixing an aqueous solution of the one or more cannabinoids and the alginate polymer to form an emulsion

Methodology Applied
Scientific EffectEmulsion: Emulsion

Implementation Method 3

a permeation enhancer; wherein the one or more cannabinoids and permeation enhancer are encapsulated

Methodology Applied
Scientific EffectPermeation: Permeation

Data Source

PatentUS20230404944A1Cannabinoid encapsulation technology
Publication Date: 2023.12.21 ZELIRA THERAPEUTICS OPERATIONS PTY LTD
  • US20230404944A1 patent drawing
  • US20230404944A1 patent drawing
  • US20230404944A1 patent drawing

AI summary

The invention relates to a composition comprising one or more cannabinoids, a permeation enhancer, and an alginate polymer, wherein the one or more cannabinoids and permeation enhancer are encapsulated. Such compositions may be useful in the treatment of neurodegenerative disorders, where delivery of a cannabinoid to the brain is required.