Lipid-Based CBD Nanoparticles for Bioavailability

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Solution Overview

Problem

Current CBD delivery systems face challenges with impurities, variable quality, low bioavailability, and instability, particularly due to the use of CBD oils and lipophilic ingredients, which lead to unpredictable delivery and side effects.

Innovation Solution

A lipid-based particle composition comprising cannabidiol (CBD) with high purity, phosphatidylcholine, cholesterol, and medium chain triglycerides, formulated into nanoparticles with a size range of 75 nm to 200 nm, providing stability and enhanced bioavailability through a solubilizing particle delivery system.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If CBD oils and lipophilic ingredients are used in delivery systems, then the therapeutic agent can be delivered, but impurities and variable quality occur leading to unpredictable delivery and side effects

Engineering Contradiction:
Improvedelivery predictabilityVSAvoidimpurities and side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent extracts and removes impurities from CBD by using high-purity CBD isolate (≥98% pure) instead of CBD oils. This extraction principle eliminates the harmful impurities and variable quality components while retaining the therapeutic CBD compound, thereby improving delivery predictability and reducing side effects.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent changes the purity parameter of CBD from typical oil-based formulations to high-purity isolate (≥98%). This parameter change from impure to pure CBD fundamentally alters the quality and reliability of the delivery system, eliminating batch-to-batch variation and unpredictable delivery issues.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If conventional CBD formulations are used, then administration is simple, but bioavailability is low and stability is poor

Engineering Contradiction:
ImprovestabilityVSAvoidformulation complexity
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent uses composite lipid-based nanoparticles comprising phosphatidylcholine, cholesterol, and medium-chain triglycerides combined with high-purity CBD. This composite material approach creates a stable delivery system that protects CBD from degradation while enhancing bioavailability, achieving both stability and controlled delivery.

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The patent changes the physical state and size parameters by formulating CBD into nanoparticles with specific size ranges (75-200 nm Z-average). This parameter change from bulk material to nanoscale particles fundamentally improves stability, solubility, and bioavailability while maintaining formulation feasibility.

Inventive Principle:
Principle #35Parameter changes

3Productivity

If nanoparticle size is reduced to 75-200 nm, then bioavailability and absorption speed increase, but manufacturing precision requirements increase

Engineering Contradiction:
Improveabsorption speedVSAvoidparticle size control
Core Design Contradiction:
ProductivityVSManufacturing precision

Solution Approach 1:

The patent optimizes the particle size parameter to a specific range (75-200 nm Z-average) that maximizes bioavailability and absorption speed. This parameter optimization balances the benefits of small particle size with manufacturing feasibility, achieving rapid absorption without excessive manufacturing complexity.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent applies local quality control by specifying the Z-average size range (75-200 nm) rather than requiring uniform size for all particles. This local quality approach focuses control on the critical average size parameter that drives bioavailability while allowing natural size distribution variation, reducing manufacturing precision requirements.

Inventive Principle:
Principle #3Local quality

4Reliability

If high purity CBD (≥98%) is used, then batch-to-batch variation is reduced, but cost of materials increases

Engineering Contradiction:
Improvebatch-to-batch consistencyVSAvoidmaterial cost
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The patent extracts pure CBD from the cannabis plant material through sophisticated purification processes to achieve ≥98% purity. This extraction process removes all impurities and variable components, ensuring batch-to-batch consistency. The increased material cost is justified by the elimination of delivery failures and side effects associated with impure formulations.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent changes the purity parameter to ≥98%, which fundamentally improves batch-to-batch consistency and reliability. This parameter change eliminates the variability inherent in lower-purity formulations, ensuring predictable delivery and reducing the need for costly quality control and waste management.

Inventive Principle:
Principle #35Parameter changes

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 composition achieves higher bioavailability, faster absorption, improved stability, and reduced batch-to-batch variation, with increased Cmax and AUC, and decreased Tmax, while minimizing side effects and maintaining efficacy over long-term storage.

Implementation Method 1

A lipid-based particle composition comprising cannabidiol (CBD) with high purity, phosphatidylcholine, cholesterol, and medium chain triglycerides, formulated into nanoparticles with a size range of 75 nm to 200 nm, providing stability and enhanced bioavailability through a solubilizing particle delivery system.

Methodology Applied
Scientific EffectSolubilization: Solvation

Implementation Method 2

wherein the nanoparticles comprise liposomes and oil-in-water nano-emulsion particles

Methodology Applied
Scientific EffectEmulsion: Emulsion

Data Source

PatentEP3840730B1Compositions for the delivery of therapeutic agents and methods of use and making thereof
Publication Date: 2023.09.20 DISRUPTION LABS INC
  • EP3840730B1 patent drawingFigure 1~2
  • EP3840730B1 patent drawingFigure 3~4
  • EP3840730B1 patent drawingFigure 5A~5E

AI summary

Some embodiments pertain to nanoparticle-based compositions and their use in methods for the delivery of CBD to subjects. In some embodiments, the compositions are stable for prolonged periods of time and provide enhanced bioavailability.