Phospholipid Nanoparticles for Cannabinoid Bioavailability

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Solution Overview

Problem

Current methods of delivering cannabinoids, such as smoking, vaporization, and oral ingestion, face challenges with unreliable dosage, low bioavailability, and adverse effects due to poor solubility and first-pass metabolism, leading to inconsistent therapeutic outcomes and increased doses required for efficacy.

Innovation Solution

Phospholipid nanoparticle compositions encapsulating cannabinoids are formed through a unified sequential process, enhancing bioavailability 2- to 8-fold and reducing doses needed for therapeutic effects by 2- to 8-fold, while minimizing adverse effects through targeted delivery across hydrophobic mucosa and systemic circulation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If cannabinoids are delivered through conventional methods (smoking, vaporization, oral ingestion), then therapeutic effects can be achieved, but bioavailability is low and doses required are high

Engineering Contradiction:
Improvecannabinoid doseVSAvoidbioavailability
Core Design Contradiction:
Quantity of substanceVSReliability

Solution Approach 1:

The patent introduces phospholipid nanoparticles as an intermediary carrier system that encapsulates cannabinoids, facilitating their transport across biological barriers. The nanoparticles serve as a mediator between the hydrophobic cannabinoid molecules and the aqueous biological environment, enabling enhanced absorption and delivery to target sites while reducing the required dose.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention changes the physical and chemical parameters of cannabinoid delivery by encapsulating them in phospholipid nanoparticles with specific size ranges (20-200 nm). This parameter change transforms the delivery system from direct administration to nanoparticle-mediated delivery, improving solubility, stability, and bioavailability while reducing the quantity needed for therapeutic effect.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If higher doses of cannabinoids are administered to overcome low bioavailability, then therapeutic effects may be achieved, but adverse effects increase

Engineering Contradiction:
Improvetherapeutic effectVSAvoidadverse effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The phospholipid nanoparticle acts as a protective intermediary that delivers cannabinoids in a controlled manner, reducing the peak concentration and systemic exposure that lead to adverse effects. The nanoparticle carrier moderates the interaction between cannabinoids and biological systems, maintaining therapeutic efficacy while minimizing harmful impacts.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

By changing the delivery parameters through nanoparticle encapsulation, the invention achieves more predictable and controlled cannabinoid release. This results in sustained therapeutic effects at lower doses, avoiding the adverse effects associated with high-dose administration while maintaining reliable therapeutic outcomes.

Inventive Principle:
Principle #35Parameter changes

3Ease of manufacture

If cannabinoids are administered without encapsulation, then the delivery process is simple, but solubility is poor and first-pass metabolism reduces efficacy

Engineering Contradiction:
Improvedelivery processVSAvoidtherapeutic efficacy
Core Design Contradiction:
Ease of manufactureVSReliability

Solution Approach 1:

The phospholipid nanoparticle serves as an intermediary that solves the solubility problem of hydrophobic cannabinoids. The amphiphilic nature of phospholipids creates a stable interface between the hydrophobic cannabinoid core and the aqueous environment, enabling effective delivery while bypassing first-pass metabolism through alternative absorption pathways.

Inventive Principle:
Principle #24Intermediary (Mediator)

4Ease of operation

If conventional delivery methods are used, then administration is straightforward, but dosage precision is unreliable

Engineering Contradiction:
ImproveadministrationVSAvoiddosage precision
Core Design Contradiction:
Ease of operationVSManufacturing precision

Solution Approach 1:

The invention changes the physical parameters of the delivery system by standardizing nanoparticle size, composition, and encapsulation efficiency. This standardization enables precise control over the amount of cannabinoid delivered per unit of administration, achieving reliable dosage precision while maintaining ease of operation through various administration routes.

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 phospholipid nanoparticle compositions significantly increase cannabinoid bioavailability and therapeutic activity, reduce adverse effects, and enable more precise and effective cannabinoid therapy with standardized precision-metered dosages, facilitating safer and more efficacious long-term treatment.

Implementation Method 1

phospholipid nanoparticle compositions of cannabinoids formed from phospholipids and simpler lipids in an unfired sequential process that encapsulate a high concentration of cannabinoids

Methodology Applied
Scientific EffectSelf-assembly: Self-Assembly

Implementation Method 2

nanoparticle compositions encapsulating cannabinoids are formed through a unified sequential process, enhancing bioavailability 2- to 8-fold

Methodology Applied
Scientific EffectEncapsulation: Emulsion

Data Source

PatentUS10596124B2Lipid nanoparticle compositions and methods as carriers of cannabinoids in standardized precision-metered dosage forms
Publication Date: 2020.03.24 NANOSPHERE HEALTH SCI INC
  • US10596124B2 patent drawing
  • US10596124B2 patent drawing

AI summary

This disclosure teaches phospholipid nanoparticle compositions of cannabinoids formed from phospholipids and simpler lipids in an unfired sequential process that encapsulate a high concentration of cannabinoids, and create standardized precision-metered dosage forms of cannabinoids; yielding an increase cannabinoid transport across hydrophobic mucosa; increase the bioavailability of the cannabinoid 2-fold to 8-fold, decrease the dose of cannabinoids 2-fold to 8-fold less than an amount of cannabinoids needed to illicit the same therapeutic effect compared to raw and non-encapsulated cannabinoids; where the nanoparticle dynamic structure reduces the adverse effects of cannabinoids; and enable safe more efficacious cannabinoid therapy.