PEG-PLGA Cannabinoid Composition for Intranasal Brain Delivery
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Solution Overview
Problem
Existing cannabinoid formulations, such as dronabinol and Sativex, suffer from poor storage stability, low water solubility, and rapid conversion to psychoactive metabolites, making them ineffective for targeted delivery to the brain and treatment of neurological conditions like Alzheimer's disease.
Innovation Solution
A pharmaceutical composition comprising a cannabinoid encapsulated by an amphiphilic copolymer, specifically polyethylene glycol (PEG) and polylactic-co-glycolic acid (PLGA), which is suitable for intranasal or inhalation delivery, providing improved stability and solubility, reducing first-pass metabolism, and minimizing psychoactive metabolites.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If cannabinoids are administered via conventional routes (oral, sublingual, inhalation), then they can be delivered to the patient, but they undergo first-pass metabolism and extensive first-pass extraction by the lungs, reducing bioavailability
Solution Approach 1:
The patent uses the nasal mucosa as an intermediary absorption route that bypasses the gastrointestinal tract and liver metabolism. The composition delivers cannabinoids directly through the nasal epithelium into the systemic circulation, avoiding first-pass metabolism and lung extraction, thereby significantly improving bioavailability and reducing substance loss.
2Speed
If cannabinoids are delivered via conventional routes, then administration is possible, but the onset of action is delayed
Solution Approach 1:
The patent extracts cannabinoids from the gastrointestinal absorption pathway and delivers them directly through the nasal route. This bypasses the slow digestive and metabolic processes, enabling rapid absorption through the highly vascularized nasal mucosa and achieving fast onset of action within minutes.
3Stability of the object's composition
If conventional cannabinoid compositions are used, then they can be formulated, but they lack optimal stability and patient compliance characteristics
Solution Approach 1:
The patent employs a composite formulation system consisting of cannabinoids dissolved or suspended in a carrier liquid containing specific excipients. This composite structure provides optimal stability by protecting cannabinoids from degradation while maintaining solubility and enabling controlled delivery through the nasal route.
Solution Approach 2:
The patent optimizes formulation parameters including pH, osmolarity, viscosity, and excipient selection to enhance composition stability. By carefully controlling these parameters, the formulation maintains cannabinoid stability, prevents precipitation or degradation, and ensures consistent delivery while remaining easy to manufacture.
4Ease of operation
If cannabinoids are administered orally or sublingually, then delivery is achieved, but patient compliance is suboptimal due to taste and convenience issues
Solution Approach 1:
The patent uses the nasal cavity as an intermediary route that avoids the gastrointestinal tract and oral cavity. This eliminates unpleasant tastes associated with oral and sublingual administration while providing a convenient, non-invasive delivery method that improves patient compliance through ease of use and acceptable sensory experience.
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 effectively targets the brain with a consistent dose of cannabinoids, bypassing liver metabolism and reducing psychoactive effects, while maintaining stability at room temperature, suitable for treating neurological conditions.
Implementation Method 1
Cannabinoids can be delivered to a patient by a route that bypasses the gastrointestinal tract and liver metabolism, such as by intranasal or subcutaneous injection
Implementation Method 2
Other methods of administration include vaporization of a cannabis material
Data Source
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AI summary
The present invention provides pharmaceutical compositions and methods for use and manufacture thereof. The pharmaceutical compositions comprise a therapeutically effective amount of a cannabinoid or a pharmaceutically acceptable salt or solvate thereof and an amphiphilic copolymer comprising at least one hydrophilic component and at least one hydrophobic component. The cannabinoid is encapsulated in the amphiphilic copolymer, and the composition is suitable for intranasal or inhalation delivery.