Liposomal Cannabinoid Formulation for Prolonged Release
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Solution Overview
Problem
Current liposomal cannabinoid formulations face challenges in achieving prolonged and controlled release of cannabinoids, particularly cannabidiol (CBD), due to rapid release rates and low solubility in aqueous solutions, which limits their therapeutic efficacy and duration of action.
Innovation Solution
The development of liposomal formulations comprising a lipid membrane and an intraliposomal aqueous core, where CBD is entrapped with a dispersing agent such as human serum albumin (HSA) or polyethylene glycol (PEG), and optionally cyclodextrin (CD), to slow down the release of CBD, achieving a mole ratio between CBD and liposome-forming lipids within a specific range (1:10) for controlled release.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If cannabinoids are formulated in liposomes for therapeutic delivery, then solubility and delivery efficiency are improved, but release rate becomes too rapid to maintain therapeutic levels
Solution Approach 1:
The patent modifies the liposome formulation by incorporating specific dispersing agents (human serum albumin, polyethylene glycol, cyclodextrins) and adjusting the molar ratio of cannabinoid to phospholipid to achieve optimal controlled release. These parameter changes transform the release profile from rapid to prolonged, maintaining therapeutic levels for extended periods while preserving solubility benefits.
2Productivity
If cannabinoids are entrapped in liposome lipid membrane, then delivery efficiency is improved, but release control becomes difficult
Solution Approach 1:
The patent introduces dispersing agents (human serum albumin, polyethylene glycol, cyclodextrins) as intermediary substances that mediate between the liposome membrane and the cannabinoid. These intermediaries provide controlled release mechanisms while maintaining the high delivery efficiency of liposomal entrapment, effectively solving the release control difficulty.
3Duration of action of moving object
If dispersing agents are added to liposomal formulation, then release rate is reduced for prolonged action, but formulation complexity increases
Solution Approach 1:
The patent achieves prolonged therapeutic action by optimizing specific parameters of the liposomal formulation, including the molar ratio of cannabinoid to phospholipid and the concentration of dispersing agents. By carefully controlling these parameters, the patent extends duration of action while minimizing formulation complexity through standardized preparation methods.
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
This approach results in a prolonged release profile of CBD, maintaining therapeutic levels for several days to weeks, enhancing the therapeutic efficacy by sustaining CBD delivery and reducing the frequency of administration.
Implementation Method 1
the liposome comprises one or more liposome forming lipids, an entrapped cannabinoid
Implementation Method 2
at least one dispersing agent of a cannabinoid that is not a cyclodextrin (CD) compound
Data Source
AI summary
The present disclosure provides prolonged release formulation of cannabinoids. The formulation comprises liposomes having a lipid membrane and an intraliposomal aqueous core, wherein said liposome comprises either an entrapped cannabinoid and at least one dispersing agent of said cannabinoid, said dispersing agent being other than a cyclodextrin (CD) compound; or an entrapped cannabinoid, at least a portion of said cannabinoid being entrapped in said lipid membrane, and wherein said lipid membrane comprises a mole ratio between said cannabinoid and said one or more liposome forming lipids in the range of 1 to 10. Also disclosed are methods of preparing and uses of the formulations for prolonged delivery of the cannabinoids and therapeutic treatments making use of same.