Oral Micellar Composition for Large Molecule Delivery
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Solution Overview
Problem
Current oral formulations for large therapeutic molecules like proteins and cannabinoids face challenges such as poor permeability, enzymatic degradation, rapid clearance, and chemical instability in the gastrointestinal tract, with few effective penetration enhancers available due to safety concerns and unpleasant taste.
Innovation Solution
A novel orally administrable composition combining a physiologically acceptable film-forming agent with a therapeutic molecule encapsulated in a micellar composition, comprising micelle-forming compounds, alkali metal salicylate, and pharmaceutically acceptable edetate, which forms nanosized micelles for enhanced absorption.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If penetration enhancers are used to facilitate mucosal administration of large molecule drugs, then permeability is improved, but safety profile deteriorates due to lowering of mucosal barrier function, impairment of mucociliary clearance protective mechanism, and irritant properties
Solution Approach 1:
The patent uses a penetration enhancer delivery system that acts as an intermediary carrier to transport the enhancer through the mucosa. The enhancer is delivered in a controlled manner that allows it to facilitate drug permeability while being removed after serving its purpose, thus avoiding long-term safety issues associated with conventional enhancers that remain in the system and cause mucosal damage
Solution Approach 2:
The patent changes the physical and chemical parameters of the penetration enhancer by formulating it in a specific delivery system with controlled concentration, solubility, and release characteristics. This allows the enhancer to function effectively at lower concentrations for shorter durations, improving safety while maintaining permeability enhancement benefits
2Stability of the object's composition
If penetration enhancers are used to facilitate mucosal administration of large molecule drugs, then permeability is improved, but ease of operation deteriorates due to extremely bitter and unpleasant taste
Solution Approach 1:
The patent introduces a taste-masking agent as an intermediary substance that interacts with the bitter penetration enhancer. This agent binds to the enhancer or forms a complex that prevents direct contact with taste receptors, thereby eliminating the unpleasant taste while allowing the enhancer to maintain its permeability-enhancing function
Solution Approach 2:
The patent creates a composite formulation combining the penetration enhancer with taste-masking agents and other excipients in specific ratios and configurations. This composite material achieves both the desired permeability enhancement and acceptable taste profile, resolving the contradiction between functionality and ease of administration
3Reliability
If molecular size increases, then therapeutic efficacy is improved for large molecule drugs, but permeability deteriorates as molecules cross the mucosa less readily
Solution Approach 1:
The patent employs a penetration enhancer as an intermediary substance that temporarily interacts with the large therapeutic molecule or the mucosal membrane. This interaction creates a facilitated transport pathway that allows large molecules to permeate the mucosa effectively, overcoming the size-related permeability barrier while maintaining therapeutic efficacy
Solution Approach 2:
The patent changes the effective size or conformation of the large therapeutic molecule through complexation with the penetration enhancer or formulation components. This parameter change allows the molecule to permeate more readily while retaining its biological activity and therapeutic effect
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 enables effective oral delivery of large therapeutic molecules by enhancing permeability and stability, allowing for rapid absorption and prolonged delivery, while maintaining a satisfactory safety profile and acceptable taste.
Implementation Method 1
a micelle-forming compound in an aqueous solvent... the therapeutic molecule encapsulated in a micellar composition... forms nanosized micelles for enhanced absorption
Implementation Method 2
at least one physiologically acceptable film forming agent combined with the therapeutic molecule... forming a film on the mucosal membrane
Implementation Method 3
drugs administered through these membranes have a rapid onset of action... providing for easy absorption... rapid absorption
Data Source
AI summary
An orally administrable micellar composition is provided. The composition comprises a pharmaceutical agent encapsulated in micelles formed by at least one micelle-forming compound in a pharmaceutically acceptable aqueous solvent comprising an alkali metal salicylate and a pharmaceutically acceptable edetate combined with at least one physiologically acceptable film forming agent.