Nanostructured Oral Formulations for High-Loading Bioavailability
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Solution Overview
Problem
Existing treatments for glycogen storage diseases and neurodegenerative disorders face challenges in achieving effective oral delivery of active compounds with high bioavailability and tolerability.
Innovation Solution
Formulations are developed that stabilize active compounds in a water-less nanostructured formulation, using a combination of hydrophilic surfactants, co-surfactants, and solvents to form nanostructures that disperse in aqueous fluids, allowing for high loading and sustained release of the active compounds.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If conventional oral formulations are used, then administration is simple, but bioavailability and effective loading of active compounds are insufficient
Solution Approach 1:
The patent changes the physical and chemical parameters of the formulation by using a water-less system with specific surfactant combinations (hydrophilic surfactant, co-surfactant, and solvent) to create nanostructures that can load high concentrations of lipophilic active compounds while maintaining stability and enabling sustained release in aqueous physiological environments
Solution Approach 2:
The formulation employs a composite system combining multiple components: hydrophilic surfactant (e.g., polysorbate), co-surfactant (e.g., polyethylene glycol), and solvent (e.g., ethanol) that work together to form stable nanostructures capable of encapsulating and delivering lipophilic active compounds with improved bioavailability
2Quantity of substance
If high loading of lipophilic active compounds is achieved, then quantity of active compound increases, but stability in aqueous environments deteriorates
Solution Approach 1:
The patent uses surfactants and co-surfactants as intermediary substances that form a protective interface between the lipophilic active compound and the aqueous environment, enabling high loading of hydrophobic compounds while maintaining stability through the formation of stable nanostructures with controlled surface properties
Solution Approach 2:
The formulation achieves stability by changing the physical state to water-less and using specific ratios of surfactant to solvent (e.g., 1:2 to 1:5 weight ratios) that optimize the balance between loading capacity and stability, preventing precipitation or aggregation when exposed to aqueous physiological fluids
3Duration of action of moving object
If sustained release is implemented, then duration of action increases, but complexity of formulation increases
Solution Approach 1:
The formulation achieves sustained release through self-service mechanisms where the nanostructures automatically release the active compound over time in response to physiological conditions (aqueous environment, pH, enzymes) without requiring external control systems or complex release mechanisms, simply by incorporating the right combination of surfactants and solvents
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 formulations enable increased loading and improved bioavailability of active compounds, maintaining stability and tolerability, facilitating effective oral delivery for treating glycogen storage diseases and neurodegenerative disorders.
Implementation Method 1
The formulations are formulated to stabilize the active compound in a water-less nanostructured formulation, while permitting full dilutability within aqueous liquids
Implementation Method 2
once orally administered, the formulations homogenously disperse in the aqueous phase (e.g. stomach fluids), to form dispersed nanostructures in which the active compound is captured and stabilized
Implementation Method 3
once orally administered, the formulations homogenously disperse in the aqueous phase (e.g. stomach fluids), to form dispersed nanostructures
Implementation Method 4
release of the active compound from the nanostructures to ensure delivery of high effective doses of the active compound over time
Data Source
AI summary
The present disclosure concerns formulations for oral delivery of at least one active agent of a compound according to formula (I) and/or (II) for the treatment of glycogen storage diseases, neurodegenerative disorders and autophagy-related conditions. The formulations are nano-structured formulations for increasing the bioavailability of the active agent after administration.