Lipid Matrix Solubility via Polyhydroxy Components
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Solution Overview
Problem
Existing lipid-based controlled-release formulations face limitations in solubility, particularly for peptides and proteins, leading to restricted duration of active agent release due to low solubility and potential discomfort for patients, and they often exhibit undesirable 'burst/lag' release profiles.
Innovation Solution
Incorporating a polyhydroxy component, such as sugars, into the lipid-based controlled-release matrix to enhance the solubility of bioactive agents, allowing for a higher loading capacity and stable, sustained release without initial burst release.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If a polyhydroxy component is incorporated into the lipid-based controlled-release matrix, then the solubility of bioactive agents is significantly increased, but the formulation complexity increases
Solution Approach 1:
The patent combines lipid-based controlled-release matrix components with polyhydroxy components (such as sugars) to create a composite formulation system. This composite approach enables the lipid matrix to accommodate higher concentrations of bioactive agents while maintaining controlled-release properties, directly resolving the solubility limitation without requiring complete reformulation of the entire system
2Duration of action of moving object
If the loading capacity of bioactive agents is increased, then the duration of release is extended, but initial burst release occurs causing peak concentrations
Solution Approach 1:
The patent modifies the physical and chemical parameters of the lipid-based matrix by incorporating polyhydroxy components, which alter the matrix structure and release kinetics. This parameter change enables sustained release of bioactive agents over extended periods while preventing initial burst release, as the modified matrix structure controls the diffusion and degradation rates more uniformly
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 polyhydroxy component significantly increases the solubility of bioactive agents within the lipid matrix, enabling longer and more stable release profiles without initial peak concentrations, thus providing a more effective and comfortable delivery method.
Implementation Method 1
Incorporating a polyhydroxy component, such as sugars, into the lipid-based controlled-release matrix to enhance the solubility of bioactive agents
Implementation Method 2
formulations which undergo at least one phase transition upon exposure to aqueous fluids, such as body fluids, thereby forming a controlled release matrix
Data Source
AI summary
The present invention relates to formulations of a lipid based controlled-release matrix, a polyhydroxy component and a bioactive agent. Such formulation are useful in the delivery of the bioactive compounds. The invention also relates to the use of a polyhydroxy component for increasing the solubility of a bioactive compound, especially a peptide in a lipid-based controlled-release matrix.