Anhydrous Topical Formulations for Bioactive Delivery
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Solution Overview
Problem
Current topical delivery methods for bioactive agents face challenges in achieving efficient percutaneous absorption of high concentrations without skin irritation, particularly for hydrophobic substances and those that are prone to degradation in aqueous environments.
Innovation Solution
Anhydrous formulations comprising a carrier medium, high concentrations of micronized bioactive substances, and an exfoliant, which are free of occlusive agents, enhance absorption by maintaining stability and utilizing penetration enhancers to reduce diffusional resistance in the stratum corneum.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Productivity
If low pH formulations or derivatized compounds are used to improve percutaneous absorption, then absorption efficiency is improved, but skin irritation increases or bioconversion to active compound decreases
Solution Approach 1:
The patent changes the physical state parameter from aqueous to anhydrous formulation, enabling high concentrations of non-derivatized bioactive substances to be delivered without the skin irritation caused by low pH formulations. The anhydrous carrier medium allows the bioactive substance to remain in its active, non-derivatized form while achieving efficient percutaneous absorption.
2Quantity of substance
If high concentrations of bioactive substances are delivered topically, then therapeutic effectiveness is improved, but formulation stability decreases and skin irritation increases
Solution Approach 1:
The patent changes the solvent system from aqueous to anhydrous, which stabilizes high concentrations of bioactive substances by preventing degradation that occurs in aqueous environments. This parameter change allows high concentrations to be maintained without compromising formulation stability.
3Ease of manufacture
If aqueous formulations are used, then ease of preparation is improved, but hydrophobic bioactive substances cannot be effectively delivered
Solution Approach 1:
The patent changes the formulation medium from aqueous to anhydrous, which fundamentally alters the solubility parameters to accommodate hydrophobic bioactive substances. This parameter change enables the effective delivery of hydrophobic compounds while maintaining ease of preparation through straightforward mixing of the anhydrous carrier medium with the bioactive substance.
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
These formulations allow for non-irritating, efficient delivery of high concentrations of bioactive substances, increasing absorption rates and stability, while exfoliating the skin to enhance penetration and prevent degradation, thereby effectively treating dermatologic conditions and introducing substances into the bloodstream.
Implementation Method 1
anhydrous formulations comprising a carrier medium, high concentrations of micronized bioactive substances, and an exfoliant, which are free of occlusive agents, enhance absorption by maintaining stability and utilizing penetration enhancers to reduce diffusional resistance in the stratum corneum
Implementation Method 2
efficient delivery of high concentrations of bioactive substances, increasing absorption rates and stability, while exfoliating the skin to enhance penetration and prevent degradation, thereby effectively treating dermatologic conditions and introducing substances into the bloodstream
Data Source
AI summary
The invention relates to topical delivery of bioactive agents. More particularly, the invention relates to anhydrous formulations for percutaneous absorption. The invention provides formulations that allow efficient topical delivery of high concentrations of bioactive substances for percutaneous absorption. The formulations according to the invention are generally non-irritating to the skin.