Nitric Oxide-Releasing Topical Composition with Dual-Phase Stability
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Solution Overview
Problem
Moisture-sensitive active pharmaceutical ingredients (APIs) face challenges in topical delivery, as stability in hydrophobic compositions reduces their effectiveness when moisture is the activating agent.
Innovation Solution
A topical pharmaceutical composition comprising a nitric oxide-releasing API in admixture with a hydrophilic and hydrophobic composition, buffered to a pH of 3 to 9, to enhance stability and release, and a method of applying this admixture to the skin to increase nitric oxide release.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If a nitric oxide-releasing API is incorporated in a hydrophobic topical composition to improve shelf life stability, then storage stability is improved, but the ability to deliver the drug is reduced when moisture is the activating agent
Solution Approach 1:
The invention divides the topical composition into two separate phases: a hydrophobic composition containing the nitric oxide-releasing API and a hydrophilic composition containing moisture. These phases are kept separate in the container but are designed to mix upon application to the skin, allowing the API to remain stable during storage while enabling effective drug delivery when activated by moisture from the hydrophilic phase.
Solution Approach 2:
The invention introduces an emulsifying agent as an intermediary substance that facilitates the interaction between the hydrophobic and hydrophilic compositions. The emulsifying agent enables the two phases to mix properly upon application, allowing the moisture from the hydrophilic phase to activate the nitric oxide-releasing API from the hydrophobic phase, thus resolving the contradiction between stability and delivery.
2Stability of the object's composition
If a hydrophobic composition is used to deliver nitric oxide-releasing API, then API stability is improved, but the rate of nitric oxide release is reduced
Solution Approach 1:
The invention creates a dynamic system where the composition transitions from a stable, separate-phase state during storage to an active, mixed state upon application. The hydrophobic and hydrophilic phases are designed to mix when applied to the skin, dynamically changing the environment from stable (during storage) to reactive (during use), thereby controlling both API stability and nitric oxide release rate at different stages.
Solution Approach 2:
The invention utilizes parameter changes in pH and moisture content to control the release rate. The hydrophilic composition provides moisture and a specific pH environment that triggers the nitric oxide-releasing API to activate. By controlling the pH and moisture parameters in the hydrophilic phase, the invention can regulate the rate of nitric oxide release while maintaining API stability in the hydrophobic phase during storage.
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 provides increased nitric oxide release and antimicrobial activity, promoting wound healing and sustained therapeutic effects.
Implementation Method 1
The hydrophilic composition may be configured to modulate a release of an active pharmaceutical ingredient in the hydrophobic composition by adjusting a pH
Implementation Method 2
at least one of an amphiphilic compound or an emulsifying agent
Data Source
AI summary
The present invention generally relates to topical compositions and methods of using the same. A preferred topical pharmaceutical composition comprises a nitric oxide-releasing active pharmaceutical ingredient in admixture with a hydrophilic composition and a hydrophobic composition wherein the nitric oxide-releasing active pharmaceutical ingredient comprises a nitric oxide-releasing compound having a diazeniumdiolate functional group.