Transdermal Delivery via Nitric Oxide Generation
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Solution Overview
Problem
Conventional topical delivery systems face limitations in penetrating substances through the skin due to the skin's barrier properties, particularly for ionic and high-molecular-weight drugs, and struggle to deliver local anaesthetics effectively across intact skin.
Innovation Solution
A transdermal delivery system comprising a layer containing nitrite and a hydrogel with hydrogen ions, where the hydrogel provides an acidic environment to produce nitric oxide, facilitating the diffusion of both nitric oxide and pharmaceutically active agents through the skin.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Device complexity
If conventional topical delivery systems are used, then the system structure is simple, but the penetration of substances through the skin is limited due to the stratum corneum barrier
Solution Approach 1:
The patent introduces nitric oxide as an intermediary substance that facilitates drug penetration through the stratum corneum barrier. The nitric oxide generating system acts as a mediator between the conventional topical delivery system and the skin barrier, enabling substances that would normally be blocked to penetrate effectively through the skin.
2Ease of manufacture
If conventional topical delivery systems are used, then the system is easy to manufacture, but it is difficult to deliver ionic and high-molecular-weight drugs in therapeutically sufficient amounts
Solution Approach 1:
Nitric oxide serves as a mediator that enhances the delivery of ionic and high-molecular-weight drugs through the skin barrier. This intermediary mechanism allows conventional topical systems to deliver therapeutically sufficient amounts of drugs that would otherwise be blocked by the stratum corneum, without complicating the manufacturing process.
Solution Approach 2:
The patent utilizes changes in pH parameters to trigger nitric oxide release from nitrite precursors. By incorporating acidifying agents that lower pH at the application site, the system activates nitric oxide generation, which in turn enhances drug penetration and delivery to therapeutically effective levels.
3Ease of operation
If conventional topical delivery systems are used, then the system is simple to operate, but local anaesthetics do not readily penetrate intact skin
Solution Approach 1:
Nitric oxide acts as an intermediary that facilitates the penetration of local anaesthetics through intact skin. The nitric oxide generating system is applied simultaneously with or before the anaesthetic, creating a transient increase in skin permeability that allows the anaesthetic to penetrate effectively without requiring complex application procedures.
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
This system enables the controlled and efficient transdermal delivery of a wide range of pharmaceutically active agents, including anaesthetics, by mimicking the body's endogenous nitric oxide generation mechanism, improving local anaesthesia and reducing pain during procedures like venepuncture and bloodletting.
Implementation Method 1
a hydrogel that contains hydrogen ions; wherein the layer containing a nitrite and/or the hydrogel comprises a pharmaceutically active agent
Implementation Method 2
a system that mimics this endogenous mechanism of NO generation, using inorganic nitrite and an organic acid to produce NO on the skin surface
Implementation Method 3
a barrier consisting of a membrane to allow diffusion of the pharmaceutically active agent and nitrite ions
Data Source
AI summary
The present invention provides a system comprising: (i) a layer containing a nitrite; and (ii) a hydrogel that contains hydrogen ions; wherein the layer containing a nitrite and/or the hydrogel comprises a pharmaceutically active agent. The invention also provides the use of a system of the invention in medicine, and in the treatment of pain.