Transdermal Formulation for Sustained CD38 Reduction
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Solution Overview
Problem
Current therapeutic agents face challenges in achieving effective bioavailability and targeted delivery due to issues like low solubility, rapid elimination, and inability to reach therapeutic levels at specific sites, such as the lungs, joints, or endothelium.
Innovation Solution
A transdermal formulation comprising curcuminoids, senolytic flavonoids, and a polyol solvent, optionally with a fatty acid, designed for sustained delivery to reduce CD38 ectoenzyme activities, enhance NAD+ levels, and promote sirtuin activity, thereby addressing endothelial dysfunction and associated diseases.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If oral or IV routes of administration are used to deliver therapeutic agents, then systemic bioavailability is achieved, but adequate therapeutic levels at the targeted local site cannot be provided
Solution Approach 1:
The patent uses transdermal delivery as an intermediary route between oral/IV administration and direct local delivery. The formulation penetrates through the skin barrier to deliver agents like curcuminoids and senolytic flavonoids directly into systemic circulation while maintaining sustained local concentrations at target sites such as endothelium, joints, and lungs, thereby resolving the contradiction between systemic availability and local therapeutic adequacy
Solution Approach 2:
The patent modifies the physical and chemical parameters of the therapeutic agents by formulating them in a transdermal delivery system with specific excipients and penetration enhancers. This changes the absorption characteristics, bioavailability profile, and sustained release parameters of the agents, enabling them to achieve both systemic presence and adequate local concentrations that cannot be obtained through conventional oral or IV routes
2Quantity of substance
If therapeutic agents are delivered systemically to achieve therapeutic levels, then bioavailability is improved, but rapid elimination by the liver reduces effective concentration at target site
Solution Approach 1:
The transdermal formulation provides continuous, sustained delivery of therapeutic agents through the skin over extended periods. This continuous delivery mechanism bypasses the liver's first-pass elimination and maintains steady-state concentrations of agents like curcuminoids and senolytic flavonoids at target sites, ensuring prolonged therapeutic action without the rapid elimination seen in oral or IV administration
Solution Approach 2:
The formulation is designed to pre-establish sustained release characteristics and skin penetration capabilities before administration. The transdermal system is prepared with penetration enhancers and sustained-release matrices in advance, allowing it to immediately begin delivering therapeutic agents at controlled rates upon application, thereby preventing rapid elimination and maintaining therapeutic levels throughout the desired duration
3Quantity of substance
If therapeutic agents are administered orally to achieve systemic delivery, then bioavailability is enhanced, but low solubility and gut uptake limitations prevent effective delivery
Solution Approach 1:
The patent employs transdermal delivery as an intermediary route that avoids the gastrointestinal tract and its limitations (low solubility, poor gut uptake). The formulation uses skin penetration enhancers and transdermal-specific excipients as mediators to deliver therapeutic agents like curcuminoids and senolytic flavonoids directly through the skin into systemic circulation, bypassing gut-related absorption barriers while achieving effective systemic delivery
Solution Approach 2:
The patent changes the formulation parameters and delivery route from oral to transdermal. This involves modifying the physical state, solubility characteristics, and release kinetics of therapeutic agents by incorporating transdermal penetration enhancers and sustained-release matrices, thereby improving systemic delivery efficiency while accepting the increased formulation complexity inherent in transdermal systems
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 formulation achieves effective transdermal delivery, reducing CD38 activity and enhancing NAD+ levels, which in turn promotes sirtuin activity and improves endothelial function, offering new methods for preventing and treating various diseases, including endothelial dysfunction, osteoarthritis, and long COVID.
Implementation Method 1
Transdermal delivery formulations... provide sustained delivery of therapeutic agents through the skin
Data Source
AI summary
A transdermal formulation for the delivery of one or more active agents to a subject is provided. The formulation can be applied to the treatment of various diseases or conditions associated with an elevated CD38 level.