Transdermal PDE5 Inhibitor Delivery via Hostile Biophysical Environment
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Solution Overview
Problem
Current treatments for erectile dysfunction rely on oral delivery of phosphodiesterase type 5 inhibitors, which result in high systemic exposure and side effects, lacking transdermal formulations approved by the FDA.
Innovation Solution
Development of transdermal delivery compositions containing phosphodiesterase type 5 inhibitors and nitric oxide donors in a hostile biophysical environment, using stabilization polymers and surfactants to enhance skin penetration and reduce systemic exposure.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If phosphodiesterase type 5 inhibitors are delivered orally, then therapeutic effect is achieved, but systemic exposure increases and side effects occur
Solution Approach 1:
The patent applies local quality by delivering the phosphodiesterase type 5 inhibitor directly to the local site of action (penile tissue) through transdermal application, rather than systemic oral delivery. This creates a high concentration at the target site while minimizing systemic exposure, thereby achieving therapeutic effect with reduced side effects.
Solution Approach 2:
The patent uses the skin as an intermediary delivery route, applying the inhibitor through a transdermal formulation that allows controlled penetration into the penile tissue. This intermediary approach bypasses first-pass metabolism and systemic circulation, directly delivering the drug to the target tissue with reduced systemic burden.
2Object-generated harmful factors
If transdermal delivery is developed, then systemic exposure is reduced, but formulation complexity increases
Solution Approach 1:
The patent employs composite materials by formulating the phosphodiesterase type 5 inhibitor with penetration enhancers, lipids, and other excipients in a transdermal formulation. This composite approach enables controlled transdermal delivery while managing the complexity through a unified formulation system that achieves both reduced systemic exposure and practical applicability.
3Quantity of substance
If transdermal delivery is used, then targeted local delivery is achieved, but delivery speed to target tissue must be increased
Solution Approach 1:
The patent applies preliminary action by using formulation components that pre-condition the skin and enhance penetration capability before the active ingredient reaches the target tissue. The formulation includes penetration enhancers and lipids that prepare the skin barrier for rapid drug delivery, ensuring both high local concentration and fast delivery speed upon application.
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 transdermal delivery method achieves rapid and targeted therapy with significantly lower systemic exposure, reducing side effects and allowing for effective treatment of erectile dysfunction within minutes, compared to oral administration.
Implementation Method 1
transdermal delivery compositions containing phosphodiesterase type 5 inhibitors and nitric oxide donors in a hostile biophysical environment, using stabilization polymers and surfactants to enhance skin penetration
Data Source
AI summary
The present invention generally relates to the transdermal delivery of various compounds. In some aspects, transdermal delivery may be facilitated by the use of a hostile biophysical environment. One set of embodiments provides a composition for topical delivery comprising a phosphodiesterase type 5 inhibitor and/or a salt thereof, and optionally, a hostile biophysical environment and/or a nitric oxide donor. In some cases, the composition may be stabilized using a combination of a stabilization polymer (such as xanthan gum, KELTROL® BT and/or KELTROL® RD), propylene glycol, and a polysorbate surfactant such as Polysorbate 20, which combination unexpectedly provides temperature stability to the composition, e.g., at elevated temperatures such as at least 40° C. (at least about 104° F.), as compared to compositions lacking one or more of these.