Nitric Oxide Transdermal Delivery via Phosphatidylcholine Vesicles

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Solution Overview

Problem

Current topical drug delivery systems for nitric oxide are inefficient and unstable, as nitric oxide is highly reactive and difficult to store and deliver effectively through the skin, leading to limited therapeutic applications and potential side effects.

Innovation Solution

The development of transdermal compositions that entrap nitric oxide within a lecithin, such as phosphatidylcholine, forming vesicles or liquid crystals, which stabilizes the nitric oxide and allows for controlled release, enhancing its penetration and absorption into skin tissues.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If nitric oxide is delivered topically in conventional systems, then therapeutic effect is achieved, but the system is unstable and ineffective due to nitric oxide's high reactivity

Engineering Contradiction:
Improvestability of nitric oxide deliveryVSAvoidstability of nitric oxide
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent introduces phosphatidylcholine as an intermediary carrier substance that mediates between the unstable nitric oxide and the skin tissue. The phosphatidylcholine forms vesicles that encapsulate nitric oxide, protecting it from degradation while maintaining its biological activity. This intermediary carrier system resolves the contradiction by stabilizing the reactive nitric oxide without compromising its therapeutic effect.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the physical state and chemical environment of nitric oxide by incorporating it into phosphatidylcholine vesicles. This parameter change transforms nitric oxide from a free, highly reactive gas into a stabilized form within a lipid structure, improving its stability and deliverability while preserving its therapeutic properties.

Inventive Principle:
Principle #35Parameter changes

2Ease of operation

If nitric oxide is stored and delivered through conventional topical systems, then application is simple, but penetration and absorption into skin tissues is limited

Engineering Contradiction:
Improvesimplicity of topical applicationVSAvoidamount of nitric oxide penetrating skin
Core Design Contradiction:
Ease of operationVSQuantity of substance

Solution Approach 1:

Phosphatidylcholine serves as a bridging intermediary that facilitates nitric oxide penetration through the skin barrier. The vesicular structure formed by phosphatidylcholine interacts with skin lipids, enabling enhanced absorption while maintaining the simplicity of topical application. This resolves the contradiction by improving penetration without complicating the application process.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent creates a composite delivery system combining nitric oxide with phosphatidylcholine. This composite vesicular structure leverages the penetrating properties of phosphatidylcholine to enhance nitric oxide delivery into skin tissues, improving the quantity of substance absorbed while maintaining ease of topical application.

Inventive Principle:
Principle #40Composite materials

3Device complexity

If conventional topical delivery systems are used for nitric oxide, then system simplicity is maintained, but therapeutic effectiveness is reduced due to instability

Engineering Contradiction:
Improvesimplicity of delivery systemVSAvoidtherapeutic effectiveness
Core Design Contradiction:
Device complexityVSReliability

Solution Approach 1:

The phosphatidylcholine intermediary is integrated into the delivery system to simultaneously improve stability and maintain simplicity. The vesicular structure provides stabilization functionality while the overall system remains a simple topical application, resolving the contradiction between device complexity and therapeutic effectiveness.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

By changing the physical-chemical parameters of nitric oxide through phosphatidylcholine encapsulation, the patent achieves enhanced therapeutic effectiveness without significantly increasing system complexity. The modification occurs at the molecular level rather than at the system level, preserving simplicity while improving reliability.

Inventive Principle:
Principle #35Parameter changes

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 compositions provide a stable and effective delivery of nitric oxide for treating conditions like erectile dysfunction, wound healing, and hair growth, with reduced side effects and improved therapeutic outcomes by maintaining nitric oxide's bioavailability and stability.

Implementation Method 1

The phosphatidylcholine or lecithin may be contained within a second phase that causes the phosphatidylcholine or lecithin to form vesicles, e.g., micelles or liposomes

Methodology Applied
Scientific EffectVesicle formation:

Implementation Method 2

The phosphatidylcholine or lecithin may be contained within a second phase that causes the phosphatidylcholine or lecithin to form vesicles, e.g., micelles or liposomes

Methodology Applied
Scientific EffectLiquid crystal formation: Liquid Crystals

Implementation Method 3

Topical delivery systems for substances such as drugs, pain relieving compounds, vitamins, and skin improving compounds have been in use for a number of years

Methodology Applied
Scientific EffectTransdermal delivery: Permeation

Data Source

PatentUS9937202B2Topical nitric oxide systems and methods of use thereof
Publication Date: 2018.04.10 TRANSDERMAL TECHNOLOGIES INC
  • US9937202B2 patent drawing

AI summary

The present invention generally relates to compositions and methods for transdermal drug delivery. The compositions can be used in a variety of applications, including treating erectile dysfunction or sexual dysfunction, treating wounds, or causing or promoting hair growth. For example, in one aspect, the present invention is generally directed to compositions for delivery of nitric oxide. The nitric oxide may be present within a first phase comprising a lecithin, such as phosphatidylcholine. In certain embodiments, the lecithin is present in liposomes, micelles, or other vesicles. The composition can take the form of a gel, a cream, a lotion, an ointment, a solution, a solid “stick,” etc., that can be rubbed or sprayed onto the skin, e.g., onto the penis, vulva, or other suitable portion. The composition can also be applied to a mucosal surface. In some embodiments, a composition comprising nitric oxide is unexpectedly stable.