Topical Sodium Nitrite Formulation for Sickle Cell Ulcers

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Solution Overview

Problem

Current treatments for sickle cell disease-related leg ulcers are inadequate, as they primarily focus on stimulating granulation formation without addressing pathological changes in microcirculation, and there is a need for a therapy that restores nitric oxide bioavailability to improve wound healing and pain management.

Innovation Solution

A topical sodium nitrite formulation, dispersed in a white petrolatum ointment, is applied to the affected area, which generates nitric oxide in tissues with low oxygen tension, promoting vasodilation and wound healing, and reducing pain and microbial growth.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments (antibiotics, compression bandages, dressing changes) are used to stimulate granulation formation, then wound healing is promoted, but pathological changes in microcirculation are not addressed

Engineering Contradiction:
Improvewound healing effectivenessVSAvoidcompleteness of treatment approach
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent introduces sodium nitrite as an intermediary substance that converts to nitric oxide in the wound environment. This nitric oxide mediator addresses the underlying microcirculation pathology while simultaneously promoting granulation formation, thus resolving the contradiction between treating symptoms and addressing root causes

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If nitric oxide is administered systemically to restore bioavailability, then microcirculation is improved, but systemic side effects occur

Engineering Contradiction:
Improvenitric oxide bioavailabilityVSAvoidsystemic side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies sodium nitrite topically directly to the ulcerated skin, creating a localized source of nitric oxide generation at the wound site. This local application restores nitric oxide bioavailability in the affected microcirculation while avoiding systemic distribution and associated side effects

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The sodium nitrite formulation leverages the wound environment itself (low oxygen tension, specific pH) to automatically convert the prodrug into active nitric oxide. The wound bed becomes self-sufficient in generating therapeutic nitric oxide without requiring systemic administration or complex delivery systems

Inventive Principle:
Principle #25Self-service

3Reliability

If topical sodium nitrite formulation is applied to generate nitric oxide in tissues, then vasodilation and wound healing are promoted, but formulation stability and controlled release must be maintained

Engineering Contradiction:
Improvetherapeutic effectVSAvoidformulation stability
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent utilizes changes in local wound parameters (low oxygen tension, acidic pH) to trigger conversion of sodium nitrite to nitric oxide. The formulation remains stable in the ointment base until applied, then automatically activates in response to the wound environment, achieving both stability and controlled release

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite formulation by dispersing sodium nitrite in a white petrolatum ointment base. This composite structure provides physical stability and controlled release properties, protecting the sodium nitrite until topical application when the therapeutic effect is activated

Inventive Principle:
Principle #40Composite materials

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 topical sodium nitrite cream significantly reduces leg ulcer size and pain, enhances blood flow, and promotes wound healing, with minimal systemic absorption and no significant adverse effects, indicating its potential as a well-tolerated and effective treatment for sickle cell disease-related ulcers.

Implementation Method 1

generates nitric oxide in tissues with low oxygen tension

Methodology Applied
Scientific EffectChemical reduction: Reduction

Data Source

PatentEP3217960B1Topical sodium nitrite formulation
Publication Date: 2020.01.08 THE GOVERNMENT OF THE UNITED STATES OF AMERICA AS REPRESENTED BY THE SECRETARY DEPARTMENT OF HEALTH & HUMAN SERVICES
  • EP3217960B1 patent drawingFigure 1A~1B
  • EP3217960B1 patent drawingFigure 1C
  • EP3217960B1 patent drawingFigure 2A~2B

AI summary

A sodium nitrite formulation for topical administration is described. The formulation includes an aqueous solution of non-acidified sodium nitrite dispersed in a white petrolatum ointment. The concentration of sodium nitrite in the formulation is about 0.5% to about 3.0% by weight. To prepare the formulation, non-acidified sodium nitrite is completely dissolved in a small quantity of water, sterile filtered and dispersed in white petrolatum ointment.