Transdermal Formulations Using Alkyl Alcohol and Organic Acid

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Solution Overview

Problem

Many therapeutic agents fail to penetrate the skin in therapeutically effective concentrations without penetration-enhancing agents, and there is a need for compositions that both moisturize the skin and enhance transdermal permeation of these agents.

Innovation Solution

Compositions comprising a first component, a second component, a C2-10 alkyl alcohol, and an organic acid, which include specific compounds and ratios, are used to facilitate skin hydration and enhance the transdermal permeation of therapeutic agents through the skin.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If penetration-enhancing agents are used to increase therapeutic agent penetration through the skin, then transdermal permeation is improved, but skin moisture loss increases and dry skin occurs

Engineering Contradiction:
Improvetransdermal permeationVSAvoidskin moisture loss
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent uses a multi-component composition including penetration-enhancing agents (such as fatty acids, alcohols, and surfactants) as intermediaries that facilitate therapeutic agent penetration while simultaneously providing moisturizing components (such as humectants and emollients) to prevent skin moisture loss. This mediator approach allows the system to enhance permeation without causing the harmful side effect of dry skin.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Quantity of substance

If penetration-enhancing agents are used to facilitate therapeutic agent penetration, then transdermal absorption is improved, but skin hydration decreases

Engineering Contradiction:
Improvetherapeutic agent penetrationVSAvoidskin hydration
Core Design Contradiction:
Quantity of substanceVSLoss of substance

Solution Approach 1:

The patent merges multiple functions into a single transdermal composition: penetration enhancement (using agents like oleic acid, ethanol, or polysorbates), moisturization (using humectants like glycerin or hyaluronic acid), and therapeutic delivery. This combined formulation ensures that while penetration-enhancing agents facilitate therapeutic agent absorption, the moisturizing components counteract their drying effects, maintaining skin hydration.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The invention employs a composite formulation consisting of multiple components with complementary properties: penetration-enhancing agents (fatty acids, alcohols, surfactants), moisturizing agents (humectants, emollients, occlusives), and therapeutic agents. This composite material approach allows the system to achieve effective drug penetration while maintaining skin barrier function and hydration, resolving the contradiction between enhanced absorption and skin moisture retention.

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

These compositions effectively increase skin hydration and enhance the penetration of therapeutic agents, allowing them to reach therapeutically effective concentrations in the bloodstream, addressing the challenges of dry skin and agent penetration.

Implementation Method 1

compositions that facilitate the penetration of therapeutic agents through the skin are needed

Methodology Applied
Scientific EffectPermeation enhancement: Permeation

Implementation Method 2

the loss of skin moisture results in dry skin that can be uncomfortable, painful, or unattractive. Compositions that ameliorate dry skin and increase or maintain skin hydration are also needed

Methodology Applied
Scientific EffectHydration: Absorption (physical)

Data Source

PatentUS9687528B2Transdermal formulations
Publication Date: 2017.06.27 HOFFMAN STEVEN

AI summary

The present disclosure is directed to transdermal and moisturizing compositions.