Electron Transfer Phosphate Carrier for Transdermal Delivery

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Solution Overview

Problem

Current pharmaceutical delivery methods face challenges in achieving optimal bioavailability and absorption rates, particularly for transdermal delivery, where the skin's barrier properties limit the rate of pharmaceutical transport, leading to inefficient delivery of therapeutically beneficial blood levels for systemic medication.

Innovation Solution

A carrier comprising C1-C4 alcohols, polyols, polymers, water, and di- and/or mono-(electron transfer agent) phosphate derivatives or complexes thereof is used to enhance the bioavailability and transport of biologically active compounds, forming vesicles that can traverse intercellular pathways and deliver compounds intracellularly or into systemic circulation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If transdermal delivery is used to administer pharmaceuticals, then the pharmaceutical can be delivered through the skin, but the skin's barrier properties limit the rate of pharmaceutical transport

Engineering Contradiction:
Improvetransdermal delivery capabilityVSAvoidpharmaceutical transport rate
Core Design Contradiction:
Ease of operationVSProductivity

Solution Approach 1:

The patent uses electron transfer agent phosphate derivatives as intermediary substances that facilitate the transport of pharmaceuticals through the skin. These compounds act as mediators between the pharmaceutical and the skin barrier, enabling enhanced transdermal delivery while maintaining the integrity of the skin's protective function.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent employs C1-C4 alcohols and polyols to change the physical and chemical parameters of the pharmaceutical formulation, such as solubility, viscosity, and molecular size. These parameter changes enable the pharmaceutical to penetrate the skin barrier more effectively while maintaining controlled transport rates.

Inventive Principle:
Principle #35Parameter changes

2Ease of operation

If the pharmaceutical is absorbed through the intestinal or stomach wall, then it enters the bloodstream, but a significant proportion is metabolised and excreted by the liver before reaching the bloodstream

Engineering Contradiction:
Improveenteral absorptionVSAvoidbioavailability
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The electron transfer agent phosphate derivatives serve as intermediaries that protect the pharmaceutical from hepatic metabolism. These compounds facilitate direct absorption into the bloodstream while reducing first-pass metabolism, thereby improving bioavailability and reliability of drug delivery.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Stability of the object's composition

If the pharmaceutical forms a non-absorbable complex or is degraded chemically or enzymatically, then absorption decreases

Engineering Contradiction:
Improvepharmaceutical stabilityVSAvoidabsorption rate
Core Design Contradiction:
Stability of the object's compositionVSProductivity

Solution Approach 1:

The patent modifies the chemical parameters of the pharmaceutical through complexation with electron transfer agent phosphate derivatives. This changes the pharmaceutical's stability profile, preventing degradation while maintaining or enhancing absorption rate through improved solubility and resistance to enzymatic breakdown.

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

The described carrier significantly increases the efficacy and transport of biologically active compounds, as demonstrated by enhanced plasma levels and skin penetration of compounds like PTH, CoQ10, and insulin, offering improved bioavailability and therapeutic effectiveness.

Implementation Method 1

forming vesicles that can traverse intercellular pathways and deliver compounds intracellularly or into systemic circulation

Methodology Applied
Scientific EffectVesicle formation: Emulsion

Implementation Method 2

The described carrier significantly increases the efficacy and transport of biologically active compounds, as demonstrated by enhanced plasma levels and skin penetration

Methodology Applied
Scientific EffectTransdermal transport: Permeation

Implementation Method 3

one or more di- and/or mono-(electron transfer agent) phosphate derivatives or complexes thereof

Methodology Applied
Scientific EffectElectron transfer: Redox Reactions

Data Source

PatentUS9168216B2Carrier comprising one or more di and/or mono-(electron transfer agent) phosphate derivatives or complexes thereof
Publication Date: 2015.10.27 VITAL HEALTH SCIENCES PTY LTD
  • US9168216B2 patent drawing
  • US9168216B2 patent drawing
  • US9168216B2 patent drawing

AI summary

The invention relates to a carrier for administering biologically active compounds comprising one or more C1-C4 alcohols, polyols and polymers thereof, water and one or more di and/or mono-(electron transfer agent) phosphate derivatives or complexes thereof. The carrier may be used in administering biologically active compounds, in particular pharmaceuticals including cosmetic agents.