Thixotropic Gel Delivery System for High-Concentration Transdermal Actives
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Solution Overview
Problem
Existing drug delivery methods, particularly oral administration, result in significant side effects, liver toxicity, and inefficiencies, while topical delivery systems face challenges in solubilizing high concentrations of active agents without causing skin irritation.
Innovation Solution
Formulations comprising an active agent, an oil phase, an organic solvent, and a thickener, with minimal water content, that form a thixotropic thinning gel, allowing for high concentrations of actives like NSAIDs, opioids, and proteins to be solubilized and delivered transdermally with reduced skin sensitivity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If oral administration of opioids is used to achieve pain relief, then therapeutic effect is achieved, but side effects including liver toxicity, addiction, and constipation occur
Solution Approach 1:
The patent extracts the opioid active agent from the oral administration route and delivers it directly to the site of action through the skin. The formulation isolates the therapeutic component (opioid) and transports it transdermally, bypassing the gastrointestinal system and liver metabolism that cause harmful side effects.
Solution Approach 2:
The patent introduces a thixotropic gel formulation as an intermediary system between the opioid and the body. This gel contains penetration enhancers and specific excipients that facilitate transdermal delivery, acting as a mediator that enables the opioid to reach the bloodstream through the skin without oral administration.
2Productivity
If high concentrations of active agents are solubilized in topical formulations, then targeted delivery efficiency is improved, but skin irritation increases
Solution Approach 1:
The patent changes the physical and chemical parameters of the formulation system by using a thixotropic gel base with specific viscosity characteristics and penetration enhancers. These parameter changes allow high concentrations of actives to be solubilized while the gel structure and enhancers work together to minimize skin irritation during application and absorption.
Solution Approach 2:
The patent creates a composite formulation system combining multiple components: thixotropic thickeners, penetration enhancers, solvents, and active agents. This composite material approach allows the formulation to simultaneously achieve high active concentration solubility and reduced skin irritation through the synergistic interaction of its components.
3Stability of the object's composition
If minimal water systems are used in formulations, then product stability and preservation are improved, but solubilization capacity is reduced
Solution Approach 1:
The patent changes the solvent system parameters by using oil-based and alcohol-based vehicles instead of water-based systems. This parameter change maintains product stability and eliminates the need for water while the formulation incorporates multiple solubilizing agents and penetration enhancers to maintain adequate solubilization capacity for high active concentrations.
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 formulations enable quick penetration of high active concentrations with minimal skin irritation, potentially replacing oral delivery and addressing issues like opioid addiction and constipation, while facilitating multi-drug combinations with lower overall dosages.
Implementation Method 1
said formulation optionally forms a thixotropic thinning gel
Implementation Method 2
High concentrations of actives (for example: naproxen (15%), acetaminophen (30%), ibuprofen (25%)) can surprisingly be solubilized and delivered topically
Implementation Method 3
an oil and/or solvent soluble skin penetration enhancer
Data Source
AI summary
In accordance with the present disclosure, there are provided formulations comprising:(a) at least one active agent;(b) an oil, and optionally a thickener therefor;(c) an organic solvent, and a thickener therefor; and(d) an oil and/or solvent soluble skin penetration enhancer;wherein:said formulation comprises <10 wt % water; andsaid formulation optionally forms a thixotropic thinning gel.Also provided are gels comprising oil and organic solvent, methods for preparing same and methods for the topical delivery of an active agent to a subject in need thereof.