Nano-domain Gel for Sustained Topical Drug Release
Solution Overview
Problem
Topical delivery systems for active agents face challenges in achieving long-term stability, controlled release, and penetration into skin layers while avoiding systemic effects, with existing formulations often having limited thermodynamic stability and penetration.
Innovation Solution
A novel topical formulation comprising an oily phase in the form of nano-domains dispersed in a gelled aqueous phase, featuring a unique combination of components including an active agent, hydrophilic surfactants, co-surfactants, polar solvents, and penetrating promoters, which forms a depot effect in the skin, enabling prolonged and controlled release.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If conventional lipophilic carriers or emulsion-based creams are used for topical delivery, then the active agent can be delivered to the skin, but the system lacks long-term stability and controlled release capability
Solution Approach 1:
The invention uses a composite delivery system combining lipophilic oily domains (for active agent solubilization) with a hydrophilic gel matrix (for structural stability and controlled release). This composite structure integrates the advantages of both lipophilic and hydrophilic phases, achieving long-term stability while enabling controlled release of the active agent through the gel network.
Solution Approach 2:
The invention modifies the physical parameters of the delivery system by creating a gel matrix with specific rheological properties (viscosity, gel strength) that control the diffusion rate of the active agent. The gel concentration, cross-linking density, and network structure are adjusted to achieve the desired controlled release profile while maintaining long-term stability.
2Ease of operation
If emulsion-based creams are used, then the active agent can be dispersed in aqueous phase, but penetration into skin layers is limited
Solution Approach 1:
The invention segments the delivery system into distinct oily domains (nanoscale droplets) dispersed within the gel matrix. This segmentation creates numerous small interfaces that enhance skin penetration while the gel matrix provides a reservoir for sustained release, improving both penetration capability and delivery performance.
Solution Approach 2:
The gel matrix acts as an intermediary between the oily domains containing the active agent and the skin tissue. It facilitates controlled transfer of the active agent from the oily phase to the skin while preventing premature release or degradation, thereby enhancing penetration while maintaining reliable delivery.
3Quantity of substance
If high oil content is used to solubilize active agent, then solubilization capacity increases, but thermodynamic stability decreases
Solution Approach 1:
The invention changes the physical state of the continuous phase from liquid to gel, which fundamentally alters the thermodynamic stability of the system. The gel matrix provides a rigid network structure that prevents coalescence of oily domains and phase separation, enabling high oil content (5-50 wt%) to be maintained with improved thermodynamic stability while preserving solubilization capacity.
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 formulation achieves high stability, enhanced penetration, and prolonged release of active agents, maintaining a depot effect in the skin with minimal systemic exposure, providing a prolonged and controlled release profile.
Implementation Method 1
lipophilic carriers, that solubilize the active agent therein
Implementation Method 2
oily nano-domains dispersed in a viscosified/gelled continuous aqueous phase
Implementation Method 3
dispersed in a viscosified or gelled continuous aqueous phase
Implementation Method 4
at least two hydrophilic surfactants, at least one co-surfactant
Implementation Method 5
at least two penetrating promotors... high penetration through the Stratum Corneum
Implementation Method 6
designed to load various active agents, and are suitable for topical administration of the active in a controlled, typically prolonged, release manner
Data Source
AI summary
The disclosure concerns viscous or gelled delivery systems based on oily nano-domains dispersed in a viscosified/gelled continuous aqueous phase, and suitable for prolonged and/or sustained topical delivery of various active compounds.