Lipid Microcapsules for Dispersed Active Ingredient Skin Penetration
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Solution Overview
Problem
Formulating pharmaceutical active ingredients that are poorly soluble and unstable, leading to difficulties in skin penetration and tolerance, particularly due to the need for high concentrations of solubilizers which can be irritating and difficult to use.
Innovation Solution
A pharmaceutical composition featuring lipid microcapsules dispersed in a pharmaceutically acceptable vehicle, where the active ingredient is not within the microcapsules, but rather in a dispersed form within the vehicle, enhancing skin penetration and stability without requiring high solvent content.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If active ingredient is incorporated in solubilized form, then penetration into skin is improved, but stability and tolerance worsen
Solution Approach 1:
Lipid microcapsules serve as an intermediary carrier system that enables dispersed active ingredients to penetrate skin effectively. The microcapsules with oily internal phase and lipid envelope facilitate the transport of hydrophobic active ingredients through the skin barrier without requiring solubilization, thus maintaining stability while achieving good penetration.
Solution Approach 2:
The invention changes the physical state of the active ingredient from solubilized to dispersed form, and modifies the delivery system by introducing lipid microcapsules. This parameter change allows the active ingredient to maintain its dispersed state (improving stability) while the microcapsule system enables effective skin penetration.
2Reliability
If active ingredient is incorporated in dispersed form, then stability is improved, but penetration into skin worsens
Solution Approach 1:
Lipid microcapsules act as a mediator between the dispersed active ingredient and the skin. The oily internal phase of the microcapsules interacts with the dispersed active ingredient, while the lipid envelope facilitates interaction with the skin barrier, enabling effective penetration without compromising the dispersed state and stability of the active ingredient.
Solution Approach 2:
The invention uses a composite delivery system consisting of lipid microcapsules with specific envelope materials (phospholipids, cholesterol, fatty acids) and oily internal phase, combined with dispersed active ingredient. This composite structure enables both stability of the dispersed active ingredient and effective skin penetration.
3Quantity of substance
If high concentration of solubilizer is used, then solubility is improved, but tolerance and ease of manufacture worsen
Solution Approach 1:
The invention extracts the need for high concentrations of solubilizers by using lipid microcapsules as an alternative delivery system. The microcapsules provide solubility enhancement through their oily internal phase and lipid envelope structure, eliminating the requirement for high levels of traditional solubilizers that cause irritation.
Solution Approach 2:
The invention changes the approach to solubility by transitioning from using high concentrations of solubilizing agents to using a dispersed system with lipid microcapsules. This parameter change reduces the concentration of potentially irritating substances while maintaining or improving solubility and skin tolerance.
4Quantity of substance
If high concentration of solubilizer is used, then solubility is improved, but device complexity worsens
Solution Approach 1:
The invention extracts the complex solubilization step by using pre-formed lipid microcapsules. Instead of requiring complex formulation processes to achieve solubility through high concentrations of solubilizers, the microcapsule system provides solubility enhancement through its structural design, simplifying the overall formulation process.
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 composition achieves stable and effective skin penetration of active ingredients, improving tolerance and reducing irritation, with penetration levels comparable to solubilized forms, while avoiding the use of volatile organic solvents and polymers.
Implementation Method 1
the presence of lipid microcapsules dispersed within a vehicle of a composition makes it possible to help the active ingredient dispersed within the same vehicle to penetrate into the skin layers after application to the skin
Data Source
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AI summary
The present invention relates to a composition comprising lipid microcapsules and at least one dispersed active principle, and to the method for preparing same. The invention also relates to the composition for the use thereof in the treatment of dermatological diseases.