Coated Liposome Composition With Cyclodextrin for Skin Penetration
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Solution Overview
Problem
The skin's protective functions hinder the deeper penetration of poorly soluble active ingredients, necessitating improved strategies for topical administration.
Innovation Solution
A composition of coated liposomes containing alkylated or hydroxyalkylated β-cyclodextrin derivatives and modified starch, which enhances the solubility and permeability of poorly soluble active ingredients through the skin.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If the skin's protective barrier functions are maintained, then protection against external influences is improved, but penetration of poorly soluble active ingredients deteriorates
Solution Approach 1:
The patent employs cyclodextrin derivatives as intermediary carriers that form inclusion complexes with poorly soluble active ingredients, and coated liposomes as mediating delivery systems that transport these complexes across the skin barrier. This intermediary approach allows the skin's protective barrier to remain intact while enabling effective delivery of hydrophobic substances through the cyclodextrin-liposome system.
Solution Approach 2:
The invention creates a composite delivery system combining cyclodextrin derivatives (which solubilize hydrophobic compounds) with liposomes (which provide membrane-like structures for skin penetration). This composite material approach resolves the contradiction by integrating two different mechanisms: cyclodextrins address solubility while liposomes address permeability, allowing both barrier protection and effective delivery.
2Quantity of substance
If solubility of poorly soluble active ingredients is improved using cyclodextrin derivatives, then concentration in formulation is improved, but skin permeability may deteriorate
Solution Approach 1:
The patent implements a nested structure where cyclodextrin derivatives (outer layer) form inclusion complexes with active ingredients, and these complexes are then encapsulated within liposomes (inner layer). This nested arrangement allows cyclodextrins to provide solubility enhancement at the formulation level while liposomes provide the permeability enhancement at the skin delivery level, resolving the solubility-permeability trade-off.
Solution Approach 2:
The invention changes the physical-chemical parameters of the active ingredient delivery system by transitioning from direct application of poorly soluble compounds to a two-stage carrier system. The cyclodextrin derivation changes solubility parameters, while the liposome coating changes permeability parameters, allowing optimization of both concentration and skin penetration simultaneously.
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 significantly improves the skin permeability of poorly soluble active ingredients, allowing for effective topical administration and delivery.
Implementation Method 1
wherein the active ingredient is associated with an alkylated or hydroxyalkylated derivative of β-cyclodextrin
Implementation Method 2
improving the penetration of poorly soluble active ingredients into the skin
Data Source
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AI summary
The invention relates to a system of coated liposomes loaded with an active ingredient encapsulated in cyclodextrin. Furthermore, their use for improving the penetration of poorly soluble active ingredients into the skin and a method for producing the coated liposomes are described.