Biphasic Lipid Vesicles for Transdermal Delivery of Large Molecules
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Solution Overview
Problem
The barrier properties of the skin prevent most external substances from permeating into the body, and existing delivery systems for drugs, such as liposomes and solid lipid nanoparticles, are inefficient in delivering large molecules like proteins and nucleic acids through the skin.
Innovation Solution
A biphasic lipid vesicle composition comprising a lipid bilayer, an oil-in-water emulsion, and penetration enhancing agents like non-ionic surfactants with HLB of 10 or less, which are entrapped in the vesicles to enhance skin penetration of therapeutic compounds.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional delivery systems like liposomes and solid lipid nanoparticles are used, then the skin barrier properties are maintained, but the delivery efficiency of large molecules like proteins and nucleic acids is insufficient
Solution Approach 1:
The patent modifies the physical and chemical parameters of the lipid vesicles by incorporating penetration enhancing agents with specific HLB values (3-10), adjusting the lipid composition ratios, and controlling vesicle size and charge characteristics to optimize both skin barrier compatibility and large molecule delivery efficiency
Solution Approach 2:
The invention creates composite lipid vesicle systems by combining different types of lipids (phospholipids, cholesterol, fatty acids) with penetration enhancing agents and large molecule payloads, forming a multifunctional delivery system that simultaneously maintains barrier integrity and enhances permeation
2Productivity
If penetration enhancing agents are added to improve skin permeation, then the delivery of large molecules is enhanced, but the complexity of the formulation increases
Solution Approach 1:
The patent systematically evaluates and optimizes parameters including HLB value ranges (3-10), concentration levels, lipid composition ratios, and vesicle physical characteristics to achieve effective penetration enhancement while maintaining formulation simplicity and manufacturability
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 effectively delivers large molecules like peptides, proteins, and nucleic acids into the skin, improving topical delivery and treatment of skin conditions by enhancing the permeability of the skin barrier.
Implementation Method 1
one or more penetration enhancing agents entrapped in the lipid bilayer and/or the oil-in-water emulsion wherein the one or more penetration enhancing agents are one or more non-ionic surfactants having a hydrophilic-lipophilic balance (HLB) of 10 or less
Implementation Method 2
an oil-in-water emulsion entrapped in the biphasic lipid vesicles, and stabilized by one or more surfactants
Data Source
AI summary
The present application is related to a pharmaceutical composition a biphasic lipid vesicle comprising a lipid bilayer comprising vesicle forming lipids; an oil-in-water emulsion stabilized by one or more surfactants; one or more compounds; and one or more penetration enhancing agents. The one or more penetration enhancing agents include one or more non-ionic surfactants having a hydrophilic-lipophilic balance (HLB) of about 10 or less, alone or combination with one or more penetration enhancing agents selected from one or more of terpenes, alkaloids, salicylate derivatives, and polycationic surfactants and combinations thereof. The present application is also related to a pharmaceutical composition comprising a biphasic lipid vesicle comprising a lipid bilayer comprising vesicle forming lipids; an oil-in-water emulsion stabilized by one or more polycationic surfactants; and one or more compounds.