Lipid-Polymer Composite Particles for Insoluble Bioactive Loading
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Solution Overview
Problem
Delivery of bioactive agents with low solubility in aqueous media is challenging due to stability and bioavailability issues with existing liposome and micellar nanoparticle systems.
Innovation Solution
A composition of lipid-polymer composite particles, comprising a block copolymer, lipid, and sterol, encapsulating bioactive agents, with a mean particle size of 10-1000 nm, is developed to enhance stability and bioavailability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If liposomes and micellar nanoparticles are used as carrier systems for insoluble bioactive agents, then targeted delivery is achieved, but stability and bioavailability are compromised
Solution Approach 1:
The patent employs a composite nanoparticle system combining lipids and block copolymers to create lipid-polymer composite particles. This composite structure integrates the amphipathic properties of lipids with the structural stability of block copolymers, achieving both targeted delivery capability and enhanced formulation stability that neither component achieves alone.
Solution Approach 2:
The patent modifies the physical and chemical parameters of the carrier system by controlling particle size (10-1000 nm), lipid-to-polymer ratios, and compositional parameters. These parameter optimizations resolve the contradiction by tuning the system to achieve both stability and delivery effectiveness simultaneously.
2Reliability
If liposomes and micellar nanoparticles are used as carrier systems for insoluble bioactive agents, then targeted delivery is achieved, but bioavailability is compromised
Solution Approach 1:
The lipid-polymer composite structure enhances bioavailability by combining the solubilization capacity of lipids with the controlled release properties of block copolymers, enabling higher quantities of insoluble bioactive agents to reach their target sites effectively.
Solution Approach 2:
The composite nanoparticle system provides different functional zones: the lipid component addresses solubility issues in aqueous media, while the polymer component controls release kinetics, creating local quality variations that simultaneously improve both delivery effectiveness and bioavailability.
3Productivity
If existing nanoparticle delivery systems are used, then some delivery capability is achieved, but stability and degradation issues prevent widespread implementation
Solution Approach 1:
By creating lipid-polymer composite nanoparticles, the patent resolves the reliability issue through the synergistic combination of lipid stability and polymer structural integrity, enabling widespread implementation while maintaining delivery capability.
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 provides improved stability, bioavailability, and controlled drug release of bioactive agents, allowing for effective delivery through various administration routes.
Implementation Method 1
The plurality of lipid-polymer composite particles may be formed by a multi-step process that includes homogenization of the bioactive agent with the poloxamer followed by injection of the lipid and sterol into the homogenized solution
Data Source
AI summary
The present invention features new lipid-polymer composite particles that are useful for the formulation of bioactive agents for administration to a subject. The nanoparticles include a block copolymer, a lipid, e.g., phospholipid, and a sterol. The formulations of a bioactive agent (e.g., a therapeutic agent, a nutraceutical agent, or a recreational agent) described herein provide for easier loading of lipid-polymer composite particles with higher drug loading capacity, increased stability of the formulations, and lower surface tension of water, which allows for lipid coating and entrapment.