Lipid-Polymer Nanoparticles for Stable Delivery of Insoluble Bioactives
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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 composite lipid-polymer particles combining phospholipids, cholesterol, and poloxamer block copolymers to create a hybrid carrier system that merges the targeting capability of liposomes with the stability of polymer particles, resolving the contradiction between delivery effectiveness and formulation stability
Solution Approach 2:
The patent modifies physical parameters including particle size (50-500 nm range), lipid-to-polymer ratios, and sterol concentrations to optimize both stability and bioavailability, demonstrating how parameter adjustment can simultaneously address multiple conflicting requirements
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 patent optimizes particle size parameters (50-500 nm) and compositional parameters (lipid ratios, poloxamer concentrations) to enhance bioavailability while maintaining targeted delivery, showing how parameter control can simultaneously improve both delivery effectiveness and drug availability
3Quantity of substance
If organic solvents are used to deliver lipophilic bioactive agents, then solubility is improved, but safety and stability are compromised
Solution Approach 1:
The patent introduces lipid-polymer composite particles as intermediary carriers that solubilize lipophilic bioactive agents through their amphiphilic structure, eliminating the need for harmful organic solvents while maintaining solubility and improving safety
Solution Approach 2:
The patent changes the physical state and solubility parameters by forming nanostructured lipid-polymer particles that provide a safe alternative solvent system, demonstrating how physical form modification can replace chemical solvents
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 lipid-polymer composite particles provide improved stability, bioavailability, and controlled drug release, allowing for effective delivery of bioactive agents without the need for organic solvents.
Implementation Method 1
The lipid-polymer composite particles may include a block copolymer, a lipid (e.g., a neutral lipid, a cationic lipid, or an anionic lipid), and a sterol
Implementation Method 2
a plurality of lipid-polymer composite particles encapsulating a bioactive agent
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.