Cationic PEI Drug Delivery Composition for Vessel Wall Adhesion
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Solution Overview
Problem
Current drug delivery systems for hydrophobic active agents face challenges in achieving effective local administration, particularly in maintaining structural integrity during medical procedures and maximizing uptake into vessel walls while minimizing systemic distribution.
Innovation Solution
A drug delivery composition comprising a cationic delivery agent, such as branched polyethyleneimine, combined with a hydrophobic active agent and a pharmaceutically acceptable aqueous carrier, which forms a suspension or solution to enhance adhesion and uptake at the target site, using a drug eluting balloon catheter or similar devices.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If hydrophobic active agents are administered locally, then therapeutic effect at target site is improved, but structural integrity during medical procedures deteriorates
Solution Approach 1:
The patent employs composite particle structures combining hydrophobic active agents with hydrophilic polymers and cationic agents. This composite approach allows the particles to maintain structural integrity during procedures while enabling effective local delivery of hydrophobic agents to target sites.
Solution Approach 2:
The patent introduces cationic agents and hydrophilic polymers as intermediary substances that bridge the hydrophobic active agents and the aqueous environment. These intermediaries protect the structural integrity of the delivery system during procedures while facilitating therapeutic delivery at the target site.
2Productivity
If hydrophobic active agents are delivered locally, then uptake into vessel walls is maximized, but systemic distribution increases
Solution Approach 1:
The patent creates particles with localized functional zones - hydrophobic regions for active agent containment and cationic/hydrophilic regions for targeted interaction with vessel wall tissues. This local quality differentiation enables maximized uptake at the target site while minimizing systemic distribution through electrostatic and hydrophilic guidance.
3Ease of operation
If cationic delivery agents are used, then adhesion at target site is enhanced, but structural stability deteriorates
Solution Approach 1:
The patent utilizes controlled changes in electrostatic parameters and hydrophilic/hydrophobic balance within the particle structure. By adjusting the ratio and distribution of cationic agents and hydrophilic polymers, the particles achieve enhanced adhesion at the target site while maintaining sufficient structural stability for procedural integrity.
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 retains the hydrophobic active agent at the administration site, enhancing bioavailability and reducing systemic toxicity, with improved structural integrity during medical procedures and efficient transfer to the vessel wall.
Implementation Method 1
A delivery composition for local administration of a hydrophobic active agent includes a cationic delivery agent and a hydrophobic active agent
Implementation Method 2
combined with a hydrophobic active agent and a pharmaceutically acceptable aqueous carrier, which forms a suspension or solution
Data Source
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AI summary
Disclosed herein is a delivery composition for administering a hydrophobic active agent. In one embodiment, a delivery composition for local administration of a hydrophobic active agent to a tissue or organ of a patient is disclosed. In one embodiment, the delivery composition includes a cationic delivery agent, a therapeutically effective amount of a hydrophobic active agent and a pharmaceutically acceptable aqueous carrier. In one embodiment, the cationic delivery agent includes polyethyleneimine (PEI). In an embodiment, the invention includes a drug delivery device including a substrate; and coated therapeutic agent particles disposed on the substrate, the coated therapeutic agent particles comprising a particulate hydrophobic therapeutic agent; and a vinyl amine polymer. Methods of making the delivery composition, as well as kits and methods of use are also included herein.