Smart Polymer Microneedles for Solvent-Free Transdermal Delivery
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Solution Overview
Problem
Existing drug delivery systems for lipophilic drugs face limitations such as biological safety issues, adverse side effects from solvents, difficulty in adjusting drug doses, and challenges in transdermal delivery due to high lipophilicity and molecular weight, leading to low bioavailability and limited market presence.
Innovation Solution
A smart polymer system (SPS) using a biodegradable polymer combination of polyvinyl pyrrolidone and hyaluronic acid forms colloidal particles with a core-shell structure, enabling transdermal delivery of lipophilic drugs without solvents, through biodegradable microneedles that homogenize and minimize particle size.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If organic solvents are used to improve solubility of lipophilic drugs, then solubility increases, but biological safety issues and adverse side effects occur
Solution Approach 1:
The invention extracts and eliminates the organic solvent component from the drug delivery system. By using a non-solvent-based approach with biodegradable polymers, the system achieves drug delivery without the harmful solvents that cause biological safety issues and adverse side effects, while still maintaining effective drug release.
Solution Approach 2:
Biodegradable polymers serve as an intermediary substance between the lipophilic drug and the biological system. These polymers enable drug delivery and control release kinetics without requiring organic solvents, thus mediating the interaction between the lipophilic drug and biological tissues in a safe manner.
2Ease of operation
If nasal drug delivery using high-pressure powder spray is used, then transdermal delivery is achieved, but dose adjustment is difficult and airway hypersensitivity occurs
Solution Approach 1:
The invention changes the physical state and delivery parameters of the drug by using non-solvent-based formulations with biodegradable polymers. This allows for controlled release kinetics and easier dose adjustment compared to high-pressure spray systems, while avoiding airway hypersensitivity through transdermal rather than nasal administration.
3Reliability
If oral lipophilic drug delivery is used, then first pass metabolism is avoided, but bioavailability is lowered due to liver metabolism
Solution Approach 1:
The invention replaces the oral administration route with transdermal delivery using non-solvent-based formulations. This substitution eliminates first-pass liver metabolism entirely while maintaining or improving bioavailability, as the drug enters systemic circulation directly through the skin without gastrointestinal processing.
4Object-affected harmful factors
If powder-type lipophilic drug is delivered transdermally without solubilizing, then solvent-free delivery is achieved, but skin barrier penetration is very difficult
Solution Approach 1:
The invention uses composite materials consisting of biodegradable polymers combined with lipophilic drugs in a non-solvent-based formulation. This composite structure enables skin barrier penetration by leveraging the permeability-enhancing properties of the polymer-drug complex while maintaining a solvent-free system.
Solution Approach 2:
The invention changes the physical and chemical parameters of the drug delivery system by using non-solvent-based formulations with biodegradable polymers. This alters the drug's interaction with the skin barrier, enabling penetration without requiring organic solvents to solubilize the lipophilic drug.
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 SPS system facilitates safe, efficient, and pain-free transdermal delivery of lipophilic drugs, overcoming skin barriers and enhancing bioavailability by forming nano-sized colloidal particles that are uniformly loaded onto microneedles, improving therapeutic effects.
Implementation Method 1
homogenizing a lipophilic drug in the form of crude powder in a biodegradable polymer without using a solubilizing solvent
Implementation Method 2
colloidal particles formed of a combination of a powder-type lipophilic drug and a biodegradable polymer
Implementation Method 3
transdermal drug delivery system capable of overcoming the skin barrier and thus delivering the powder-type lipophilic drug
Implementation Method 4
biodegradable polymer formed of polyvinyl pyrrolidone and hyaluronic acid
Data Source
Figure 1A
Figure 1B~1C
Figure 2A~2B
AI summary
A viscous composition for transdermal drug delivery, a method of preparing the same, and a microstructure device prepared using the viscous composition are provided. Here, the viscous composition includes colloidal particles formed of a combination of a drug and a biodegradable polymer, and the biodegradable polymer includes a first amphiphilic polymer. The use of a solvent can be minimized to homogenize the drug in the biodegradable polymer including the first amphiphilic polymer, thereby forming colloidal particles. Therefore, since a separate solvent cannot be used, the microstructure device is expected to be a transdermal drug delivery system which is safe, efficient or useful for drugs which do not include a proper solvent, show poor bioavailability or have a high molecular weight.