Multilayer Coated Microneedles for Sustained Protein Drug Release
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Existing microneedle technologies face challenges in maintaining the stability and bioavailability of water-soluble drugs, particularly polypeptides and proteins, due to quick dissolution and release, leading to reduced efficacy and the need for frequent administration.
Innovation Solution
A coated microneedle with a multilayer structure, comprising a base, needle tip, functional coating with a water-soluble polymer material and active ingredient, and a sustained-release layer made of a delayed crosslinked sodium alginate or near-neutral chitosan system, which includes a calcium source, glucolactone, and carrier, to control drug release and prevent rapid dissolution.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If water-soluble polymer materials and sugars are used as excipients to ensure stability and bioavailability of active ingredients, then the stability and bioavailability are improved, but the development is limited to quick-release formulations without sustained-release function
Solution Approach 1:
The patent uses a composite coating structure combining water-soluble polymer materials (carboxymethyl cellulose, hydroxypropyl methyl cellulose, hydroxyethyl cellulose) with sustained-release excipients (trehalose, maltose, cyclodextrins) to achieve both stability and sustained release. The composite nature allows the coating to maintain drug stability while controlling release rate over extended periods.
Solution Approach 2:
The patent modifies the physical and chemical parameters of the coating layer by adjusting the ratio of water-soluble polymer to sustained-release excipient, controlling coating thickness (5-50 μm), and optimizing moisture content. These parameter changes transform the quick-release characteristic into sustained-release while maintaining stability and bioavailability.
2Ease of manufacture
If quick-release coated microneedles are used to administer water-soluble drugs, then the administration process is simple, but the active ingredients remain in the microneedle and flow out with tissue fluid, reducing utilization rate
Solution Approach 1:
The patent applies a flexible coating layer (5-50 μm thick) made of water-soluble polymer and sustained-release excipient that acts as a barrier to prevent premature drug release. This thin film maintains the simplicity of microneedle administration while preventing active ingredients from flowing out with tissue fluid, thereby improving utilization rate.
Solution Approach 2:
The coating layer serves as an intermediary between the microneedle core and the external environment. It controls the interaction between the water-soluble drug and tissue fluid, allowing controlled release while preventing premature efflux. The coating material acts as a mediator that maintains drug stability and improves absorption efficiency.
3Reliability
If multiple single-factor control variable experiments are conducted to optimize protein drug formulas, then the formula optimization is thorough, but the experimental period is long and the cost of raw materials and detection is high
Solution Approach 1:
The patent segments the coating formulation into distinct functional components: water-soluble polymer material (providing stability and bioavailability), sustained-release excipient (providing extended release), and protective agent (providing stability). This segmentation allows independent optimization of each component's contribution, reducing the need for exhaustive single-factor experiments while maintaining thorough formula optimization.
Solution Approach 2:
The patent performs preliminary characterization of individual materials (water-soluble polymer, sustained-release excipient, protective agent) before formulating the complete coating. By pre-evaluating the properties and compatibility of each component, the formulation process is accelerated, reducing experimental time and costs while ensuring thorough optimization.
4Ease of operation
If dissoluble coated microneedles are used to load recombinant influenza virus hemagglutinin, then the microneedle can penetrate skin and deliver drug, but the specific serum IgG and antibody titers are slightly lower than subcutaneous injection
Solution Approach 1:
The patent optimizes parameters including coating thickness (5-50 μm), excipient composition (trehalose, maltose, cyclodextrins in specific ratios), and moisture content to enhance drug release control. These parameter changes improve the immunological response (serum IgG and antibody titers) while maintaining self-administration capability through simple patch application.
Solution Approach 2:
The patent uses a composite coating system combining water-soluble polymer with sustained-release excipients and protective agents. This composite structure enhances the immunological response by controlling drug release kinetics and improving absorption efficiency, achieving titers comparable to or exceeding subcutaneous injection while maintaining ease of self-administration.
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 multilayer structure ensures sustained release of water-soluble drugs, enhancing drug utilization and reducing administration frequency, while maintaining stability and bioavailability, and is cost-effective to produce.
Implementation Method 1
the sustained-release layer covers the needle tip... prevent drug-containing matrix from being dissolved quickly
Implementation Method 2
a delayed crosslinked sodium alginate system
Implementation Method 3
realize the substantiated release of a water-soluble microneedle active ingredient
Implementation Method 4
a near-neutral chitosan system
Data Source
AI summary
The present application discloses a coated microneedle with a multilayer structure, including a base, a needle tip on the base, and a functional coating. The functional coating includes a content including a water-soluble polymer material and an active ingredient, and a sustained-release layer wrapping the content. The sustained-release layer covers the needle tip. The coated microneedle can prevent a drug-containing matrix from being quickly dissolved and dispersed, prevent the active ingredient from exuding along with tissues at an action site, and increase the drug intake. The present application further discloses a method for preparing the coated microneedle and a microneedle patch including the coated microneedle.