Microinjectors for Oral Macromolecule Delivery
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
The oral delivery of macromolecules, such as insulin and anti-TNF-α drugs, is challenging due to degradation by the gastrointestinal tract's acid and digestive enzymes, and limited absorption across epithelial cell junctions, with no FDA-approved method for intraluminal injection that avoids GI tract blockage.
Innovation Solution
Development of microinjection devices with autonomous actuators and microinjectors, coated with materials like chitosan and poly(lacto-co-glycolic acid), capable of penetrating the GI mucosa and delivering drugs through the epithelial cell junctions, activated by physiological cues like temperature and pH, housed in an enteric capsule for safe passage through the stomach.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If chemical modifications or encapsulation methods are used to improve macromolecule diffusion, then absorption capability is improved, but treatment effectiveness remains limited due to degradation and poor permeation
Solution Approach 1:
The invention extracts the macromolecule from the harmful GI environment by using microinjectors to deliver the drug directly through the epithelial cell junctions into the bloodstream, bypassing the degradation-prone GI lumen and avoiding the need for chemical modifications or encapsulation
Solution Approach 2:
The microinjector acts as an intermediary device that bridges the GI lumen and the bloodstream, enabling direct translocation of macromolecules across the epithelial barrier without chemical modification, thereby solving both absorption and effectiveness problems simultaneously
2Reliability
If intraluminal injection is used to deliver macromolecules across epithelial junctions, then bioavailability is improved, but device size must be small enough to avoid GI tract blockage
Solution Approach 1:
The injection system is segmented into multiple microinjectors (e.g., arrays of 6-12 microinjectors per device) that are small enough to navigate the GI tract without blockage, while collectively delivering sufficient drug payload to achieve therapeutic bioavailability
Solution Approach 2:
The invention replaces complex mechanical injection systems with autonomous actuators that use environmental triggers (pH change, temperature) to activate injection, eliminating the need for large mechanical components while maintaining injection capability
3Ease of operation
If oral delivery is used to improve compliance and reduce costs, then treatment accessibility is improved, but macromolecules are degraded by acid and digestive enzymes
Solution Approach 1:
The microinjector is pre-loaded with the macromolecule in a protected state and remains inert during oral passage through the stomach, then activates only after reaching the target site in the intestine, preventing premature degradation and maintaining drug integrity
Solution Approach 2:
The invention extracts the macromolecule from the harmful GI environment by delivering it directly through the epithelial barrier into the bloodstream, bypassing the degradation-prone GI lumen entirely
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 devices enable efficient and safe delivery of macromolecular drugs like insulin across the GI tract, increasing bioavailability and systemic exposure, with no adverse effects on the GI tract, and can be administered orally or rectally without causing blockage.
Implementation Method 1
autonomous actuator and one or more microinjectors operably connected to the autonomous actuator
Implementation Method 2
The protective coating comprises poly-methacrylate, alginate, methylcellulose, or a combination thereof
Implementation Method 3
at least a portion of the one or more microinjectors (e.g., the patch on the tip of the microinjectors) further comprises chitosan
Data Source
AI summary
The present disclosure provides microscale devices, systems, and methods thereof for the delivery of therapeutic and prophylactic active agents (e.g., macromolecules).