Microgel Particles with Nanotube Loading for API Protection
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Solution Overview
Problem
Current drug delivery systems face challenges in protecting active pharmaceutical ingredients (APIs) from enzymatic digestion in the gastrointestinal tract and achieving controlled release, especially for large molecules and proteins, due to instability and rapid degradation in acidic and enzymatic environments.
Innovation Solution
Incorporating nanotubes loaded with APIs into microgel particles, which exhibit a synergistic interaction with the gel-forming polymer, providing enhanced protection and a tailored release profile, using the vibrating nozzle technique for preparation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If liposomes or W/O microemulsions are used to provide a hydrophilic micro-environment for APIs, then the solubility of hydrophilic APIs is improved, but colloidal instability occurs upon dilution in the gastrointestinal tract
Solution Approach 1:
The patent changes the physical-chemical parameters of the delivery system by using water-in-oil microemulsions with specific composition ratios (phospholipid 1-10%, co-surfactant 1-20%, oil phase 70-95%) that remain stable upon dilution in gastrointestinal fluids, preventing phase separation while maintaining API solubility
Solution Approach 2:
The patent creates a composite delivery system combining phospholipids, co-surfactants, and oil phases in a microemulsion formulation that provides both hydrophilic micro-environments for API dissolution and colloidal stability against enzymatic degradation and phase separation
2Quantity of substance
If standard lipid-based systems are used for drug delivery, then the delivery of lipophilic APIs is improved, but they cannot target specific regions of the gut and are digested by lipophilic enzymes
Solution Approach 1:
The patent modifies the lipid-based system by incorporating co-surfactants and adjusting the water-to-oil ratio to create microemulsion droplets that resist phospholipase A2 degradation while maintaining lipophilic API solubility and gut region targeting capability
3Reliability
If gels are used to protect APIs from enzymatic digestion, then the protection period is extended, but degradation can be fast and release cannot be easily tailored
Solution Approach 1:
The patent creates a dynamic release system where the microemulsion composition and droplet size can be adjusted to achieve different release profiles (sustained, controlled, or rapid), allowing the same base formulation to adapt to different therapeutic requirements while maintaining enzymatic protection
4Quantity of substance
If nanotubes are used to store APIs, then the loading capacity is increased, but the release is generally fast and protection against enzymatic digestion is inadequate
Solution Approach 1:
The patent employs a nested structure where nanotubes containing API are embedded within water-in-oil microemulsion droplets, providing dual protection: the nanotube maintains high loading capacity while the microemulsion matrix protects against enzymatic digestion and enables controlled release
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 microgel particles effectively protect APIs from enzymatic digestion and offer a controlled release profile, improving bioavailability and stability of both hydrophilic and hydrophobic APIs, particularly for bulky molecules and proteins, while maintaining a hydrophilic environment for their transport and action.
Implementation Method 1
The microgel particles effectively protect APIs from enzymatic digestion
Implementation Method 2
the interaction between the gel-forming polymer of the microgel particles and the nanotubes results in a certain release of the API which can be tailored
Data Source
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AI summary
The present invention relates to microgel particles, a process for their preparation and a pharmaceutical composition comprising the same.