Bioadhesive Multi-Walled Nanoparticles for Oral Drug Delivery
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Solution Overview
Problem
Current nanoparticle-based oral drug delivery systems face challenges in achieving high uptake in the gastrointestinal tract due to rapid drug release and difficulties in coating nanoparticles, which results in burst release and limited bioadhesion, hindering effective drug delivery.
Innovation Solution
Development of bioadhesive multi-walled nanoparticles with a core-shell structure, formed using a single-step sequential phase inversion method, which enhances adhesion to intestinal tissue and controlled release, thereby increasing intestinal uptake and reducing burst release.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional coating techniques are used to coat nanoparticles, then controlled release can be achieved, but the coating process becomes complex and difficult to implement due to the small size of nanoparticles
Solution Approach 1:
The patent combines the nanoparticle formation and coating processes into a single in situ multi-walled nanoparticle preparation step. The controlled release coating is formed simultaneously with the nanoparticle structure during a single phase inversion process, eliminating the need for separate coating operations and simplifying the overall manufacturing process while maintaining controlled release functionality.
2Reliability
If hydrogel-based bioadhesive polymers are used to enhance uptake, then adhesion to intestinal tissue improves, but rapid drug release occurs due to aqueous swelling
Solution Approach 1:
The patent employs composite nanoparticle structures with multiple walls or layers comprising different polymeric materials. The composite structure includes at least one bioadhesive polymer layer for intestinal tissue adhesion and at least one additional layer providing controlled release properties. This multi-layer composite architecture allows simultaneous achievement of high intestinal uptake through bioadhesion and sustained drug release without rapid burst release.
3Reliability
If multiple complicated steps are used to prepare multi-walled nanoparticles, then controlled release and bioadhesion can be achieved, but the manufacturing process becomes time-consuming and complex
Solution Approach 1:
The patent performs preliminary incorporation of multiple polymeric materials and the active agent into a single formulation system before the phase inversion process. All necessary components are pre-mixed and prepared in advance, allowing the multi-walled nanoparticle structure with controlled release and bioadhesive properties to form in a single step during phase inversion, thereby achieving complex functionality without multiple sequential manufacturing steps.
4Reliability
If bioadhesive polymer chains are used to increase transit time, then intestinal uptake improves, but the polymer chains become entangled in mucus and impede particle translocation
Solution Approach 1:
The patent applies bioadhesive properties locally to specific portions or layers of the nanoparticle structure rather than coating the entire particle surface uniformly. The in situ formation process creates multi-walled structures where bioadhesive polymer layers are positioned at specific locations optimized for intestinal tissue interaction, while other regions maintain smooth surfaces that facilitate translocation through mucus without entanglement, thus balancing adhesion and mobility.
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 bioadhesive multi-walled nanoparticles exhibit significantly higher intestinal uptake, with a total uptake increase of over 500% compared to non-bioadhesive counterparts, and controlled release profiles, improving the efficacy of drug delivery.
Implementation Method 1
formed using a single-step sequential phase inversion method
Data Source
AI summary
Nanoparticles, compositions, and methods for the improved uptake of active agents are disclosed herein. The compositions contain a monodisperse population of nanoparticles, preferably including an active agent, where the nanoparticles are formed from a polymeric material possessing specified bioadhesion characteristics. Following enteral administration, preferably oral administration, the nanoparticles exhibit total intestinal uptakes of greater than 20%, preferably greater than 45%, more preferably greater than 65%. When compared to uptake of the same compositon in the absence of the bioadhesive polymeric material, the nanoparticles have significantly increased uptake with intestinal uptake of the increased by more than 100%, preferably even greater than 500%. Further disclosed herein is a method of producing multi-walled nanoparticles, as well as methods of using thereof. Multi-walled particles prepared using the method disclosed herein are useful for controlling the release of active agents.