Nanofluidized Supplement Formulations for Buccal Bioavailability
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Solution Overview
Problem
Existing methods for delivering biologically active agents face challenges such as degradation in the gastrointestinal tract, first-pass metabolism, low bioavailability via mucosal membranes, and difficulties in achieving targeted and stable delivery, particularly through routes like the buccal mucosa, leading to inefficiencies and potential toxicity.
Innovation Solution
The development of stable, uniform formulations using nanofluidization techniques to create submicron particle dispersions that enhance delivery and absorption through transmucosal and transdermal pathways, avoiding encapsulation and utilizing shear and impact forces to maintain molecular integrity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If biologically active agents are administered orally, then ease of administration is improved, but degradation in the gastrointestinal tract and first-pass metabolism reduce bioavailability
Solution Approach 1:
The patent changes the physical state and size parameters of the biologically active agent by converting it into nanosuspension form with particle sizes of 1-1000 nm. This parameter change enables the agent to withstand gastrointestinal degradation and first-pass metabolism while maintaining oral administration convenience, thereby resolving the contradiction between ease of administration and bioavailability
Solution Approach 2:
The patent creates a composite system consisting of the biologically active agent dispersed in an aqueous carrier fluid with stabilizing agents. This composite nanosuspension formulation protects the active agent from degradation in the gastrointestinal tract while maintaining stability, thus improving both bioavailability and ease of oral administration
2Reliability
If particle size is reduced to enhance absorption, then bioavailability is improved, but manufacturing complexity increases
Solution Approach 1:
The patent employs high-energy mixing equipment that automatically generates nanosuspension particles through intense mechanical energy input. The system self-regulates particle size reduction without requiring complex multi-step processing or specialized nanofabrication equipment, thus achieving nanoscale particle sizes while keeping manufacturing relatively simple
Solution Approach 2:
The patent replaces complex chemical or biological methods for particle size reduction with a purely mechanical approach using high-energy mixers. This substitution simplifies the manufacturing process by eliminating the need for complex chemical reactions or biological processing while achieving the desired nanoscale particle sizes for improved bioavailability
3Reliability
If high concentrations of biologically active agents are administered, then therapeutic effect is improved, but toxicity and side effects increase
Solution Approach 1:
The patent creates a localized high-concentration delivery system where the nanosuspension formulation concentrates the biologically active agent at the site of absorption (mucosal membranes). This local concentration approach achieves high therapeutic effect at the target site while maintaining lower overall systemic concentrations, thereby reducing toxicity and side effects
Solution Approach 2:
The patent uses the nanosuspension carrier system as an intermediary that controls the release and delivery of the biologically active agent. This intermediary system enables precise dosing and controlled absorption, allowing high therapeutic concentrations to be achieved at the target site while preventing excessive systemic exposure that would cause toxicity
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
These formulations provide enhanced bioavailability, controlled release, and targeted delivery of biologically active agents, ensuring higher concentrations and prolonged effects without toxicity, particularly via oral mucosal membranes.
Implementation Method 1
utilizing shear and impact forces to maintain molecular integrity
Implementation Method 2
utilizing shear and impact forces to maintain molecular integrity
Implementation Method 3
enhance delivery and absorption through transmucosal and transdermal pathways
Data Source
AI summary
A method for improving stability and/or absorption of one or more biologically active agents including preparing formulations wherein a biologically active agent is dispersed using a homogenizer and/or a nanofluidizer; and optionally: i) enriching the formulation; and/or ii) delivering the formulations to a subject whereby the biologically active agent is absorbed by said subject, and/or iii) testing the formulation to identify suitable dosing ranges using computational modeling of biomolecular pathways to determine at least one feature selected from absorption in a cell, saturation of a cell, and potential toxicity in a cell, and/or iv) testing the formulation by monitoring with a low impact, minimally intrusive heart rate variability monitoring to enable rapid determination of neurological and physiological effects of a dosage, establishing dosing levels of the biologically active agent, and/or v) defining the corresponding metabolic effects of the dosage of the biologically active agent on the subject.