Ionic Liquid Nox Inhibitor Formulation for Brain Delivery
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Solution Overview
Problem
Existing Nox inhibitors face issues of negligible solubility in aqueous solvents, leading to reduced bioavailability and therapeutic efficacy, particularly for neurological diseases like Parkinson's disease, due to their low solubility and difficulty in crossing the blood-brain barrier.
Innovation Solution
Development of an IL-based formulation of a specific Nox1 and Nox4 inhibitor, 3-cyclohexyl-5-(2,4-dihydroxybenzylidene)-1-methyl-2-thiohydantoin, in the form of cholinium 3-cyclohexyl-5-(2,4-dihydroxybenzylidene)-1-methyl-2-thiohydantonate, which enhances solubility and bioavailability, allowing for neuroprotective therapy.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If Nox inhibitors are used in solid state or conventional formulations, then they can be manufactured and stored, but their solubility in aqueous solvents is negligible, leading to low bioavailability and reduced therapeutic efficacy
Solution Approach 1:
The patent transforms the physical and chemical parameters of the Nox inhibitor by converting it into an ionic liquid formulation. This involves changing the molecular state from solid/conventional to ionic liquid, which fundamentally alters solubility characteristics. The ionic liquid formulation achieves high aqueous solubility while maintaining the inhibitor's pharmacological activity, directly resolving the contradiction between solubility and therapeutic efficacy
Solution Approach 2:
The patent creates a composite ionic liquid system by combining the Nox inhibitor molecule with specific ionic liquid components. This composite formulation integrates the pharmacologically active inhibitor with ionic liquid structures that provide enhanced solubility, bioavailability, and neurological tissue penetration properties, thereby achieving both high solubility and maintained therapeutic efficacy
2Reliability
If conventional drug formulations are used, then manufacturing is straightforward, but the drugs have difficulty crossing the blood-brain barrier, limiting their effectiveness for neurological diseases
Solution Approach 1:
The patent changes the physical state and chemical properties of the drug formulation to ionic liquid, which possesses unique characteristics including enhanced ability to cross biological membranes and the blood-brain barrier. This parameter transformation enables effective delivery to neurological targets without requiring complex delivery systems
Solution Approach 2:
The ionic liquid formulation acts as an intermediary vehicle that facilitates the transport of the Nox inhibitor across the blood-brain barrier. The ionic liquid structure serves as a mediator that enables penetration into neurological tissues while maintaining the integrity and activity of the inhibitor molecule, achieving effective brain delivery without excessive formulation complexity
Data Source
AI summary
The present disclosure relates to an ionic liquid (IL)-based formulation comprising inhibitors of NADPH oxidases enzymes (Nox's), preferably isoforms 1 and 4, in particular the specific inhibitor 3-cyclohexyl-5-(2,4-dihydroxybenzylidene)-1-methyl-2-thiohydantoin, for the treatment, therapy or prevention of neurological diseases, in particular Parkinson's diseases.