Bis(Hydroxy Benzylidene) Cyclic-Ketone Tetra-Aza Corand Encapsulation
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Existing drug delivery systems face challenges with low aqueous solubility and high toxicity of therapeutic agents like Flutamide, Nilutamide, Gemcitabine, Dasatinib, and Cis-platin, leading to poor pharmacological profiles and systemic toxicity.
Innovation Solution
Development of bis(hydroxybenzylidene) cyclic ketone based tetra-aza corands that encapsulate these agents via non-covalent interactions, forming a three-dimensional cavity for controlled delivery and reducing toxicity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If therapeutic agents are administered directly to achieve high concentration at target site, then efficacy is improved, but systemic toxicity increases
Solution Approach 1:
The patent employs a host-guest inclusion complex where the therapeutic agent (guest) is encapsulated within the tetra-aza corand cavity (host). This nested structure allows the drug to be carried to the target site protected within the macrocycle, reducing premature release and systemic toxicity while maintaining therapeutic efficacy at the destination.
Solution Approach 2:
The tetra-aza corand acts as an intermediary carrier between the therapeutic agent and the biological system. It facilitates controlled delivery by forming stable inclusion complexes that protect the drug during transport and enable targeted release, thereby reducing direct contact with healthy tissues and minimizing toxicity.
2Duration of action of moving object
If liposome encapsulated drugs are used to extend local effect, then duration of action is improved, but diffusion rate into non-required tissue increases
Solution Approach 1:
The tetra-aza corand macrocycles exhibit specific cavity sizes and chemical environments tailored for selective drug encapsulation. The local chemical properties within the cavity (hydrophobic/hydrophilic character, cavity size) are optimized to maintain the drug in a controlled state, preventing unwanted diffusion while extending local therapeutic effect.
3Stability of the object's composition
If conventional encapsulation methods are used for pharmaceutical storage, then stability is improved, but delivery time to patient increases
Solution Approach 1:
The patent creates composite inclusion complexes combining the therapeutic agent with tetra-aza corand macrocycles. This composite structure provides enhanced stability during storage while maintaining drug availability for rapid delivery, as the drug remains accessible within the macrocycle cavity without requiring complex storage conditions.
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 tetra-aza corands provide a controlled and targeted delivery of therapeutic agents, minimizing systemic toxicity and enhancing local efficacy by encapsulating drugs like Flutamide, Nilutamide, Gemcitabine, Dasatinib, and Cis-platin, while maintaining solubility and stability.
Implementation Method 1
encapsulate these agents via non-covalent interactions, forming a three-dimensional cavity for controlled delivery
Data Source
AI summary
A tetra-aza corand compound of formula (Ia) and compound of formula (Ib) and salts thereof. The tetra-aza corand of formula (Ia) and (Ib) of the present invention relates to novel corand entity having a substantially enclosed volume and a framework structure, the compounds are designed as therapeutic carriers for molecule therapeutics delivery and pharmaceutical compositions thereof.