Radiopaque Embolization Microspheres With Better Suspendability
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Solution Overview
Problem
Existing radiopaque embolization microspheres incorporating halogenated radiopaque monomers are prone to aggregation, catheter blockage, and adherence to catheter walls due to increased hydrophobicity and rigidity, compromising their suspendability and injectability in suspension mixtures.
Innovation Solution
A novel halogenated radiopaque monomer (MAETIP) with iodine atoms in specific positions on the phenyl ring reduces spatial accessibility, enhancing the hydrophilicity and flexibility of the microspheres, preventing aggregation and improving suspendability and injectability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If halogenated radiopaque monomers are incorporated into embolization microspheres, then radiopacity is improved, but hydrophobicity increases and suspendability deteriorates
Solution Approach 1:
The patent applies local quality by positioning iodine atoms at specific locations (2, 4, and 6 positions) on the phenyl ring rather than uniformly distributing them. This localized arrangement optimizes radiopacity in specific regions while maintaining overall hydrophilicity of the monomer structure, thereby preserving suspendability despite the presence of radiopaque halogen atoms.
Solution Approach 2:
The patent changes the structural parameters of the radiopaque monomer by selecting specific substitution patterns on the phenyl ring. By modifying the positional parameters of iodine atoms and the nature of substituent groups, the monomer achieves an optimal balance between radiopacity and hydrophilicity, resolving the contradiction between these two properties.
2Reliability
If halogenated radiopaque monomers are incorporated into embolization microspheres, then radiopacity is improved, but aggregation increases
Solution Approach 1:
The specific local arrangement of iodine atoms at positions 2, 4, and 6 on the phenyl ring creates a distributed radiopaque structure that prevents localized hydrophobic clustering. This local quality distribution ensures uniform radiopacity while maintaining stability against aggregation throughout the microsphere composition.
Solution Approach 2:
The patent creates a composite monomer structure combining radiopaque iodine atoms with hydrophilic substituent groups on the phenyl ring. This composite design integrates the radiopacity function with hydrophilic properties that prevent aggregation, achieving both radiographic visibility and compositional stability simultaneously.
3Reliability
If halogenated radiopaque monomers are incorporated into embolization microspheres, then radiopacity is improved, but catheter blockage increases
Solution Approach 1:
The localized positioning of iodine atoms at specific phenyl ring positions creates a balanced distribution of radiopaque and hydrophilic characteristics. This prevents excessive hydrophobicity that would cause catheter adhesion and blockage, while maintaining sufficient radiopacity for imaging guidance during catheter-based embolization procedures.
Solution Approach 2:
The patent converts the potentially harmful hydrophobicity of halogenated monomers into a benefit by strategically positioning iodine atoms and selecting appropriate substituent groups. This transformation maintains the radiopaque advantage while eliminating the harmful catheter blockage effect, turning a disadvantage into a favorable property.
Data Source
AI summary
The present invention relates to a compound of the following formula (A) mainly for use as a radiopaque monomer: The invention further relates to radiopaque embolisation microspheres based at least on: 20% to 90% hydrophilic monomer; 5% to 50% compound of formula (A); 1% to 15% non-biodegradable hydrophilic crosslinking monomer; and −0.1% to 10% transfer agent. The invention also relates to a pharmaceutical composition comprising at least one embolisation microsphere according to the invention, in association with a pharmaceutically acceptable carrier, advantageously for parenteral administration. The invention further relates to a kit comprising a pharmaceutical composition according to the invention in association with a pharmaceutically acceptable carrier for parenteral administration, and to an injection means.