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Supramolecular Synthon Strategy via Organic Salt Formation for Developing Topical Gel From Rhein: Synthesis,
Nabanita Roy1, Subhajit Ghosh1, Agnibha Das1
1School of Chemical Sciences, Indian Association for the Cultivation of Science (IACS), Kolkata, West Bengal, India.
Chemistry, an Asian Journal
|May 6, 2026
Summary
Researchers developed a novel vehicle-free drug delivery (VFDD) system by transforming the hydrophobic drug Rhein into a supramolecular gel. This gel, RHC6, shows promise for topical antimicrobial applications.
Area of Science:
- Materials Science
- Pharmaceutical Sciences
- Biomedical Engineering
Background:
- Rhein possesses significant biological advantages but its hydrophobicity limits clinical applications.
- Developing topical vehicle-free drug delivery (VFDD) systems is crucial for efficient drug administration.
- Designing effective gelators for drug molecules remains a significant challenge.
Purpose of the Study:
- To overcome Rhein's hydrophobicity by creating supramolecular gels for VFDD.
- To synthesize and characterize novel Rhein-based primary ammonium monocarboxylate (PAM) salts.
- To evaluate the gelation, biological activity, and material properties of the synthesized salts.
Main Methods:
- Synthesized 11 PAM salts of Rhein by reacting it with various alkyl amines.
- Assessed gelation properties in aqueous solvent (DMSO/water).
- Determined single-crystal structures of five PAM salts to correlate with gelation behavior.
- Evaluated cell viability using normal cell lines and antibacterial activity against Gram-positive and Gram-negative bacteria, including MRSA.
Main Results:
- All 11 synthesized PAM salts exhibited gelation in aqueous media.
- Single-crystal structures provided insights into the gelation mechanism.
- RHC6 demonstrated excellent cell viability and potent antibacterial activity against a broad spectrum of bacteria, including MRSA.
- RHC6 gel displayed favorable material properties like rheoreversibility and patch-forming ability.
Conclusions:
- The primary ammonium monocarboxylate (PAM) synthon effectively transforms hydrophobic Rhein into supramolecular gels.
- RHC6 represents a promising antimicrobial agent for vehicle-free topical drug delivery.
- The developed VFDD system offers a potential advancement for treating skin infections and other topical conditions.
