Chrysin Directing an Enhanced Solubility through the Formation of a Supramolecular Cyclodextrin–Calixarene Drug Delivery System: A Potential Strategy in Antifibrotic Diabetes Therapeutics.

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HERMENEAN, Anca, DOSSI, Eleftheria, HAMILTON, Alexander, TROTTA, Maria Consiglia, RUSSO, Marina, LEPRE, Caterina Claudia, SAJTOS, Csilla, RUSZNYÁK, Ágnes, VÁRADI, Judit, BÁCSKAY, Ildikó, BUDAI, István, D’AMICO, Michele and FENYVESI, Ferenc (2024). Chrysin Directing an Enhanced Solubility through the Formation of a Supramolecular Cyclodextrin–Calixarene Drug Delivery System: A Potential Strategy in Antifibrotic Diabetes Therapeutics. Pharmaceuticals, 17 (1): 107. [Article]

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Abstract
Calixarene 0118 (OTX008) and chrysin (CHR) are promising molecules for the treatment of fibrosis and diabetes complications but require an effective delivery system to overcome their low solubility and bioavailability. Sulfobutylated β-cyclodextrin (SBECD) was evaluated for its ability to increase the solubility of CHR by forming a ternary complex with OTX008. The resulting increase in solubility and the mechanisms of complex formation were identified through phase-solubility studies, while dynamic light-scattering assessed the molecular associations within the CHR-OTX008-SBECD system. Nuclear magnetic resonance, differential scanning calorimetry, and computational studies elucidated the interactions at the molecular level, and cellular assays confirmed the system’s biocompatibility. Combining SBECD with OTX008 enhances CHR solubility more than using SBECD alone by forming water-soluble molecular associates in a ternary complex. This aids in the solubilization and delivery of CHR and OTX008. Structural investigations revealed non-covalent interactions essential to complex formation, which showed no cytotoxicity in hyperglycemic in vitro conditions. A new ternary complex has been formulated to deliver promising antifibrotic agents for diabetic complications, featuring OTX008 as a key structural and pharmacological component.
More Information
Official URL:
https://www.mdpi.com/1424-8247/17/1/107
Uncontrolled Keywords:
1115 Pharmacology and Pharmaceutical Sciences; 3214 Pharmacology and pharmaceutical sciences

Identifiers

Identification Number:
10.3390/ph17010107
ORCID for Anca Hermenean: ORCID iD orcid.org/0000-0001-8510-6653
ORCID for Maria Consiglia Trotta: ORCID iD orcid.org/0000-0001-9813-5955
ORCID for Ágnes Rusznyák: ORCID iD orcid.org/0000-0002-8837-7499
ORCID for Judit Váradi: ORCID iD orcid.org/0000-0003-1885-164X
ORCID for Ildikó Bácskay: ORCID iD orcid.org/0000-0001-8663-2890
ORCID for István Budai: ORCID iD orcid.org/0000-0002-8966-3817
ORCID for Michele D’Amico: ORCID iD orcid.org/0000-0002-6899-0595
ORCID for Ferenc Fenyvesi: ORCID iD orcid.org/0000-0003-2890-0783

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Item Type:
Article
SWORD Depositor:
Symplectic Elements
Depositing User:
Symplectic Elements
Date Deposited:
23 Jan 2024 11:06
Last Modified:
18 Dec 2024 17:51
Date of first compliant deposit:
22 January 2024
Date of first compliant Open Access:
23 January 2024
Version of first compliant deposit:
Author Accepted Manuscript
URI:
https://shura.shu.ac.uk/id/eprint/33048
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