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Impact of high cyclodextrins concentrations on ocular safety and surface permanence.

Created on 30 Jul 2026

Authors

Victoria Díaz-Tomé, Xurxo García-Otero, Carlos Bendicho-Lavilla, Vicente Domínguez-Arca, Selene Cuello-Rodríguez, Pablo Aguiar, Anxo Fernández-Ferreiro, Francisco J Otero-Espinar

Published in

Drug delivery and translational research. Jul 29, 2026. Epub Jul 29, 2026.

Abstract

Cyclodextrins (CDs) have been widely explored in ophthalmic formulations to enhance the bioavailability of poorly water-soluble drugs. While their ocular safety has been demonstrated in several studies, limited research has addressed the effects of CD concentration on both mucoadhesion and ocular tolerance. This study aimed to evaluate corneal alterations caused by high concentrations of various CDs at the original pH of the solutions and after adjustment to pH 7.4. Corneal toxicity was assessed using the Bovine Corneal Opacity and Permeability (BCOP) test and the Hen's Egg Test Chorioallantoic Membrane (HET-CAM) assay exhibiting ocular safety, except αCD at both pH conditions and RMβCD solution at original acidic pH. Additionally, the mucoadhesive properties of CDs at the corneal level were analysed in vivo via Positron Emission Tomography (PET) displayed significant mucoadhesive properties, prolonging retention time on the ocular surface. Further insights into CD-mucin interactions were obtained through Isothermal Titration Calorimetry (ITC) revealing different interaction mechanisms between CDs and mucin. These findings highlight the potential of CDs in ophthalmic drug delivery, offering a promising strategy for improving ocular drug bioavailability in the eye of ophthalmic formulations, provided their concentration and physicochemical properties are optimized.

PMID:
42527778
Bibliographic data and abstract were imported from PubMed on 30 Jul 2026.

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