RT Journal Article
T1 Biopharmaceutical Assessment of Dexamethasone Acetate-Based Hydrogels Combining Hydroxypropyl Cyclodextrins and Polysaccharides for Ocular Delivery
A1 Mazet, Roseline
A1 García Otero, Xurxo
A1 Choisnard, Luc
A1 Wouessidjewe, Denis
A1 Verdoot, Vincent
A1 Bossard, Frédéric
A1 Díaz Tomé, Victoria
A1 Blanc Marquis, Véronique
A1 Otero Espinar, Francisco Javier
A1 Fernández Ferreiro, Anxo
A1 Gèze, Annabelle
K1 Dexamethasone acetate
K1 Cyclodextrins
K1 Eye drops
K1 Hydrogels
K1 Rheology
K1 Cytotoxicity studies
K1 Transcorneal permeation
K1 Radiolabeled ocular biopermanence
AB We previously developed two optimized formulations of dexamethasone acetate (DXMa) hydrogels by means of special cubic mixture designs for topical ocular administration. These gels were elaborated with hydroxypropyl-β-CD (HPβCD) and hydroxypropyl-γ-CD (HPγCD) and commercial hydrogels in order to enhance DXMa water solubility and finally DXMa’s ocular bioavailability and transcorneal penetration. The main objective of this study was to characterize them and to evaluate in vitro, ex vivo, and in vivo their safety, biopermanence, and transcorneal permeation. Gels A and B are Newtonian fluids and display a viscosity of 13.2 mPa.s and 18.6 mPa.s, respectively, which increases their ocular retention, according to the in vivo biopermanence study by PET/CT. These hydrogels could act as corneal absorption promoters as they allow a higher transcorneal permeation of DXMa through porcine excised cornea, compared to DEXAFREE® and MAXIDEX®. Cytotoxicity assays showed no cytotoxic effects on human primary corneal epithelial cells (HCE). Furthermore, Gel B is clearly safe for the eye, but the effect of Gel A on the human eye cannot be predicted. Both gels were also stable 12 months at 25 °C after sterilization by filtration. These results demonstrate that the developed formulations present a high potential for the topical ocular administration of dexamethasone acetate
PB MDPI
YR 2020
FD 2020
LK http://hdl.handle.net/10347/23816
UL http://hdl.handle.net/10347/23816
LA eng
NO Mazet, R.; García-Otero, X.; Choisnard, L.; Wouessidjewe, D.; Verdoot, V.; Bossard, F.; Díaz-Tomé, V.; Blanc-Marquis, V.; Otero-Espinar, F.-J.; Fernandez-Ferreiro, A.; Gèze, A. Biopharmaceutical Assessment of Dexamethasone Acetate-Based Hydrogels Combining Hydroxypropyl Cyclodextrins and Polysaccharides for Ocular Delivery. Pharmaceutics 2020, 12, 717
NO This work was supported by Labex ARCANE (ANR-11-LABX-0003-01) and Institut de Chimie Moléculaire de Grenoble (FR 2607) and the Glyco@Alps program (ANR-15-IDEX-02). A.F.-F. acknowledges the support obtained from the Instituto de Salud Carlos III (ISCIII) through its research grants (JR18/00014). X.G.-O. acknowledges the financial support of the IDIS (Health Research Institute of Santiago de Compostela) (predoctoral research fellowships)
DS Minerva
RD 30 abr 2026