Cyclodextrin-polysaccharide-based, in situ-gelled system for ocular antifungal delivery

Anxo Fernández-Ferreiro; Noelia Fernández Bargiela; María Santiago Varela; Maria Gil Martínez; Maria Pardo; Antonio Piñeiro Ces; José Blanco Méndez; Miguel González Barcia; Maria Jesus Lamas; FranciscoJ Otero-Espinar

doi:10.3762/bjoc.10.308

Cyclodextrin-polysaccharide-based, in situ-gelled system for ocular antifungal delivery

Beilstein J Org Chem. 2014 Dec 8:10:2903-11. doi: 10.3762/bjoc.10.308. eCollection 2014.

Affiliations

¹ Pharmacy and Pharmaceutical Technology Department, Faculty of Pharmacy, University of Santiago de Compostela (USC), Praza Seminario de Estudos Galegos s/n, Santiago de Compostela, 1570, Spain ; Pharmacy Department, Xerencia de Xestión Integrada de Santiago de Compostela, SERGAS, Travesía Choupana s/n, Santiago de Compostela, 15706, Spain.
² Pharmacy and Pharmaceutical Technology Department, Faculty of Pharmacy, University of Santiago de Compostela (USC), Praza Seminario de Estudos Galegos s/n, Santiago de Compostela, 1570, Spain.
³ Ophthalmology Department, Hospital de Conxo, Xerencia de Xestión Integrada de Santiago de Compostela, SERGAS, Rua Ramón Baltar s/n, Santiago de Compostela, 15706, Spain.
⁴ Grupo Obesidomica, Instituto de Investigación Sanitaria (IDIS-ISCIII), SERGAS, Travesía da Choupana s/n, Santiago de Compostela, 15706, Spain.
⁵ Pharmacy Department, Xerencia de Xestión Integrada de Santiago de Compostela, SERGAS, Travesía Choupana s/n, Santiago de Compostela, 15706, Spain.
⁶ Pharmacy and Pharmaceutical Technology Department, Faculty of Pharmacy, University of Santiago de Compostela (USC), Praza Seminario de Estudos Galegos s/n, Santiago de Compostela, 1570, Spain ; Industrial Pharmacy Institute, Faculty of Pharmacy, University of Santiago de Compostela (USC), Praza Seminario de Estudos Galegos s/n, Santiago de Compostela, 15701, Spain.

Abstract

Fluconazole was studied with two different hydrophilic cyclodextrins (hydroxypropyl-β-cyclodextrin (HPBCD) and sulfobutyl ether-β-cyclodextrin (SBECD)) for the formation of inclusion complexes. HPBCD and SBECD showed low cell cytotoxicity in human keratocytes as assessed by the label-free xCELLigence system for real-time monitoring. The fluconazole-HPBCD complex was incorporated into an ion-sensitive ophthalmic gel composed of the natural polysaccharides gellan gum and κ-carrageenan. This system showed good bioadhesive properties and effective control of fluconazole release.

Keywords: cyclodextrins; eye drops; fluconazole; hydroxypropyl-β-cyclodextrin; sulfobutylether-β-cyclodextrin.