Iontophoresis enhances voriconazole antifungal potency and corneal penetration

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dc.creatorGelfuso, Guilherme Martins
dc.creatorNunes, Ricardo Ferreira
dc.creatorDalmolin, Luciana Facco
dc.creatorRé, Ana Carolina dos Santos
dc.creatorSantos, Giselly de Almeida dos
dc.creatorSá, Fernando Augusto Pires de
dc.creatorCunha Filho, Marcilio Sérgio Soares da
dc.creatorAlonso, Antonio
dc.creatorMendanha Neto, Sebastião Antônio
dc.creatorAnjos, Jorge Luiz Vieira dos
dc.creatorAires, Carolina Patrícia
dc.date.accessioned2023-11-24T15:06:43Z
dc.date.available2023-11-24T15:06:43Z
dc.date.issued2020
dc.description.abstractStrategies to enhance corneal penetration of voriconazole (VOR) could improve the treatment of fungal keratitis. Here, we evaluated the use of iontophoresis for ocular VOR delivery from either: (i) a cyclodextrin inclusion complex (CD VOR), (ii) a liposome (LP VOR), and (iii) a chitosan-coated liposome (LP VOR CS). LP VOR CS presented mean diameter of 139.2 ± 1.3 nm and zeta potential equal to + 3.3 ± 1.5 mV compared to 134.6 ± 1.7 and −8.2 ± 3.0 mV of LP VOR, which, together with mucin mucoadhesion study, confirmed chitosan-coating. Both drug and liposomal formulations were stable under the influence of an applied electric current. Interestingly, in vitro studies in Candida glabrata culture indicated a decrease in VOR MIC values following iontophoresis (from 0.28 to 0.14 µg/mL). Iontophoresis enhanced drug penetration into the cornea. After 10 min of a 2 mA/cm2 applied current, corneal retained amounts were 45.4 ± 11.2, 30.4 ± 2.1 and 30.6 ± 2.9 µg/cm2 for, respectively, CD VOR, LP VOR, and LP VOR CS. In conclusion, iontophoresis increases drug potency and enhances drug penetration into the cornea, showing potential to be used as “an emergency burst delivery approach”.
dc.description.resumoStrategies to enhance corneal penetration of voriconazole (VOR) could improve the treatment of fungal keratitis. Here, we evaluated the use of iontophoresis for ocular VOR delivery from either: (i) a cyclodextrin inclusion complex (CD VOR), (ii) a liposome (LP VOR), and (iii) a chitosan-coated liposome (LP VOR CS). LP VOR CS presented mean diameter of 139.2 ± 1.3 nm and zeta potential equal to + 3.3 ± 1.5 mV compared to 134.6 ± 1.7 and −8.2 ± 3.0 mV of LP VOR, which, together with mucin mucoadhesion study, confirmed chitosan-coating. Both drug and liposomal formulations were stable under the influence of an applied electric current. Interestingly, in vitro studies in Candida glabrata culture indicated a decrease in VOR MIC values following iontophoresis (from 0.28 to 0.14 µg/mL). Iontophoresis enhanced drug penetration into the cornea. After 10 min of a 2 mA/cm2 applied current, corneal retained amounts were 45.4 ± 11.2, 30.4 ± 2.1 and 30.6 ± 2.9 µg/cm2 for, respectively, CD VOR, LP VOR, and LP VOR CS. In conclusion, iontophoresis increases drug potency and enhances drug penetration into the cornea, showing potential to be used as “an emergency burst delivery approach”.
dc.identifier.citationGELFUSO, Guilherme M. et al. Iontophoresis enhances voriconazole antifungal potency and corneal penetration. International Journal of Pharmaceutics, Amsterdam, v. 576, e118991, 2020. DOI: 10.1016/j.ijpharm.2019.118991. Disponível em: https://www.sciencedirect.com/science/article/pii/S037851731931052X?via%3Dihub. Acesso em: 12 set. 2023.
dc.identifier.doi10.1016/j.ijpharm.2019.118991
dc.identifier.issn0378-5173
dc.identifier.issne- 1873-3476
dc.identifier.urihttps://www.sciencedirect.com/science/article/pii/S037851731931052X?via%3Dihub
dc.language.isoeng
dc.publisher.countryHolanda
dc.publisher.departmentInstituto de Física - IF (RMG)
dc.rightsAcesso Restrito
dc.subjectCandida glabrata
dc.subjectFungal keratitis
dc.subjectLiposome
dc.subjectOcular iontophoresis
dc.titleIontophoresis enhances voriconazole antifungal potency and corneal penetration
dc.typeArtigo

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