2011
DOI: 10.1128/aac.01175-10
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Penetration of Topically Administered 0.5-Percent Caspofungin Eye Drops into Human Aqueous Humor

Abstract: Ten participants attending elective anterior segment eye surgery received 0.5% caspofungin eye drops either 1 drop hourly for 4 h or 1 drop an hour before surgery. The eye drops were generally well tolerated. In the absence of inflammation or corneal abrasion, topical caspofungin does not achieve clinically relevant concentrations.Fungal keratitis is a potentially blinding condition, with Candida, Aspergillus, and Fusarium spp. (2, 21) being the common pathogens. Current treatment for fungal keratitis is inade… Show more

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Cited by 8 publications
(5 citation statements)
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References 23 publications
(36 reference statements)
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“…32 Our group has recently reported that caspofungin 0.5% eye drops were able to penetrate into intact human eyes due to use of a more sensitive analytical assay (LLOQ = 10 ng/mL) 33 to detect caspofungin in human aqueous humor (concentrations ranging from 28.9 to 95.1 ng/mL). 34 The concentrations observed in our study, however, were mostly below the MIC 90 (0.06-2 µg/mL) required for most fungal species. 35,36 This could be the result of its large molecular weight (1213 Da) and the fact that caspofungin is highly protein bound (96.5%), 37 which limits its penetration into intact eyes.…”
Section: Caspofungin and Voriconazole For Alternaria Keratitiscontrasting
confidence: 60%
“…32 Our group has recently reported that caspofungin 0.5% eye drops were able to penetrate into intact human eyes due to use of a more sensitive analytical assay (LLOQ = 10 ng/mL) 33 to detect caspofungin in human aqueous humor (concentrations ranging from 28.9 to 95.1 ng/mL). 34 The concentrations observed in our study, however, were mostly below the MIC 90 (0.06-2 µg/mL) required for most fungal species. 35,36 This could be the result of its large molecular weight (1213 Da) and the fact that caspofungin is highly protein bound (96.5%), 37 which limits its penetration into intact eyes.…”
Section: Caspofungin and Voriconazole For Alternaria Keratitiscontrasting
confidence: 60%
“…There are not previous studies reporting the delivery of CSP because is the first time it has been applied topically in vaginal mucosa. Only a topical study of eye drops has been found in the literature [ 30 ].…”
Section: Introductionmentioning
confidence: 99%
“…Several in vitro and in vivo studies have shown promising results with respect to the safety, efficacy and dosage of these agents [143,144]. The studies done in an animal model [145] as well as in human volunteers [146] on the ocular penetration of caspofungin have shown that its penetration is better in an inflamed cornea or if the epithelial layer is denuded. Caspofungin used in concentrations of 1%/0.5% in solution for topical use and intravenous (IV) formulation for systemic use have been reported to have an adjunctive role in the management of ocular fungal infections caused by Alternaria [147,148], voriconazole refractory Candida albicans keratitis [149] and recurrent Candida parapsilosis keratitis [150].…”
Section: Echinocandinsmentioning
confidence: 99%