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J Ocul Pharmacol Ther. 2018 Jul/Aug;34(6):460-467. doi: 10.1089/jop.2017.0139. Epub 2018 May 24.

Comparison of the Ocular Penetration and Pharmacokinetics Between Natamycin and Voriconazole After Topical Instillation in Rabbits.

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1
Shenyang Xingqi Pharmaceutical Co., Ltd., Shenyang, People's Republic of China .

Abstract

PURPOSE:

To investigate the ocular penetration of natamycin (NAT) and voriconazole (VRC) after topical instillation in New Zealand white rabbits using simplified liquid chromatography-tandem mass spectrometry (LC-MS/MS) and high-performance liquid chromatography.

METHODS:

Seventy-eight healthy rabbits were randomly divided into 3 groups. In the first 2 groups, 72 rabbits were used for single-dose testing (36 for NAT, 36 for VRC), in which 50 μL of 5.0% NAT or 1.0% VRC was instilled into the rabbits' left eyes. In the 3rd group, 6 rabbits were used for repeated-dose testing in which 50 μL of 5.0% NAT was instilled into their left eyes 12 times (once per hour) during the daytime. These animals were sacrificed immediately to collect their aqueous humors and corneas.

RESULTS:

After a single topical instillation, the highest concentrations in the cornea and aqueous humor for VRC were 34.1 μg/g and 14.7 μg/mL, respectively. The permeability ratios of aqueous/cornea were from 0.1 to 1.26. The highest concentrations in cornea and aqueous humor for NAT were 299.3 ng/g and 27.1 ng/mL, respectively. The permeability ratios of aqueous/cornea were from 0.02 to 0.23. In the repeated-dose group, the NAT concentrations in the cornea and aqueous humor were 10,569 ng/g and 54.4 ng/mL, respectively. The permeability ratio was as low as 0.0051.

CONCLUSION:

The better corneal penetration of VRC suggests that it is more suitable for deep corneal fungal infections than NAT via topical ocular administration.

KEYWORDS:

LC-MS/MS; natamycin; penetration; pharmacokinetics; voriconazole

PMID:
29792548
DOI:
10.1089/jop.2017.0139

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