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Issue 37, 2019
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In vitro and in vivo evaluation of benzathine foscarnet microcrystals as a potential intravitreal drug depot

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Abstract

Sodium foscarnet is an antiviral drug against cytomegalovirus retinitis, and clinically it is used via frequent intravitreal injection which causes various ocular complications. Here we propose to use benzathine foscarnet in a new salt form with much lower aqueous solubility, and as a potential long-acting intravitreally injectable solid form for foscarnet. Benzathine foscarnet (1 : 1) microcrystals were synthesized and evaluated both in vitro and in vivo. The aqueous solubility of benzathine foscarnet was 14.2 mM, which is in between those of the currently-used sodium foscarnet and our previously-reported calcium foscarnet salt. In a rabbit model, the injected microcrystals last for about 3 weeks in the vitreous, suggesting its solubility and dissolution profile is appropriate for its intended use. However, the injected benzathine foscarnet microcrystals also caused adverse effects in vivo.

Graphical abstract: In vitro and in vivo evaluation of benzathine foscarnet microcrystals as a potential intravitreal drug depot

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Supplementary files

Article information


Submitted
25 Apr 2019
Accepted
30 Jun 2019
First published
09 Jul 2019

This article is Open Access

RSC Adv., 2019,9, 21318-21322
Article type
Paper

In vitro and in vivo evaluation of benzathine foscarnet microcrystals as a potential intravitreal drug depot

J. Wang, Y. Tao, J. Feng, Y. Niu, J. Liu and Y. Huang, RSC Adv., 2019, 9, 21318
DOI: 10.1039/C9RA03070K

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