Bioavailability and anticataract effects of a topical ocular drug delivery system containing disulfiram and hydroxypropyl-beta-cyclodextrin on selenite-treated rats

Current Eye Research
Siling WangChunfu Wu

Abstract

To test the effect of aqueous eye drops containing a high concentration of disulfiram (DSF) in a cyclodextrin- based drug delivery system. This system increases both the drug solubility in aqueous eye drops and the permeability of drug into the rabbit eye, by the formation of a drug-cyclodextrin inclusion complex, and so enhances the ocular bioavailability and anti-cataract effect of DSF. The DSF and hydroxypropyl-beta-cyclodextrin (HPbetaCD) inclusion (DSF/HPbetaCD) was studied using solubility methods, IR spectra and X-ray diffraction patterns. Suitable formulations for DSF eye drops were first identified by a trans-corneal penetration experiment in vitro. Finding a new p-bromophenacyl bromide (p-BPB) derivative reagent for diethyldithiocarbamic acid (DDC), which was a metabolite of DSF, allowed precise determination of the contents of DSF in aqueous humor. The ocular bioavailability was calculated by a transcorneal experiment of DSF in vivo. The lens opacity of a selenite-induced cataract in rat pups was monitored using a slit lamp with an anterior eye segment analysis system. The formation of DSF/HPbetaCD inclusion and the addition of hydroxypropylmethylcellulose (HPMC), as a penetration enhancer, played very important role...Continue Reading

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Citations

Sep 2, 2008·Pharmaceutical Research·Ripal GaudanaAshim K Mitra
Nov 25, 2014·Therapeutic Delivery·Amr ElShaerRaid G Alany
Nov 24, 2007·Biotechnology Journal·Steven S-S WangHwai-Shen Liu
Apr 18, 2012·Macromolecular Bioscience·Shengyan LiuFrank X Gu
Sep 12, 2006·Experimental Eye Research·P GeraldineP A Thomas
Mar 12, 2015·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·Yujiro HoshiHideyo Takahashi
May 27, 2021·Journal of Drug Delivery Science and Technology·László JicsinszkyGiancarlo Cravotto

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