Preparation of ophthalmic formulations containing cilostazol as an anti-glaucoma agent and improvement in its permeability through the rabbit cornea

Journal of Oleo Science
Norio OkamotoOsamu Mimura

Abstract

To evaluate the pharmacological properties of cilostazol (CLZ), we examined its intraocular pressure (IOP) -lowering effect. CLZ is an inhibitor of Type III phosphodiesterase that increases intracellular cyclic AMP levels by restraining platelet aggregation, and has a potential protective effect against atherosclerosis. We attempted to apply it for use as an anti-glaucoma agent; however, the application of CLZ in the ophthalmic field is limited due to its poor water solubility. We attempted to enhance CLZ solubility using 2-hydroxypropyl-beta-cyclodextrin (HPbetaCD). The solubility of CLZ increased with increasing HPbetaCD concentrations, and 0.05% CLZ was dissolved in 10% HPbetaCD. Moreover, fine particle suspension of 0.5% CLZ in 5% HPbetaCD (soluble CLZ: ca. 0.027%) were prepared using a Microfluidizer, an impact-type emulsifying comminution device. In an in vitro transcorneal penetration experiment through the rabbit cornea, the CLZ penetration rate was dependent on the CLZ content of the solutions and suspensions. When a 0.05% CLZ ophthalmic solution was instilled into a rabbit eye, the absorption rate constant for CLZ into an aqueous humor was 0.0059+/-0.001 min(-1), and the elimination rate constant was 0.048+/-0.024 min...Continue Reading

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Citations

Nov 6, 2015·International Journal of Molecular Sciences·Meng MengDaojun Cheng
Dec 17, 2015·Journal of Ocular Pharmacology and Therapeutics : the Official Journal of the Association for Ocular Pharmacology and Therapeutics·Venkata Kashyap Yellepeddi, Srinath Palakurthi
Jan 18, 2018·International Journal of Molecular Sciences·Noriaki NagaiYoshikazu Shimomura
Sep 3, 2017·British Journal of Pharmacology·Sahar AwwadAlastair Lockwood
Nov 15, 2017·Drug Delivery and Translational Research·María Sebastián-MorellóAlicia López-Castellano
Jun 3, 2020·Journal of Medicinal Chemistry·Kuei-Ju ChengJing-Ping Liou

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