Chitosan/Hydroxyethyl cellulose inserts for sustained-release of dorzolamide for glaucoma treatment: in vitro and in vivo evaluation

Publication date: Available online 3 September 2019Source: International Journal of PharmaceuticsAuthor(s): Juçara R. Franca, Giselle Foureaux, Leonardo L. Fuscaldi, Tatiana G. Ribeiro, Rachel O. Castilho, Maria I. Yoshida, Valbert N. Cardoso, Simone O.A. Fernandes, Sebastião Cronemberger, José Carlos Nogueira, Anderson J. Ferreira, André A.G. FaracoAbstractEye drops containing hydrophilic drugs are commonly used to reduce intraocular pressure (IOP) in glaucoma patients, but compliance to the treatement is commonly reduced by frequent dosing and eventual systemic side effects. Sustained-release drug delivery systems, such as ocular inserts, can reduce dosing, limit systemic exposure, reduce side effects, and, then, improve patient adherence to therapy. Here, we developed and evaluated chitosan/hydroxyethyl cellulose-based ocular inserts for sustained release of dorzolamide, a hydrophilic drug. Dorzolamide inserts (DI) were produced by solvent/casting method and characterized by various physicochemical techniques. Pharmacokinetics studies were performed using scintigraphic images and ex vivo biodistribution. The effectiveness of inserts was tested in glaucomatous rats. Characterization studies showed that the drug strongly interacted with the polymeric matrix, but in vitro results showed that DI took only 3 h to release 75% of dorzolamide entraped. However, scintigraphic images and ex vivo biodistribution studies revealed that more than 50% of 99mTc-dorzolamide remained in...
Source: International Journal of Pharmaceutics - Category: Drugs & Pharmacology Source Type: research