Pharmacokinetic Simulations of Intravitreal Biologicals : Aspects of Drug Delivery to the Posterior and Anterior Segments

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Rimpelä , A-K , Kiiski , I , Deng , F , Kidron , H & Urtti , A 2019 , ' Pharmacokinetic Simulations of Intravitreal Biologicals : Aspects of Drug Delivery to the Posterior and Anterior Segments ' , Pharmaceutics , vol. 11 , no. 1 , 9 . https://doi.org/10.3390/pharmaceutics11010009

Title: Pharmacokinetic Simulations of Intravitreal Biologicals : Aspects of Drug Delivery to the Posterior and Anterior Segments
Author: Rimpelä, Anna-Kaisa; Kiiski, Iiro; Deng, Feng; Kidron, Heidi; Urtti, Arto
Contributor: University of Helsinki, Faculty of Pharmacy
University of Helsinki, Division of Pharmaceutical Chemistry and Technology
University of Helsinki, Department of Clinical Pharmacology
University of Helsinki, Division of Pharmaceutical Biosciences
University of Helsinki, Drug Research Program
Date: 2019-01
Language: eng
Number of pages: 11
Belongs to series: Pharmaceutics
ISSN: 1999-4923
URI: http://hdl.handle.net/10138/299247
Abstract: Biologicals are important ocular drugs that are be delivered using monthly and bimonthly intravitreal injections to treat retinal diseases, such as age-related macular degeneration. Long acting delivery systems are needed for prolongation of their dosing interval. Intravitreal biologicals are eliminated from the eye via the aqueous humor outflow. Thus, the anterior and posterior segments are exposed to the drug. We utilized a kinetic simulation model to estimate protein drug concentrations in the vitreous and aqueous humor after bolus injection and controlled release administration to the vitreous. The simulations predicted accurately the experimental levels of 5 biologicals in the vitreous and aqueous humor. The good match between the simulations and experimental data demonstrated almost complete anterior segment bioavailability, and major dose sparing with ocular controlled release systems. Overall, the model is a useful tool in the design of intraocular delivery of biologicals.
Subject: 317 Pharmacy
intravitreal inject ion
ocular drug delivery
bevacizumab
ranibizumab
aflibercept
controlled release
RABBIT
VOLUME
CLEARANCE
RITUXIMAB
THERAPY
PROTEIN
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