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Problems in Ophthalmic Drug Delivery: Evaluation of the Interaction Between Preservatives and Cyclodextrins

AUTHORS

Bizhan Malaekeh-Nikouei 1 , Bibi Sedigheh Fazly Bazzaz 2 , * , Vahid Soheili 3 , Kobra Mohammadian 3

AUTHORS INFORMATION

1 Nanotechnology Research Centre, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, IR Iran

2 Biotechnology Research Center, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, IR Iran

3 Medicinal Chemistry Department, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, IR Iran

ARTICLE INFORMATION

Jundishapur Journal of Microbiology: 6 (5); 6333
Published Online: June 30, 2013
Article Type: Research Article
Received: May 13, 2012
Accepted: August 8, 2012
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Abstract

Background: Today, the use of cyclodextrins (CDs) is a major concern in drug formulations to improve solubility and stability of compounds. It has been known that CDs can reduce the antimicrobial effectiveness of preservatives by formation of inclusion complexes.

Objectives: In this study the interaction between commonly used preservatives, benzalkonium chloride (BZCl) or methyl paraben (MP), with synthetic CDs (HP ?-CD or SBE ?-CD) in the presence or absence of ethylene diamine tetra acetic acid (EDTA), as a preservative potentiator, and fluorometholone was investigated.

Materials and Methods: The tests were performed during a 4 week period according to the preservative effectiveness test of USP 2010.

Results: The results showed that CDs reduce the effectiveness of BZCl and MP even in the presence of drug molecules. The only exception was HP ?-CD 5% solution with BZCl and EDTA which was effective against tested microorganisms both in the presence and absence of drug molecules.

Conclusions: The solution of HP ?-CD 5% with BZCl 0.02% and EDTA 0.1% was selected as a good carrier for dissolving fluorometholone for use as an eye drop.

Keywords

Benzalkonium Compounds Cyclodextrins Ethylenediaminetetraacetic Acid Fluorometholone Parabens

© 2013, Author(s). This is an open-access article distributed under the terms of the Creative Commons Attribution-NonCommercial 4.0 International License (http://creativecommons.org/licenses/by-nc/4.0/) which permits copy and redistribute the material just in noncommercial usages, provided the original work is properly cited.
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