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Development of ciprofloxacin-loaded contact lenses using fluorous chemistry.pdf
Biomaterials 124 (2017) 55e64
Contents lists available at ScienceDirect
Biomaterials
journal homepage: /locate/biomaterials
Development of cipro?oxacin-loaded contact lenses using ?uorous chemistry
Guoting Qin a, *, Zhiling Zhu b, Siheng Li b, Alison M. McDermott a, Chengzhi Cai b, **
a College of Optometry, University of Houston, Houston, TX, 77204, USA b Department of Chemistry, University of Houston, Houston, TX, 77204, USA
article info
Article history: Received 30 November 2016 Received in revised form 17 January 2017 Accepted 29 January 2017 Available online 31 January 2017
Keywords: Fluorous chemistry Contact lenses Drug delivery Antimicrobial activity
abstract
In this work, we developed a simple method to load drugs into commercially available contact lenses utilizing ?uorous chemistry. We demonstrated this method using model compounds including ?uoroustagged ?uorescein and antibiotic cipro?oxacin. We showed that ?uorous interactions facilitated the loading of model molecules into ?uorocarbon-containing contact lenses, and that the release pro?les exhibited sustained release. Contact lenses loaded with ?uorous-tagged cipro?oxacin exhibited antimicrobial activity against Pseudomonas aeruginosa in vitro, while no cytotoxicity towards human corneal epithelial cells was observed. To mimic the tear turnover, we designed a porcine eye infection model under ?ow conditions. Signi?cantly, the modi?ed lenses also exhibited antimicrobial ef?cacy against Pseudomonas aeruginosa in the ex vivo infection model. Overall, utilizing ?uorous chemistry, we can construct a drug delivery system that exhibits high drug loading capacity, sustained drug release, and robust biological activity.
? 2017 Elsevier Ltd. All rights reserved.
1. Introduction
Currently more than 90% of ophthalmic drugs are delivered in the form of eye drop solutions [1]. However, only ~ 1e7% of the administered dose is actively absorbed [2]. Therefore, high drug dosage and frequent administration are necessar
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