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Wertheimer, Christian; Kueres, Alexander; Siedlecki, Jakob; Braun, Christian; Kassumeh, Stefan; Wolf, Armin; Mayer, Wolfgang; Priglinger, Claudia; Priglinger, Siegfried; Eibl-Lindner, Kirsten (2018): The intraocular lens as a drug delivery device for an epidermal growth factor-Receptor inhibitor for prophylaxis of posterior capsule opacification. In: Acta Ophthalmologica, Vol. 96, No. 7, E874-E882
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Purpose Posterior capsule opacification (PCO) occurs as a common complication after cataract surgery. Erlotinib is an inhibitor of the epidermal growth factor-Receptor and reduces critical cellular events leading to PCO. In this in vitro study, Erlotinib-modified intraocular lenses (IOLs) employed as a drug delivery device have been evaluated for PCO prevention. Methods Results The IC50 concentration of Erlotinib was determined by using FHL-124 cells. For the human capsular bag model, 40 cadaver eyes underwent sham cataract surgery. Sixteen capsular bags were exposed to the IC50 of Erlotinib. Intraocular lens (IOL) of three different materials was pharmacologically modified and tested in the anterior segment model and implanted into 24 capsular bags. To test for corneal toxicity, pairs of human cornea were exposed to high concentrations of Erlotinib and corneal endothelial cells (CEC) were exposed to the modified IOL. Release kinetics of Erlotinib from the IOL was measured. IC50 of Erlotinib was determined to be 10 mu m. Erlotinib alone (p = 0.002) and when soaked into IOLs (p < 0.001) significantly increased the number of days needed until total cell coverage of the capsular bags in comparison with the control. Modified IOLs mitigated cell growth in the anterior segment model (p < 0.001). No short-term corneal toxicity was observed up to a concentration of 100 mu m, and IOLs did not show toxicity on CEC. Erlotinib was released constantly from IOL. Conclusion Erlotinib might be of clinical relevance in PCO prophylaxis, as its short-term application induces a long-term deceleration of cellular growth. Erlotinib can be introduced into the eye via soaked IOLs.