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Open AccessArticle

Permeability of the Retina and RPE-Choroid-Sclera to Three Ophthalmic Drugs and the Associated Factors

1
Department of Ophthalmology, Seoul National University College of Medicine, Seoul National University Bundang Hospital, Seongnam 13620, Korea
2
Department of Chemical and Biomolecular Engineering, Sogang University, Seoul 04107, Korea
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editors: Francisco Javier Otero-Espinar and Anxo Fernández Ferreiro
Pharmaceutics 2021, 13(5), 655; https://doi.org/10.3390/pharmaceutics13050655
Received: 6 April 2021 / Revised: 30 April 2021 / Accepted: 1 May 2021 / Published: 4 May 2021
(This article belongs to the Special Issue Ophthalmic Drug Delivery Volume II)
In this study, Retina-RPE-Choroid-Sclera (RCS) and RPE-Choroid-Sclera (CS) were prepared by scraping them off neural retina, and using the Ussing chamber we measured the average time–concentration values in the acceptor chamber across five isolated rabbit tissues for each drug molecule. We determined the outward direction permeability of the RCS and CS and calculated the neural retina permeability. The permeability coefficients of RCS and CS were as follows: ganciclovir, 13.78 ± 5.82 and 23.22 ± 9.74; brimonidine, 15.34 ± 7.64 and 31.56 ± 12.46; bevacizumab, 0.0136 ± 0.0059 and 0.0612 ± 0.0264 (×10−6 cm/s). The calculated permeability coefficients of the neural retina were as follows: ganciclovir, 33.89 ± 12.64; brimonidine, 29.83 ± 11.58; bevacizumab, 0.0205 ± 0.0074 (×10−6 cm/s). Between brimonidine and ganciclovir, lipophilic brimonidine presented better RCS and CS permeability, whereas ganciclovir showed better calculated neural retinal permeability. The large molecular weight drug bevacizumab demonstrated a much lower permeability than brimonidine and ganciclovir. In conclusion, the ophthalmic drug permeability of RCS and CS is affected by the molecular weight and lipophilicity, and influences the intravitreal half-life. View Full-Text
Keywords: permeability; retina; retinal pigment epithelium; Ussing chamber; intravitreal half-life permeability; retina; retinal pigment epithelium; Ussing chamber; intravitreal half-life
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MDPI and ACS Style

Kim, H.M.; Han, H.; Hong, H.K.; Park, J.H.; Park, K.H.; Kim, H.; Woo, S.J. Permeability of the Retina and RPE-Choroid-Sclera to Three Ophthalmic Drugs and the Associated Factors. Pharmaceutics 2021, 13, 655. https://doi.org/10.3390/pharmaceutics13050655

AMA Style

Kim HM, Han H, Hong HK, Park JH, Park KH, Kim H, Woo SJ. Permeability of the Retina and RPE-Choroid-Sclera to Three Ophthalmic Drugs and the Associated Factors. Pharmaceutics. 2021; 13(5):655. https://doi.org/10.3390/pharmaceutics13050655

Chicago/Turabian Style

Kim, Hyeong M.; Han, Hyounkoo; Hong, Hye K.; Park, Ji H.; Park, Kyu H.; Kim, Hyuncheol; Woo, Se J. 2021. "Permeability of the Retina and RPE-Choroid-Sclera to Three Ophthalmic Drugs and the Associated Factors" Pharmaceutics 13, no. 5: 655. https://doi.org/10.3390/pharmaceutics13050655

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