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Research Progress on Synthesis and Application of Cyclodextrin Polymers

Cytotoxicity of β-Cyclodextrins in Retinal Explants for Intravitreal Drug Formulations

Faculty of Pharmaceutical Sciences, University of Iceland, Hofsvallagata 53, IS-107 Reykjavik, Iceland
Institute for Ophthalmic Research, University of Tübingen, Elfriede-Aulhorn-Strasse 5-7, 72076 Tübingen, Germany
Author to whom correspondence should be addressed.
Academic Editor: Marina Isidori
Molecules 2021, 26(5), 1492;
Received: 15 February 2021 / Revised: 2 March 2021 / Accepted: 3 March 2021 / Published: 9 March 2021
(This article belongs to the Special Issue Cyclodextrin Chemistry and Toxicology)
Cyclodextrins (CDs) have been widely used as pharmaceutical excipients for formulation purposes for different delivery systems. Recent studies have shown that CDs are able to form complexes with a variety of biomolecules, such as cholesterol. This has subsequently paved the way for the possibility of using CDs as drugs in certain retinal diseases, such as Stargardt disease and retinal artery occlusion, where CDs could absorb cholesterol lumps. However, studies on the retinal toxicity of CDs are limited. The purpose of this study was to examine the retinal toxicity of different beta-(β)CD derivatives and their localization within retinal tissues. To this end, we performed cytotoxicity studies with two different CDs—2-hydroxypropyl-βCD (HPβCD) and randomly methylated β-cyclodextrin (RMβCD)—using wild-type mouse retinal explants, the terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) assay, and fluorescence microscopy. RMβCD was found to be more toxic to retinal explants when compared to HPβCD, which the retina can safely tolerate at levels as high as 10 mM. Additionally, studies conducted with fluorescent forms of the same CDs showed that both CDs can penetrate deep into the inner nuclear layer of the retina, with some uptake by Müller cells. These results suggest that HPβCD is a safer option than RMβCD for retinal drug delivery and may advance the use of CDs in the development of drugs designed for intravitreal administration. View Full-Text
Keywords: cyclodextrin; retinal explant; cytotoxicity; uptake cyclodextrin; retinal explant; cytotoxicity; uptake
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MDPI and ACS Style

Prajapati, M.; Christensen, G.; Paquet-Durand, F.; Loftsson, T. Cytotoxicity of β-Cyclodextrins in Retinal Explants for Intravitreal Drug Formulations. Molecules 2021, 26, 1492.

AMA Style

Prajapati M, Christensen G, Paquet-Durand F, Loftsson T. Cytotoxicity of β-Cyclodextrins in Retinal Explants for Intravitreal Drug Formulations. Molecules. 2021; 26(5):1492.

Chicago/Turabian Style

Prajapati, Manisha, Gustav Christensen, François Paquet-Durand, and Thorsteinn Loftsson. 2021. "Cytotoxicity of β-Cyclodextrins in Retinal Explants for Intravitreal Drug Formulations" Molecules 26, no. 5: 1492.

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