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Open AccessArticle

A Way to Increase the Bioaccesibility and Photostability of Roflumilast, a COPD Treatment, by Cyclodextrin Monomers

Departamento de Bioquímica y Biología Molecular-A, Facultad de Biología, Universidad de Murcia—Regional Campus of International Excellence “Campus Mare Nostrum”, E-30100 Murcia, Spain
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Polymers 2019, 11(5), 801; https://doi.org/10.3390/polym11050801
Received: 26 March 2019 / Revised: 29 April 2019 / Accepted: 30 April 2019 / Published: 4 May 2019
(This article belongs to the Special Issue Cyclodextrin-Containing Polymers)
Roflumilast is an orally available inhibitor of phosphodiesterase (PDE) type 4, which is widely used in chronic obstructive pulmonary diseases. However, it has low solubility and adverse effects include diarrhea and nausea. Since its solubilization may improve treatment and, dismissing any adverse effects, its interaction with cyclodextrins (CDs) was studied. The Higuchi-Connors method was used to determine the complexation constant with different CDs, pH values and temperatures. Molecular docking was used to predict interaction between the complexes. An in vitro digestion experiment was carried out to test roflumilast protection. Finally, the photostability of the complex was evaluated. The complex formed with β-CD had the highest K11 value (646 ± 34 M−1), although this value decreased with increasing temperature. Similarly, K11 decreased as the pH increased. In vitro digestion showed that CDs protect the drug during digestion and even improve its bioaccessibility. Finally, CDs reduced the drug’s extreme photosensitivity, originating a fluorescence signal, which is described for first time. The kinetic parameters of the reaction were obtained. This study not only completes the complexation study of roflumilast-CD, but also points to the need to protect roflumilast from light, suggesting that tablets containing the drug might be reformulated. View Full-Text
Keywords: roflumilast; cyclodextrins; digestion; fluorescence; phosphodiesterase roflumilast; cyclodextrins; digestion; fluorescence; phosphodiesterase
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MDPI and ACS Style

Matencio, A.; Hernández-García, S.; García-Carmona, F.; López-Nicolás, J.M. A Way to Increase the Bioaccesibility and Photostability of Roflumilast, a COPD Treatment, by Cyclodextrin Monomers. Polymers 2019, 11, 801. https://doi.org/10.3390/polym11050801

AMA Style

Matencio A, Hernández-García S, García-Carmona F, López-Nicolás JM. A Way to Increase the Bioaccesibility and Photostability of Roflumilast, a COPD Treatment, by Cyclodextrin Monomers. Polymers. 2019; 11(5):801. https://doi.org/10.3390/polym11050801

Chicago/Turabian Style

Matencio, Adrián; Hernández-García, Samanta; García-Carmona, Francisco; López-Nicolás, José M. 2019. "A Way to Increase the Bioaccesibility and Photostability of Roflumilast, a COPD Treatment, by Cyclodextrin Monomers" Polymers 11, no. 5: 801. https://doi.org/10.3390/polym11050801

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