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Open AccessArticle

Development and Characterization of a Tacrolimus/Hydroxypropyl-β-Cyclodextrin Eye Drop

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Pharmacology, Pharmacy and Pharmaceutical Technology Department, Faculty of Pharmacy, University of Santiago de Compostela (USC), 15705 Santiago de Compostela, Spain
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Molecular Imaging Group, University Clinical Hospital, Health Research Institute of Santiago de Compostela (IDIS), 15706 Santiago de Compostela, Spain
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Clinical Pharmacology Group, University Clinical Hospital, Health Research Institute of Santiago de Compostela (IDIS), 15706 Santiago de Compostela, Spain
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Clinical Neurosciences Group, University Clinical Hospital, Health Research Institute of Santiago de Compostela (IDIS), 15706 Santiago de Compostela, Spain
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Nuclear Magnetic Resonance Unit, Research Infrastructures Area, University of Santiago de Compostela (USC), 15782 Santiago de Compostela, Spain
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Paraquasil Group, University Clinical Hospital, Health Research Institute of Santiago de Compostela (IDIS), 15706 Santiago de Compostela, Spain
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Physiology Department–CIMUS, University of Santiago de Compostela (USC), 15782 Santiago de Compostela, Spain
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Ophthalmology Department, Clinical University Hospital Santiago de Compostela (SERGAS), 15706 Santiago de Compostela, Spain
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Department of Surgery and Medical-Surgical Specialties and CIMUS, University of Santiago de Compostela (USC), 15782 Santiago de Compostela, Spain
*
Authors to whom correspondence should be addressed.
Pharmaceutics 2021, 13(2), 149; https://doi.org/10.3390/pharmaceutics13020149
Received: 20 December 2020 / Revised: 14 January 2021 / Accepted: 19 January 2021 / Published: 23 January 2021
(This article belongs to the Special Issue Ophthalmic Drug Delivery Volume II)
Uveitis is a vision inflammatory disorder with a high prevalence in developing countries. Currently, marketed treatments remain limited and reformulation is usually performed to obtain a tacrolimus eye drop as a therapeutic alternative in corticosteroid-refractory eye disease. The aim of this work was to develop a mucoadhesive, non-toxic and stable topical ophthalmic formulation that can be safely prepared in hospital pharmacy departments. Four different ophthalmic formulations were prepared based on the tacrolimus/hydroxypropyl-β-cyclodextrin (HPβCD) inclusion complexes’ formation. Phase solubility diagrams, Nuclear Magnetic Resonance (NMR) and molecular modeling studies showed the formation of 1:1 and 1:2 tacrolimus/HPβCD inclusion complexes, being possible to obtain a 0.02% (w/v) tacrolimus concentration by using 40% (w/v) HPβCD aqueous solutions. Formulations also showed good ophthalmic properties in terms of pH, osmolality and safety. Stability studies proved these formulations to be stable for at least 3 months in refrigeration. Ex vivo bioadhesion and in vivo ocular permanence showed good mucoadhesive properties with higher ocular permanence compared to the reference pharmacy compounding used in clinical settings (t1/2 of 86.2 min for the eyedrop elaborated with 40% (w/v) HPβCD and Liquifilm® versus 46.3 min for the reference formulation). Thus, these novel eye drops present high potential as a safe alternative for uveitis treatment, as well as a versatile composition to include new drugs intended for topical ophthalmic administration. View Full-Text
Keywords: tacrolimus; hydroxypropyl-β-cyclodextrin; topical ophthalmic administration; eye drops; uveitis; PET/CT imaging tacrolimus; hydroxypropyl-β-cyclodextrin; topical ophthalmic administration; eye drops; uveitis; PET/CT imaging
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MDPI and ACS Style

García-Otero, X.; Díaz-Tomé, V.; Varela-Fernández, R.; Martín-Pastor, M.; González-Barcia, M.; Blanco-Méndez, J.; Mondelo-García, C.; Bermudez, M.A.; Gonzalez, F.; Aguiar, P.; Fernández-Ferreiro, A.; Otero-Espinar, F.J. Development and Characterization of a Tacrolimus/Hydroxypropyl-β-Cyclodextrin Eye Drop. Pharmaceutics 2021, 13, 149. https://doi.org/10.3390/pharmaceutics13020149

AMA Style

García-Otero X, Díaz-Tomé V, Varela-Fernández R, Martín-Pastor M, González-Barcia M, Blanco-Méndez J, Mondelo-García C, Bermudez MA, Gonzalez F, Aguiar P, Fernández-Ferreiro A, Otero-Espinar FJ. Development and Characterization of a Tacrolimus/Hydroxypropyl-β-Cyclodextrin Eye Drop. Pharmaceutics. 2021; 13(2):149. https://doi.org/10.3390/pharmaceutics13020149

Chicago/Turabian Style

García-Otero, Xurxo; Díaz-Tomé, Victoria; Varela-Fernández, Rubén; Martín-Pastor, Manuel; González-Barcia, Miguel; Blanco-Méndez, José; Mondelo-García, Cristina; Bermudez, Maria A.; Gonzalez, Francisco; Aguiar, Pablo; Fernández-Ferreiro, Anxo; Otero-Espinar, Francisco J. 2021. "Development and Characterization of a Tacrolimus/Hydroxypropyl-β-Cyclodextrin Eye Drop" Pharmaceutics 13, no. 2: 149. https://doi.org/10.3390/pharmaceutics13020149

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