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Pharmaceutics 2017, 9(3), 22; doi:10.3390/pharmaceutics9030022

Development and Characterization of an Amorphous Solid Dispersion of Furosemide in the Form of a Sublingual Bioadhesive Film to Enhance Bioavailability

1
Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), Università degli Studi di Palermo, Palermo, PA 90123, Italy
2
Dipartimento dell'Innovazione Industriale e Digitale, Ingegneria Chimica, Gestionale, Informatica, Meccanica, Università degli Studi di Palermo, Palermo, PA 90128, Italy
3
SiSaf Ltd, Innovation Centre, Northern Ireland Science Park, Queen’s Island, Belfast BT3 9DT, UK
4
Consiglio Nazionale delle Ricerche, Istituto di Biofisica–UOP Palermo, Palermo, PA 90146, Italy
*
Author to whom correspondence should be addressed.
Academic Editor: Thomas Rades
Received: 26 May 2017 / Revised: 17 June 2017 / Accepted: 19 June 2017 / Published: 24 June 2017
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Abstract

Administered by an oral route, Furosemide (FUR), a diuretic used in several edematous states and hypertension, presents bioavailability problems, reported as a consequence of an erratic gastrointestinal absorption due to various existing polymorphic forms and low and pH-dependent solubility. A mucoadhesive sublingual fast-dissolving FUR based film has been developed and evaluated in order to optimize the bioavailability of FUR by increasing solubility and guaranteeing a good dissolution reproducibility. The Differential Scanning Calorimetry (DSC) analyses confirmed that the film prepared using the solvent casting method entrapped FUR in the amorphous state. As a solid dispersion, FUR increases its solubility up to 28.36 mg/mL. Drug content, thickness, and weight uniformity of film were also evaluated. The measured Young’s Modulus, yield strength, and relative elongation of break percentage (EB%) allowed for the classification of the drug-loaded film as an elastomer. Mucoadhesive strength tests showed that the force to detach film from mucosa grew exponentially with increasing contact time up to 7667 N/m2. FUR was quickly discharged from the film following a trend well fitted with the Weibull kinetic model. When applied on sublingual mucosa, the new formulation produced a massive drug flux in the systemic compartment. Overall, the proposed sublingual film enhances drug solubility and absorption, allowing for the prediction of a rapid onset of action and reproducible bioavailability in its clinical application. View Full-Text
Keywords: mucoadhesive film; sublingual absorption; amorphous solid dispersion; furosemide bioavailability; transmucosal delivery mucoadhesive film; sublingual absorption; amorphous solid dispersion; furosemide bioavailability; transmucosal delivery
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MDPI and ACS Style

De Caro, V.; Ajovalasit, A.; Sutera, F.M.; Murgia, D.; Sabatino, M.A.; Dispenza, C. Development and Characterization of an Amorphous Solid Dispersion of Furosemide in the Form of a Sublingual Bioadhesive Film to Enhance Bioavailability. Pharmaceutics 2017, 9, 22.

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