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Development of a Mucoadhesive and In Situ Gelling Formulation Based on κ-Carrageenan for Application on Oral Mucosa and Esophagus Walls. I. A Functional In Vitro Characterization
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Mar. Drugs 2019, 17(3), 153; https://doi.org/10.3390/md17030153

Development of a Mucoadhesive and an in Situ Gelling Formulation Based on κ-Carrageenan for Application on Oral Mucosa and Esophagus Walls. II. Loading of a Bioactive Hydroalcoholic Extract

1
Department of Drug Sciences, University of Pavia, Viale Taramelli, 12‐27100 Pavia, Italy
2
Department of Earth and Environmental Science, University of Pavia, Via S. Epifanio, 14‐27100 Pavia, Italy
*
Author to whom correspondence should be addressed.
Received: 9 January 2019 / Revised: 21 February 2019 / Accepted: 27 February 2019 / Published: 5 March 2019
(This article belongs to the Special Issue Marine Biopolymers and Drug Delivery)
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Abstract

The aim of the present work was to load a Hibiscus sabdariffa (HS) hydroalcoholic extract into in situ gelling formulations for the treatment of oral mucositis and esophagitis. Such formulations, selected as the most promising options in a previous work of ours, were composed by κ-carrageenan (κ-CG), a sulfated marine polymer able to gelify in presence of saliva ions, hydroxypropyl cellulose (HPC), used as mucoadhesive agent, and CaCl2, salt able to enhance the interaction κ-CG/saliva ions. HS extract, which is rich in phytochemicals such as polyphenols, polysaccharides and organic acids, was selected due to its antioxidant and anti-inflammatory properties. For HS extraction, three different methodologies (maceration, Ultrasound Assisted Extraction (UAE) and Microwave Assisted Extraction (MAE)) were compared in terms of extraction yield and extract antioxidant activity, revealing that MAE was the best procedure. Rheological and mucoadhesive properties of HS-loaded formulations were investigated. Such formulations were characterized by a low viscosity at 25 °C, guaranteeing an easy administration, a proper in situ gelation behavior and marked elastic and mucoadhesive properties at 37 °C, functional to a protective action towards the damaged mucosa. Finally, the biocompatibility and the proliferative effect of HS-loaded formulations, as well as their antioxidant and anti-inflammatory properties, were proved in vitro on human dermal fibroblasts. View Full-Text
Keywords: oral mucositis; Hibiscus sabdariffa extract; κ-carrageenan; in situ gelation; mucoadhesion; antioxidant; anti-inflammatory properties oral mucositis; Hibiscus sabdariffa extract; κ-carrageenan; in situ gelation; mucoadhesion; antioxidant; anti-inflammatory properties
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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Vigani, B.; Rossi, S.; Gentile, M.; Sandri, G.; Bonferoni, M.C.; Cavalloro, V.; Martino, E.; Collina, S.; Ferrari, F. Development of a Mucoadhesive and an in Situ Gelling Formulation Based on κ-Carrageenan for Application on Oral Mucosa and Esophagus Walls. II. Loading of a Bioactive Hydroalcoholic Extract. Mar. Drugs 2019, 17, 153.

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