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Mucoadhesive Interpolyelectrolyte Complexes for the Buccal Delivery of Clobetasol

This work aimed to investigate the feasibility to design: (a) a mucoadhesive interpolyelectrolyte complex (IPEC) loaded with clobetasol propionate (CP) intended to treat oral lichen planus and (b) individuate an orodispersible dosage form suitable for its administration. IPECs were synthesized by mi...

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Autores principales: Garipova, Venera R., Gennari, Chiara G. M., Selmin, Francesca, Cilurzo, Francesco, Moustafine, Rouslan I.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6414932/
https://www.ncbi.nlm.nih.gov/pubmed/30966120
http://dx.doi.org/10.3390/polym10010085
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author Garipova, Venera R.
Gennari, Chiara G. M.
Selmin, Francesca
Cilurzo, Francesco
Moustafine, Rouslan I.
author_facet Garipova, Venera R.
Gennari, Chiara G. M.
Selmin, Francesca
Cilurzo, Francesco
Moustafine, Rouslan I.
author_sort Garipova, Venera R.
collection PubMed
description This work aimed to investigate the feasibility to design: (a) a mucoadhesive interpolyelectrolyte complex (IPEC) loaded with clobetasol propionate (CP) intended to treat oral lichen planus and (b) individuate an orodispersible dosage form suitable for its administration. IPECs were synthesized by mixing Eudragit(®) E PO (EPO) and different grades of cross-linked polyacrylate derivatives, in different molar ratios, namely 1:1, 1:2, and 2:1. All IPECs resulted at nanoscale independently of their composition (120–200 nm). Both zeta-potentials (ζ) and mucoadhesive performances were influenced by the ratio between polymers. On the bases of the preliminary data, IPECs made of Polycarbophil and EPO in the 1:2 ratio were loaded with CP. The encapsulation efficiency was up 88% independently of the CP-IPEC ratio. The drug encapsulation caused IPEC destabilization in water, as it was noticed by the increase of ζ values and the formation of aggregates. Oral lyophilisates were prepared by freeze-drying slurries made of placebo or CP loaded IPECs, maltodextrin with a dextrose equivalent 38 and Span(®)80. The optimized formulation permitted to obtain a fast disintegration upon contact with water reducing the tendency of IPECs to aggregate. Moreover, oral lyophilisates allowed improving the apparent solubility of CP throughout the in vitro release experiment.
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spelling pubmed-64149322019-04-02 Mucoadhesive Interpolyelectrolyte Complexes for the Buccal Delivery of Clobetasol Garipova, Venera R. Gennari, Chiara G. M. Selmin, Francesca Cilurzo, Francesco Moustafine, Rouslan I. Polymers (Basel) Article This work aimed to investigate the feasibility to design: (a) a mucoadhesive interpolyelectrolyte complex (IPEC) loaded with clobetasol propionate (CP) intended to treat oral lichen planus and (b) individuate an orodispersible dosage form suitable for its administration. IPECs were synthesized by mixing Eudragit(®) E PO (EPO) and different grades of cross-linked polyacrylate derivatives, in different molar ratios, namely 1:1, 1:2, and 2:1. All IPECs resulted at nanoscale independently of their composition (120–200 nm). Both zeta-potentials (ζ) and mucoadhesive performances were influenced by the ratio between polymers. On the bases of the preliminary data, IPECs made of Polycarbophil and EPO in the 1:2 ratio were loaded with CP. The encapsulation efficiency was up 88% independently of the CP-IPEC ratio. The drug encapsulation caused IPEC destabilization in water, as it was noticed by the increase of ζ values and the formation of aggregates. Oral lyophilisates were prepared by freeze-drying slurries made of placebo or CP loaded IPECs, maltodextrin with a dextrose equivalent 38 and Span(®)80. The optimized formulation permitted to obtain a fast disintegration upon contact with water reducing the tendency of IPECs to aggregate. Moreover, oral lyophilisates allowed improving the apparent solubility of CP throughout the in vitro release experiment. MDPI 2018-01-17 /pmc/articles/PMC6414932/ /pubmed/30966120 http://dx.doi.org/10.3390/polym10010085 Text en © 2018 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Garipova, Venera R.
Gennari, Chiara G. M.
Selmin, Francesca
Cilurzo, Francesco
Moustafine, Rouslan I.
Mucoadhesive Interpolyelectrolyte Complexes for the Buccal Delivery of Clobetasol
title Mucoadhesive Interpolyelectrolyte Complexes for the Buccal Delivery of Clobetasol
title_full Mucoadhesive Interpolyelectrolyte Complexes for the Buccal Delivery of Clobetasol
title_fullStr Mucoadhesive Interpolyelectrolyte Complexes for the Buccal Delivery of Clobetasol
title_full_unstemmed Mucoadhesive Interpolyelectrolyte Complexes for the Buccal Delivery of Clobetasol
title_short Mucoadhesive Interpolyelectrolyte Complexes for the Buccal Delivery of Clobetasol
title_sort mucoadhesive interpolyelectrolyte complexes for the buccal delivery of clobetasol
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6414932/
https://www.ncbi.nlm.nih.gov/pubmed/30966120
http://dx.doi.org/10.3390/polym10010085
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