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Polymers 2018, 10(1), 85; https://doi.org/10.3390/polym10010085

Mucoadhesive Interpolyelectrolyte Complexes for the Buccal Delivery of Clobetasol

1
Department of Pharmaceutical, Analytical and Toxicological Chemistry, Kazan State Medical University, 49 Butlerov Street, 420012 Kazan, Russia
2
Department of Pharmaceutical Science, University of Milan, Via G. Colombo 71, 20133 Milan, Italy
*
Author to whom correspondence should be addressed.
Received: 28 November 2017 / Revised: 8 January 2018 / Accepted: 8 January 2018 / Published: 17 January 2018
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Abstract

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. View Full-Text
Keywords: Carbopol; clobetasol; Eudragit® E PO; interpolyelectrolyte complex; mucoadhesion; oral lichen planus; oral lyophilisates; maltodextrin; resuspendibility Carbopol; clobetasol; Eudragit® E PO; interpolyelectrolyte complex; mucoadhesion; oral lichen planus; oral lyophilisates; maltodextrin; resuspendibility
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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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Garipova, V.R.; Gennari, C.G.M.; Selmin, F.; Cilurzo, F.; Moustafine, R.I. Mucoadhesive Interpolyelectrolyte Complexes for the Buccal Delivery of Clobetasol. Polymers 2018, 10, 85.

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