Mucoadhesive Interpolyelectrolyte Complexes for the Buccal Delivery of Clobetasol.

Venera Garipova,Chiara Gennari,Francesco Cilurzo,Francesca Selmin,Rouslan Moustafine

doi:10.3390/polym10010085

Venera Garipova, Chiara Gennari + Show 3 more

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https://doi.org/10.3390/polym10010085

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Journal: Polymers	Publication Date: Jan 17, 2018
Citations: 28	License type: CC BY 4.0

Affiliation: Kazan State Medical University, University of Milan

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.

Highlights

Interpolyelectrolyte complexes (IPECs) are formed in aqueous dispersions by spontaneous association of oppositely charged polyelectrolytes due to strong but reversible electrostatic interactions [1]
All IPECs obtained by mixing E PO (EPO) and four types of carbomers differing in chemical composition, molecular weight, or cross-linking were insoluble in water
The lower values of maximum detachment force (MDF), associated to a more negative of zeta potential, might be the result of greater repulsion between negative charges of mucin and IPECs. These results indicate that mucoadhesion of IPECs made of Carbopol® Ultrez 10 NF polymer (C10), C71G, and Noveon® AA-1 (NAA-1) are mainly attributed to the formation of electrostatic interactions

Summary

Introduction

Interpolyelectrolyte complexes (IPECs) are formed in aqueous dispersions by spontaneous association of oppositely charged polyelectrolytes due to strong but reversible electrostatic interactions [1]. Depending on the main features of selected polymers, IPECs exhibit peculiar physico-chemical properties due to their electrostatic interactions and flexibility. Upon mixing two aqueous solutions of oppositely charged polyelectrolytes in a stoichiometric ratio, the resulting IPEC is insoluble and precipitates out [6], often as a colloid [7]. The definition of a suitable drying technique, and the relative protocol, is required to improve their physical and microbiological stability. Polymers 2018, 10, 85; doi:10.3390/polym10010085 www.mdpi.com/journal/polymers drying could cause thecould formation of irreversible aggregates of irregular shape and considering stability

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