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Polysaccharides for the design of fast and sustained release buccal films

Abstract

Polysaccharides for the design of fast and sustained release buccal films

The growing interest and the potential of natural-derived polysaccharides have attracted research attention for the development of biocompatible buccal films. Drug delivery through the buccal mucosa offers several benefits over oral and parenteral formulations. Systemic buccal drug delivery bypasses stomach degradation and hepatic first- pass metabolism, providing a non-invasive approach [1]. Polysaccharide such as alginate, chitosan, pullulan and cellulose derivatives have been studied as components of buccal films to facilitate the fast or the sustained release of therapeutic agents [2]. Chitosan is a polysaccharide obtained from the deacetylation of chitin, found in the exoskeleton of crustaceans. It is a copolymer formed by randomly distributed N-acetyl-glucosamine and N-glycosamine units positively charged at pH values below the pKa of its amino groups. Alginate is usually from brown algae. It is a copolymer formed by (1,4) β-D-mannuronate (M) and α-L- guluronate (G) groups. Alginate can then be negatively charged, being able to interact electrostatically with positively charged compounds. The characteristics to take into account for the design of buccal films are mucoadhesive capability, flexibility, tensile properties, and requirements for buccal administration including acceptability and palatability.

A combination of cellulose and starch derivatives have been exploited to obtain a drug delivery system with a fast release kinetics for the pediatric administration of ibuprofen. The buccal films were in vitro characterized determining mechanical properties (i.e. thickness, flexibility), drug content, in vitro drug release kinetics in simulated saliva and physical and chemical stability. Moreover, mucoadhesive properties, ex vivo permeation through rabbit buccal mucosa and mucosal absorption were investigated.

Buccal films with favorable physico-mechanical properties for the delivery of ibuprofen have been successfully obtained exploiting polysaccharide-based polymers. The buccal film composition was optimized to control the drug release into the oral cavity.