Peptide (insulin) loaded nanoparticles (NPs) have been embedded into buccal chitosan films (Ch-films-NPs). These films were produced by solvent casting and involved incorporating in chitosan gel (1.25% w/v), NPs-Insulin suspensions at three different concentrations (1, 3, and 5mg of NPs per film) using glycerol as plasticiser. Film swelling and mucoadhesion were investigated using 0.01M PBS at 37°C and texture analyzer, respectively. Formulations containing 3mg of NPs per film produced optimised films with excellent mucoadhesion and swelling properties. Dynamic laser scattering measurements showed that the erosion of the chitosan backbone controlled the release of NPs from the films, preceding in vitro drug (insulin) release from Ch-films-NPs after 6h. Modulated release was observed with 70% of encapsulated insulin released after 360h. The use of chitosan films yielded a 1.8-fold enhancement of ex vivo insulin permeation via EpiOral™ buccal tissue construct relative to the pure drug. Flux and apparent permeation coefficient of 0.1μg/cm(2)/h and 4×10(-2)cm(2)/h were respectively obtained for insulin released from Ch-films-NPs-3. Circular dichroism and FTIR spectroscopy demonstrated that the conformational structure of the model peptide drug (insulin) released from Ch-films-NPs was preserved during the formulation process.
Keywords: ATR-FTIR; Buccal mucosa delivery; CD; Chitosan films; DLS; EpiOral™; Insulin; NP; Nanoparticles; PBS; PEG; PEG-b-PLA; PVA; PVP; Peptide delivery; TFA; TH; attenuated total reflectance-Fourier transform infra-red; circular dichroism; dynamic laser scattering; nanoparticle; phosphate buffered saline; poly(ethylene glycol)methyl ether-block-polylactide; polyethylene glycol; polyvinyl pyrrolidone; polyvinylalcohol; trehalose; trifluoroacetic acid.
Copyright © 2013 Elsevier B.V. All rights reserved.