Statistical optimisation of the mucoadhesivity and characterisation of multipolymeric propranolol matrices for buccal therapy

A Box-Behnken experimental design was employed to optimise a polymeric blend for the preparation of propranolol HCl matrices with maximum mucoadhesivity and was thereafter modified for achieving controlled drug release. The quantitative effects of the polymers used i.e. poly(acrylic acid) (PAA) and poly(vinyl pyrrolidone) (PVP) on mucoadhesion could be predicted using polynomial equations. A formulation of 20% PAA, 20% CMC and 20% PVP was identified for maximising mucoadhesivity and obtaining a controlled drug release profile. Reproducibility of the optimal formulation in terms of mucoadhesivity and controlled drug release was confirmed. The optimal formulation was characterised in terms of mucoadhesivity, release kinetics, swelling/erosion, hydration dynamics and surface pH. From the model fitting analyses, drug release was found to be diffusion, polymeric relaxation and erosion based with the former two being more dominant over erosion. This was in agreement with the erosion and swelling studies which showed swelling and erosion occurring in the tablet matrix. Textural profiling showed initial rapid hydration, which could be beneficial for enhanced mucoadhesivity. Surface pH of the multipolymeric matrices was similar to salivary pH and did not show extremes in changes over the test period. The optimal preparation of multipolymeric propranolol matrices identified in this study shows potential for buccal administration. (c) 2006 Elsevier B.V. All rights reserved.