Abstract
Objective: The objectives of this study were to prepare and characterize a buccal mucoadhesive patch using poly (vinyl alcohol) (PVA), poly (vinyl pyrrolidone) (PVP) as a mucoadhesive matrix, Eudragit S100 as a backing layer, and lidocaine HCl as a model drug.Methods: Lidocaine HCl buccal patches were prepared using double casting technique. Molecular interactions in the polymer matrices were studied using attenuated total reflectance-fourier transform infrared spectroscopy (ATR-FTIR), differential scanning calorimetry (DSC) and X-ray diffractometry. Mechanical and mucoadhesive properties were measured using texture analyzer. In vitro permeation of lidocaine HCl from the patch was conducted using Franz diffusion cell.Results: Both of the free and lidocaine HCl patches were smooth and transparent, with good flexibility and strength. ATR-FTIR, DSC and X-ray diffractometry studies confirmed the interaction of PVA and PVP. Mechanical properties of matrices containing 60% PVP were significantly lower than those containing 20% PVP (*P<0.05). Mucoadhesive properties had a tendency to decrease with the concentration of PVP in the patch. The patch containing 60% PVP had significantly lower muco-adhesiveness than those containing 20% PVP (*P<0.05). In vitro permeation revealed that the pattern of lidocaine HCl permeation started with an initial fast permeation, followed by a slower permeation rate. The initial permeation fluxes follow the zero-order model of which rate was not affected by the PVP concentrations in the PVA/PVP matrix.Conclusion: Mucoadhesive buccal patches fabricated with PVA/PVP were successfully prepared. Incorporation of PVP in PVA/PVP matrix affected the strength of polymeric matrix and mucoadhesive property of patches.
Highlights
Buccal drug delivery has gained considerable attention as an alternative dosage form [1]
Both of the blank and lidocaine HCl matrices were prepared by a solvent casting method using an aqueous solution of 12% polymer
The clearness and transparency of lidocaine HCl matrices suggest that lidocaine HCl was solubilized in the polymer matrix
Summary
Buccal drug delivery has gained considerable attention as an alternative dosage form [1]. Mucoadhesive patches for buccal mucosa administration may have a number of different designs [7, 8]. These patches usually contain hydrophilic polymers that are able to form sticky hydrogels after getting in contact with water, and adhere to the buccal mucosa and the impermeable backing membrane [3]. Low water permeability and drug impermeability properties such as melted wax [10], ethyl cellulose [1, 4, 11], and Eudragit RL100 [12] have been used as a backing membrane. In order to improve the film properties, including film-forming ability, mechanical and mucoadhesive properties, a combination of hydrophilic polymers is generally used
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