Abstract
In the current study, the development of mucoadhesive tablets for buccal delivery of a non-steroidal anti-inflammatory drug was investigated. Binary complexes with piroxicam and cyclodextrins (β-cyclodextrin (β-CD), methylated-β-cyclodextrin (Me-β-CD), and hydroxypropyl-β-cyclodextrin (HP-β-CD)) were prepared by the co-evaporation method. All formulations were characterized by means of differential scanning calorimetry, infrared spectroscopy and powder X-ray diffractometry. Mucoadhesive tablets of binary systems were formulated by direct compression using chitosan as mucoadhesive polymer. The in vitro release profiles of tablets were conducted in simulated saliva and, the drug permeation studies, across porcine buccal mucosa. The results suggest that the rank order effect of cyclodextrins for the drug release was Me-β-CD > HP-β-CD > β-CD, whereas the ex vivo studies showed that the tablets containing chitosan significantly increased the transport of the drug compared to their free complexes. Finally, histological assessment revealed loss of the superficial cell layers, which might be attributed to the presence of cyclodextrins.
Highlights
Buccal mucosa is an alternative site for the delivery of drugs into the systemic circulation [1]
The main aim of this work was to evaluate the influence of cyclodextrins (β-CD, Me-β-CD, HP-β-CD) on the drug dissolution [15,16] and its permeability through buccal porcine mucosa
Phosphate buffer saline (PBS) pH 7.4 was prepared by dissolving sodium chloride (8.0 g), potassium chloride (0.20 g), sodium phosphate dibasic (1.44 g), and potassium phosphate monobasic (0.24 g) in 1 L of distilled water
Summary
Buccal mucosa is an alternative site for the delivery of drugs into the systemic circulation [1]. The drug administered through the buccal mucosa enters to the systemic circulation directly via the jugular vein [2], minimizing the first-pass hepatic metabolism, and avoiding the adverse gastro-intestinal tract [3]. Buccal delivery of active pharmaceutical ingredients (APIs) is an alternative, non-invasive route of administration that provides beneficial health effects. Buccal mucosal has a rich vascularization and a high permeability for many APIs in addition to the fact that first-pass effect is avoided [4]. Several drug delivery systems intended for buccal administration have been developed. It is thought that the majority of drugs are transported through the paracellular route by passive diffusion [6]
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