The present study aimed to formulate orodispersible tablets of flutamide (FTM) to increase its bioavailability. Orodispersible tablets were prepared by direct compression technique using three different approaches namely; super-disintegration, effervescence and sublimation. Different combined approaches were proposed and evaluated to optimize tablet characteristics. Sodium starch glycolate (SSG) was used as the superdisintegrant. The prepared powder mixtures were subjected to both pre and post compression evaluation parameters including; IR spectroscopy, micromeritics properties, tablet hardness, friability, wetting time, disintegration time and in-vitro drug release. IR studies indicated that there was no interaction between the drug and the excipients used except Ludipress. The results of micromeritics studies revealed that all formulations were of acceptable to good flowability. Tablet hardness and friability indicated good mechanical strength. Wetting and dispersion times decreased from 46 to 38 s by increasing the SSG concentration from 3.33 to 6.66% w/w in tablets prepared by superdisintegration method. The F8 formulation which was prepared by combined approaches of effervescence and superdisintegrant addition gave promising results for tablet disintegration and wetting times but failed to give faster dissolution rate. The incorporation of 1:5 solid dispersion of FTM: PEG6000 instead of the pure drug in the same formulation increased the drug release rate from 73.12 to 96.99% after 15 min. This increase in the dissolution rate may be due to the amorphization of the drug during the solid dispersion preparation. The presence of the amorphous form of the drug was shown in the IR spectra.

The aim of the study was to design and evaluate mucoadhesive buccal patches of naproxen for local treatment of pain and inflammations of the oral cavity. Buccal patches were fabricated by solvent casting technique using hydroxypropylmethylcellulose E4M, Eudragit RLPO, ethyl cellulose, polyvinylpyrrolidone, methyl cellulose, hydroxypropylcellulose and chitosan either alone or as mixtures. Ten formulations were subjected to various evaluation parameters. Based on the evaluation of the results, it was concluded that Formula-2 (F-2) containing 1% HPMC and 0.5% Eudragit RLPO showed good mucoadhesive strength (47.07 g), promising controlled and complete drug release within 210 min, highest residence time (120 min in vivo and 125 min in vitro), acceptable elasticity (13.834 %mm-2), swelling index (85.4% in 15 min) and surface pH (6.5). Accordingly, F-2 could be selected as the best formula among the formulations studied and was subject to further in vivo study. The obtained in vivo results indicate that the concentration of naproxen in the oral cavity was maintained above 4 μg/mL for a period of 120 min, which was within and higher than the reported range of the IC50 of naproxen. A significant in vitro/in vivo correlation was obtained (R2 = 0.9787). The results indicate that the mucoadhesive buccal patches of naproxen may be a good choice to bypass the undesirable systemic side effects and can be proposed as a new therapeutic tool against dental and buccal inflammatory diseases and disturbs.

The aim of the study was to design and evaluate mucoadhesive buccal patches of naproxen for local treatment of pain and inflammations of the oral cavity. Buccal patches were fabricated by solvent casting technique using hydroxypropylmethylcellulose E4M, Eudragit RLPO, ethyl cellulose, polyvinylpyrrolidone, methyl cellulose, hydroxypropylcellulose and chitosan either alone or as mixtures. Ten formulations were subjected to various evaluation parameters. Based on the evaluation of the results, it was concluded that Formula-2 (F-2) containing 1% HPMC and 0.5% Eudragit RLPO showed good mucoadhesive strength (47.07 g), promising controlled and complete drug release within 210 min, highest residence time (120 min in vivo and 125 min in vitro), acceptable elasticity (13.834 %mm-2), swelling index (85.4% in 15 min) and surface pH (6.5). Accordingly, F-2 could be selected as the best formula among the formulations studied and was subject to further in vivo study. The obtained in vivo results indicate that the concentration of naproxen in the oral cavity was maintained above 4 μg/mL for a period of 120 min, which was within and higher than the reported range of the IC50 of naproxen. A significant in vitro/in vivo correlation was obtained (R2 = 0.9787). The results indicate that the mucoadhesive buccal patches of naproxen may be a good choice to bypass the undesirable systemic side effects and can be proposed as a new therapeutic tool against dental and buccal inflammatory diseases and disturbs.