Modeling of ketoprofen release from a mucoadhesive orodental gel for better control of dental pain and gingivitis

Abstract

This research paper addressed the formulation and performance of a mucoadhesive gel containing the anti-inflammatory drug ketoprofen. Various polymers were used in the formulation at different levels together with different types of crosslinking additives. The compatibility between ketoprofen and the employed polymers was tested using differential scanning calorimetry (DSC). Sustained release profiles were obtained from gels containing pluroic F127, carbopol981 and polycarbophil.  Fast release was obtained from sodium alginate and HPMC at low levels. Response surface modeling of the release data indicated that the optimum ketoprofen release rates (44-58 %) were obtained from gel formulations containing carbopol 981 at 1% w/w level. Gel formulations containing sodium alginate (5 % w/w) released more than 40 % of their content of ketoprofen within two hours. The fastest rate was obtained from formulations containing hydroxylpropyl methylcellulose (HPMC E15) where, more than 90 % of the drug content was released at polymer level of 20 % w/w as obtained from model optimized formulations. The clinical evaluation of the anti-inflammatory and analgesic action of the prepared formulations compared to commercial ketoprofen tablets indicated significant difference (P < 0.05) in pain intensity and swelling associated with ginigivitis in favor of the gel formulation over the oral tablet. Therefore, formulation of ketoprofen into a mucoadhesive orodental gel can be considered an easy and more effective alternative to oral solid dosage forms.