Mefenamic acid modified-release by encapsulation in a k-carrageenan/sericin blend

Abstract

Multiple dosages of mefenamic acid have been reported to result in side effects such as gastrointestinal discomfort, headaches and fatigue. Therefore, a modified release system for this drug could improve patient well-being and treatment adhesion. In this study, we developed a carrier based on k-carrageenan and sericin biomacromolecules. The produced particles presented great encapsulation rates, above 86.19 % and drug loading above 48.85 % In addition, the beads had a reproducible spherical shape and size ranging from 1.28 to 1.46 mm. The presence of the Active Pharmaceutical Ingredient (API) and its compatibility with the matrix were verified by XRD, SEM and FTIR. The in vitro release in simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 9.0) without enzymes were less than 10 % and up to 100 %, respectively, which suggests gastroresistance. The release kinetics followed the Weibull model (R2adj 0.787–0.9922 and AIC 65.9798–36.7948) and indicated a release mechanism based on matrix swelling, polymer chain relaxation and erosion. Cell viability assay in the intestinal cell model Caco-2 showed that the blend and placebo were not cytotoxic (cell viability > 84 %), therefore suggesting citocompability. demonstrating that the carrier is biocompatible. Our results suggest that the proposed polymer matrix is capable of a high mefenamic acid loading, with in vitro indication of a sustained release of mefenamic acid for intestinal delivery, compatible with the gastrointestinal tissue.