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Mucoadhesive drug formulations have been studied and used as alternatives to conventional formulations in order to achieve prolonged retention at the intended site. In addition to providing a controlled drug release, several drugs and disease conditions might benefit from mucoadhesive formulations, contributing to better therapeutic outcomes. Here, we describe the development and the in vitro/in vivo characterization of a mucoadhesive in situ gellifying formulation using PF127, a thermo reversible polymer, entrapping budesonide (BUD), a potent corticosteroid used for the treatment of a wide range of inflammatory diseases, including those affecting mucosas, such as in the GI tract. PF127 formulations (15–17%) were successfully prepared by a cold method as a thermo reversible in situ gelling dispersion for mucosal drug delivery, as confirmed by DSC. Sol-gel temperatures of PF127 formulations (25–39 °C) were observed by dynamic gelation and determined by microrheology and oscillatory rheometry. X-ray diffractograms and TEM images showed that BUD was completely solubilized within the polymeric micelles. In vitro , the gels showed 5–14 g force of mucoadhesion, and the ex vivo studies confirmed that the formulation efficiently adhered to the mucosa. Histopathological analysis combined with fluorescence images and ex vivo intestinal permeation confirmed that the formulation remained on the TGI mucosa for at least 4 h after administration. In vivo studies conducted in a murine model of intestinal mucositis demonstrated that the 16% PF127 BUD formulation was able to resolve the inflammatory injury in the intestinal mucosa. Results demonstrate that fine-tuning of PF127 formulations along with adequate selection of the drug agent, thorough characterization of the dispersions and their interactions with biological interfaces leads to the development of effective controlled drug delivery systems targeted to GI inflammatory diseases. Unlabelled Image [ABSTRACT FROM AUTHOR]

Context: Ketoprofen is a non-steroid anti-inflammatory drug (NSAID) used in the treatment of rheumatic diseases and in mild to moderate pain. Ketoprofen has a short biological half-life and the commercially available conventional release formulations require dosages to be administered at least 2-3 times a day. Due to these characteristics, ketoprofen is a good candidate for the preparation of controlled release formulations. Objectives: In this work, a multiparticulate-sustained release dosage form containing ketoprofen in a carnauba wax matrix was developed. Methods: Particles were prepared by an emulsion congealing technique. System variables were optimized using fractional factorial and response surface experimental design. Characterization of the particles included size and morphology, flow rate, drug loading and in vitro drug release. Results: Spherical particles were obtained with high drug load and sustained drug release profile. The optimized particles had an average diameter of approximately 200 µm, 50% (w/w) drug load, good flow properties and prolonged ketoprofen release for more than 24 h. Conclusions: Carnauba wax microspheres prepared in this work represent a new multiparticulate-sustained release system for the NSAID ketoprofen, exhibiting good potential for application in further pharmaceutical processes. [ABSTRACT FROM AUTHOR]