Self-emulsifying drug delivery system (SEDDS) of Ibuprofen: formulation, in vitro and in vivo evaluation.

The goal of the present study was to develop a self-emulsifying drug delivery system for the oral poorly water-soluble drug ibuprofen and to evaluate its oral bioavailability. Phase diagrams were constructed to determine the phase behaviour of the microemulsions and to compare the efficiency of various surfactant-oil mixtures. The SEDDS formulations of ibuprofen were prepared from a mixture of Labrafil M2125, Cremophor RH40, and Plurol oleique. The prepared emulsions were characterized for in vitro and in vivo behaviour. A FTIR study confirmed there is no interaction between the drug and excipients. DSC studies showed that the drug is in a solubilised form in the self-emulsifying formulations. The formulations were evaluated for thermodynamic stability, dispersibility, refractive index, viscosity and cloud point. Formulations showed a negative charge on globules which indicates their stability. The optimized formulation produced a microemulsion with a globule size of 177.5 nm. The in vitro release profile of the optimized formulation was significantly higher than that of the marketed formulation and pure drug. The anti-inflammatory activity of the optimized formulation was significantly higher than that of the marketed formulation and pure drug. The AUC and Cmax values after oral administration were higher for the ibuprofen SEDDS in comparison with the marketed product. These results suggest that SEDDS of Ibuprofen can be a useful tool to increase the bioavailability and an alternative to enhance the bioavailability of poorly soluble drugs.Key words: ibuprofen self-emulsifying system phase diagram zeta potential, anti-inflammatory activity.