Statistically designed dexibuprofen loaded solid lipid nanoparticles for enhanced oral bioavailability

초록

Dexibuprofen (DBPN), a non-steroidal anti-inflammatory drug (NSAID), exhibit its action by inhibiting COX enzymes. It belongs to BCS class II drugs, owing to its poor dissolution and reduced oral bioavailability. Herein, solid lipid nanoparticles (SLNs) were prepared by modified microemulsion method followed by their optimi-zation via Design-Expert (R) (version 12). The optimized formulation was evaluated using various techniques including, Transmission electron microscopy (TEM), Fourier transform infrared spectrophotometer (FTIR), Powder x-ray diffractometer (PXRD) and Dynamic scanning calorimeter (DSC). In-vitro release and pharmaco-kinetic studies of DBPN-SLNs were executed and compared with drug suspension. A 12-weeks stability study was performed at 4 degrees C and 40 degrees C. Optimized formulation has spherical morphology including particle size (PS) of 213.8 nm, polydispersity index (PDI) of 0.201, zeta potential (ZP) of-33.6 mV and %EE of 92%. FTIR analysis showed no chemical interaction of the constituents of SLNs, whereas XRD and DSC respectively demonstrated the conversion of crystalline drug to amorphous and thermal behavior of the optimized formulation. In-vitro dissolution data indicated that SLNs has momentously retarded the drug release at various pH level when compared with drug suspension. Pharmacokinetic study revealed a significantly enhanced (9-fold) oral bioavailability of DBPN-SLNs than DBPN suspension. Moreover, DBPN-SLNs were stable for at-least 12 weeks. Hence, it can be concluded that incorporation of DBPN into SLNs produce sustained release behavior with improved bioavailability.

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