Abstract

Background: Ibuprofen (IBU), drug choice of non-steroidal anti-inflammatory and analgesic, which were formulated in nanosuspension dosage to improve its therapeutic efficacy. Objective: The aim of the study is to develop and evaluate sustained release ibuprofen nanosuspension by using Eudragit RL100 polymer using preliminary optimized ratio of drug to polymer. Method: Nano-precipitation method was used to prepare IBU nanosuspension. Type of surfactant or stabilizer (Formulation variable) and stirring time (Process variable) were varied to optimize the formulation. Characterization of the nanosuspension was performed by measuring particles size, zeta potential, drug entrapment efficiency, drug loading capacity and in-vitro drug release studies. In vivo pharmacodynamic studies were also carried out on rats. Results: Drug:polymer (1:5) was found to be effective and optimized ratio for further studies. On the basis of result out of F1-F10 formulations, F2 showed, smallest particle size of 240 nm, zeta potential 21.2 mV, entrapment efficiency of 74.92%. SEM image showed that the nanoparticles were spherical in shape with smooth surface. FTIR showed no significant interactions between Eudragit and drug even after encapsulation. In vitro release from the nanosuspension showed biphasic sustained release the drug action. From the in vivo (anti-inflammatory activity) studies revealed that prepared nanosuspension sustained its action for longer period of time. Conclusion: Thus, it can be concluded that IBU loaded nanosuspension considered useful approach for sustained drug release and reduce dosing frequency.

Keywords: Anti-inflammatory, eudragit RL100, ibuprofen, nanosuspension, sustained release.

Graphical Abstract