Formulation Design, Optimization and Characterization of Eprosartan Mesylate Nanoparticles

Introduction: Polymeric nanoparticles loaded with eprosartan mesylate by nano precipitation technique have been prepared for improving the solubility and dissolution rate. It is a BCS class- II, water insoluble antihypertensive drug with 13% oral bioavailability. Polymeric nanoparticles of such drug were developed using Eudragit L-100 and S-100 as polymers by nano precipitation method. FT-IR and DSC studies reveal that drug is compatible with the selected polymers and it does not show any extra peaks. Materials and Method: PEG 200 was used as a non-volatile, non toxic solvent to dissolve the selected drug and polymers Poloxamer 188 and Gelucire 44/14 were used as surfactant-cum stabilizer for stabilization of formed nano dispersion. Optimization of formulations by 22 central composite design has been employed to find out the robust formulation by selecting concentration of Eudragit L-100 as polymer and polaxamer 188 as stabilizer for the selected responses like entrapment efficiency, particle size, zeta potential and polydispersibility index. Prepared polymeric nanoparticles were further characterized for particle size, zeta potential, entrapment efficiency and in-vitro drug release. Result: From the study, Eudragit L-100 and poloxamer 188 based formulations formed stable nanoparticles with good entrapment efficiency as well as better drug solubility or dissolution rate in PEG 200 as compared to Eudragit S-100 based formulations. Short term stability study for an optimized run (R3) up to 3 months showed stability without significant variation of entrapment efficiency and in vitro dissolution rate. Conclusion: Dissolution kinetic data and diffusion exponent values suggested that optimized formulation followed Higuchi model with non-Fickian transport mechanism.