FORMULATION AND IN VITRO CHARACTERIZATION OF THE SOLID LIPID NANOPARTICLES OF NAFTOPIDIL FOR ENHANCING ORAL BIOAVAILABILITY

Abstract

Objective: Naftopidil (NAF) is a selective alpha1-adrenergic receptor antagonist with a nearly 20% bioavailability due to poor aqueous solubility, permeability, and extensive first-pass metabolism. To improve the bioavailability of the NAF, the solid lipid nanoparticles (SLN) of NAF were prepared. Methods: SLNs NAF were prepared using the solvent emulsification/evaporation method with excipients Compritol 888 ATO and Poloxamer 188. Formulation F10 shows better entrapment efficiency (EE) as compare to other formulations so, it has selected to optimize the particle size, zeta potential, surface morphology, Fourier transform infrared spectroscopy (FTIR), and in vitro drug release and stability studies were assessed. Results: The results showed that NAF was successfully incorporated in SLN. Having EE of all formulations ranged from 56% to 88%, drug loading ranged from 17% to 20%, drug content ranged from 77% to 98%, particle size and zeta potential of F10 were 270.2 nm and 21.7 mV, respectively, and FTIR revealed no interaction between drug and lipid in the formulation. The release of NAF-SLNs increased significantly, reaching a maximum of 4.547–82.418% in pH 6.8 buffer, the release data were fitted into the Korsmeyer-Peppas model yielding the highest correlation coefficient (R2=0.916). The stability study revealed that the formulation stability and bioavailability might be improved. Conclusion: It can be concluded that SLN could be effective nanoplatforms for increasing NAF oral bioavailability.