The present study reports the significance of polymeric nanoparticles in oral drug delivery from pharmacokinetic perspective. Impact of different dose polymeric nanoparticulate formulations on various pharmacokinetic parameters has been reported. All nano-formulations were found to have significant effect on important pharmacokinetic parameters like C(max), T(max), AUC, absolute bioavailability, absorption rate constant (K(a)), elimination rate constant (K(el)), elimination half life (t(1/2)), mean residence time (MRT) and mean absorption time (MAT). Further, drug in polymeric nanoparticles exhibited the flip-flop pharmacokinetics suggesting its slow and sustained release from the polymeric matrix. Together, polymeric nanoparticles hold promise for the oral delivery of molecules having pharmacokinetic hurdles in their delivery approach.