Recently, for the pharmacokinetic control of target materials, interest has been dedicated toward polymeric nanocarrier systems with surface modifications, since these systems enables efficient drug delivery that could not be achieved by conventional formulation strategies. In this review, our latest outcomes on preparation and biopharmaceutical evaluations of surface-modified polymeric nanocarriers for pharmacokinetic control, especially oral absorption behavior, are presented. For designing the functional nanocarriers like mucoadhesive/penetrative nanoparticles, Flash nanoprecipitation (FNP) approach, a technique for promoting the nucleation over growth of precipitated particles by controlling thermodynamic and kinetic conditions, was strategically applied with combination use of polystyrene (PS)-block-polyethylene glycol or PS-block-polyacrylic acid. As the results from physicochemical, pharmacokinetic, and pharmacodynamic evaluations, either functional nanocarriers could highlight desirable characteristics to control the oral absorption behavior of model drug, cyclosporine A, possibly contributing to enhancing the biopharmaceutical properties.