The large number of cytokines and growth factors implicated in the regulation of liver regeneration has led to the possibility of using these molecules in therapy, namely, in the case of recombinant human hepatocyte growth factor (rhHGF). The importance and potential clinical usefulness of rhHGF has been extensively studied and documented, with results suggesting that this molecule could be a powerful tool toward increased success in hepatic regenerative therapy. However, the peptidic nature of this drug presents several challenges toward its effective administration and targeting. The possibility of encapsulating rhHGF in dextran sulfate/chitosan nanoparticles to allow its oral administration and direct liver-targeting is discussed in this manuscript. Details of a rapid and simple method for the preparation of such rhHGF-loaded nanocomplexes are presented. Beyond the practical aspects of the method, characterization techniques and main experimental features of obtained nanocarriers are also briefly analyzed and discussed.