For a targeted drug delivery, it was great biomedical potential, significance, importance and application value to construct a colloidal-chemistry stable nanocomposite. Functionalized multi-walled carbon (MWNTs-(OX)) has attracted considerable attention due to the unique atomic structure, strong cell membrane penetration, specific surface area and low toxicity. It has also been used widely for targeted drug delivery as an ideal nanocomposite. In this paper, a facile one-pot strategy to MWNTs-(OX) with hyperbranched polyglycerol (PG) by surface-initiated ring-opening polymerization of glycidol was used to form MWNTs-(OX)-PG. Then, the partial periphery of PG layer was converted to carboxy groups and covalently linked to FA to form MWNTs-(OX)-PG-COOH-FA. Meanwhile, the properties of MWNTs-(OX,) MWNTs-(OX)-PG, MWNTs-(OX)-PG-COOH and MWNTs-(OX)-COOH-FA were characterized by Fourier transform infrared (FT-IR), Ultraviolet-visible spectrophotometry (UV), Thermogravimetric analysis (TGA), Scanning transmission electron microscopy (STEM) and elemental analysis, and the results indicated that MWNTs-(OX)-PG-COOH-FA preformed excellent dispersity, interface stability and long-term storage. This paper opened up a new strategy to rational design folic acid-functionalized MWNTs-(OX)-PG multifunctional nanohybrids as biomaterials. [GRAPHICS] .