Water dispersible and biocompatible polyPEGylated ND nanoparticles were prepared via surface-initiated atom transfer radical polymerization. Cell internalization study reveals that ND nanoparticles facilitate the transport of doxorubicin hydrochloride into A549 cells, indicating their potential applications in cancer therapy.Over the past few decades, carbon nanomaterials (CNMs) have attracted a great deal of scientific and technological attention due to their unique structure and remarkable electronic, mechanical and thermal properties. These materials have shown promising applications in different fields such as electronics, energy conversion and storage, and biomedicine etc. 1-6 Nanodiamond (ND) is a relative new class of CNM, which has been investigated extensively for biomedical applications in recent years due to its excellent physicochemical properties, biocompatibility, inexpensive large scale synthesis and small size (2-10 nm). 7-18 It has been reported that fluorescent ND nanoparticles could be used as bioprobes for single particle tracing in cells and even in small organisms such as Caenorhabditis elegans. [19][20][21] It has also been suggested that ND might be useful for controlled drug delivery and gene therapy as well as tissue engineering. 22-26 For many of these biomedical applications, effective dispersion of ND in aqueous solution especially in physiological solution is necessary. On the other hand, like many other nanomaterials, ND nanoparticles are readily recognized as foreigners by the mononuclear phagocytic system (MPS) of cells and are rapidly cleared from blood circulation after intravenous administration, resulting in cumulative negative effects on the MPS and leading to impairment of this vital host defence system. 27-31 Therefore, effective dispersion of ND in aqueous media and preventing it from recognition by the MPS are crucial for the practical biomedical applications of ND.Polyethylene glycol (PEG) is a class of hydrophilic polymer with outstanding physicochemical and biological properties, such as excellent water-solubility and biocompatibility. 32,33 The conjugation of PEG chains on the nanoparticle surface (PEGylation) is expected to render nanoparticle dispersion as well as reduce protein opsonization and subsequent phagocytosis by MPS to the nanoparticles, which can help these PEGylated nanoparticles escape from the reticuloendothelial system (RES) after intravenous administration. To date, PEGylation of many nanoparticles, such as liposome, quantum dots, gold nanoparticles, carbon nanotubes and other nanomaterials could extremely reduce the nanoparticles' uptake by MPS and prolong their blood circulation time. [34][35][36][37][38] Our previous study has demonstrated that PEG or polyPEGMA molecules could be immobilized onto the surface of ND via both ''grafting to'' and ''grafting from'' methods. 39 The polyPEGMA conjugated ND showed enhanced dispersibility in both aqueous and organic media.In current work, we present the polyPEGylation of ND through surface-initiated atom t...