SCIENCE CHINA Materials, Volume 61 , Issue 11 : 1404-1419(2018) https://doi.org/10.1007/s40843-018-9242-3

Dendrimer-based nanoparticles in cancer chemotherapy and gene therapy

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  • ReceivedFeb 6, 2018
  • AcceptedMar 5, 2018
  • PublishedApr 11, 2018


This review discusses recent studies on dendrimer-based nanoparticles in cancer chemotherapy and gene therapy. In order to achieve the high efficacy and low side effects of chemotherapy and gene therapy, it is essential to combine the unique features of dendrimers and the specific tumor microenvironment to target delivery and control release of therapeutic agents to tumor tissues and cells. Strategies to design the dendrimer-based delivery system in this review include non-modified dendrimers, dendrimer conjugates, assembled amphiphilic dendrimers, nanohybrid dendrimer carriers and dendrimers with inherent activity. In addition, specific functional groups on these dendrimers as stimuli-responsive system for targeting delivery and controlled release of therapeutic agents are discussed.

Funded by

the National Natural Science Foundation of China(81601594,51690153,21474045,21720102005)


This work was supported by the National Natural Science Foundation of China (81601594, 51690153, 21474045 and 21720102005).

Interest statement

The authors declare that they have no conflict of interest.

Contributions statement

Jiang L, Zhou S, Zhang X and Wu W wrote the paper; Jiang L and Jiang X designed the outlines.

Author information

Lei Jiang is an assistant porfessor of the School of Pharmacy in China Pharmaceutical University. She received her PhD degree from Shenyang Pharmaceutical University. She was a postdoctoral fellow at MOE Key Laboratory of High Performance Polymer Materials and Technology, and the Department of Polymer Science & Engineering, College of Chemistry & Chemical Engineering in Nanjing University.

Sensen Zhou received his BSc degree in polymer science and engineering from Heifei University of Technology in 2015. Now, he is a PhD candidate at Nanjing University. His current research interests include the design of biomaterials in drug delivery and bioimaging.

Xiqun Jiang is a professor of MOE Key Laboratory of High Performance Polymer Materials and Technology, and the Department of Polymer Science & Engineering, College of Chemistry & Chemical Engineering in Nanjing University. He is the winner of the National Science Foundation for Distinguished Young Scholars of China.


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  • Scheme 1

    A scheme showing the exploration of dendrimer-based NPs in cancer chemotherapy and gene therapy.

  • Figure 1

    Dendrimer-drug complexes: (a) nonmodified dendrimers-drug complexes; (b) ligand modified PEGylated dendrimers-drug complexes; (c) sensitive bonds cross-linked dendrimers-drug complexes, (d) sensitive bonds as linker on dendrimers-drug complexes.

  • Figure 2

    Dendrimer-drug conjugates: (a) dendrimer–drug conjugate by a hydrazone linkage; (b) dendrimer-drug conjugate by a boronate ester bond; (c) dendrimer-drug conjugate by disulfide bond; (d) dendrimer-drug conjugate via GFLG or (e) collagen peptide; (f) dendrimer-drug conjugate by light-responsive bonds.

  • Figure 3

    Schematic illustrations of (a) molecular and supramolecular engineering on tumor-specific multiple stimuli activated dendrimeric nanoassemblies with metabolic blockade and (b) their synergistic effects for overcoming physiological barriers and cellular factors of chemotherapy resistance. Reprinted from Ref. [106]. Copyright 2017, the American Chemical Society.

  • Figure 4

    (a) Schematic of the cluster-bomb-like nanoassembly and how it accomplishes the CAPIR cascade. (b) The nanoassembly structure: the dendrimers were self-assembled with DOPE and DSPE-PEG lipids as well as cholesterol to form the nanoassembly with a dendrimer core and lipidic shell, which was confirmed by cryo-TEM imaging. Scale bar = 50 nm. Reprinted from Ref [109]. Copyright 2014, WILEY-VCH.

  • Figure 5

    (a) Chemical structures of the TRPDs and (b) G4 PATU dendrimer.

  • Figure 6

    (a) Lysine, (b) arginine and (c) histidine modified dendrimers.

  • Figure 7

    Liver cancer cells were treated with (a) nonmodified or (b) pHLIP conjugated PLL NPs at pH 6.0 (for representing tumor acidic pH environments and solid tumor cells) or pH 7.4 for 30 min. Reprinted from Ref. [165]. Copyright 2013, WILEY-VCH.

  • Figure 8

    Structures of dendrimer-bearing lipids.

  • Figure 9

    Structures of nanoparticle-modified dendrimers. (a) Dendrimer-conjugated quantum dot, (b) dendrimer-conjugated gold nanoparticle, and (c) dendrimer-conjugated Fe3O4.

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