Dimeric camptothecin-loaded mPEG-PCL nanoparticles with high drug loading and reduction-responsive drug release

  • Yanwei Chi
  • Zhiying Wang
  • Jie Wang
  • Wenpei Dong
  • Pengyang Xin
  • Jingjing Bi
  • Tao JiangEmail author
  • Chang-Po ChenEmail author
Original Contribution


Camptothecin (CPT) is a potent and broad-spectrum anti-tumor drug, but its clinical application is limited due to its poor water solubility, toxicity, and low drug-loading potential. Different delivery protocols have been developed to optimize the therapeutic effects of CPT. In this study, CPT was modified into a dimer (CPT-Mal-CPT), in which two CPT molecules are connected by a reduction-responsive maleimide thioether bond. Moreover, biocompatible methoxy poly(ethylene glycol)-b-poly(ε-caprolactone) (mPEG–PCL)-loaded CPT-Mal-CPT nanoparticles were prepared to overcome the limits of CPT application. The power X-ray diffractometer (PXRD) results indicate low crystallinity and amorphous nature of CPT-Mal-CPT. The CPT-Mal-CPT-loaded micelles showed a drug-loading content of 9.6% and a drug-loading efficiency of 56%. In addition, dimeric CPT micelles showed reduction-responsive release under 10-mM dithiothreitol (DTT), while negligible CPT release was detected in the absence of DTT. MTT assay indicated that cytotoxicity of dimeric CPT micelle was similar to free CPT.


mPEG-PCL Dimer Camptothecin Reduction-responsive Drug delivery 


Funding information

This work was supported by the Natural Science Project of the Education Department of Henan Province Natural Science Project(15A150053).

Compliance with ethical standards

Conflict of interest

The authors declare that they have no conflict of interest.

Supplementary material

396_2019_4581_MOESM1_ESM.pdf (235 kb)
ESM 1 (PDF 235 kb)


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Copyright information

© Springer-Verlag GmbH Germany, part of Springer Nature 2019

Authors and Affiliations

  1. 1.Collaborative Innovation Center of Henan Province for Green Manufacturing of Fine Chemicals, School of Chemistry and Chemical EngineeringHenan Normal UniversityXinxiangPeople’s Republic of China

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