Manipulation of pH-Sensitive interactions between podophyllotoxin-chitosan for enhanced controlled drug release

Chao Chen, Yong Yu, Xiaoli Wang, Ping Shi, Yibing Wang, Ping Wang

Research output: Contribution to journalArticlepeer-review

30 Scopus citations


Podophyllotoxin (PPT) offers a broad-spectrum of anticancer activities, but little has been reported for its controlled release. This work shows that by manipulating molecular interactions between PPT and Chitosan, efficient nanoscale capsulation of PPT can be realized. The drug encapsulation efficiency is as high as 52%, with a final particle drug loading in the order of 10% (wt/wt). It further demonstrates that changes in pH can also significantly affect the rate of drug release from the Chitosan nanoparticles. Upon contact with cancer cells, chitosan nanoparticles enable efficient internalization and drug release. In vitro evaluations with HepG-2 and MCF-7 cells indicate that the chitosan nanoparticle carriers can improve drug efficacy in comparison to free PPT, most likely by regulating the intrinsic apoptotic signaling pathway to induce apoptosis. Overall, PPT chitosan nanoparticles promise a safe and efficient drug delivery system for PPT.

Original languageEnglish (US)
Pages (from-to)451-461
Number of pages11
JournalInternational Journal of Biological Macromolecules
StatePublished - Feb 1 2017

Bibliographical note

Funding Information:
This work was supported by the National Natural Science Foundation of China ( 21303050 and 31471659 ), the China Postdoctoral Science Foundation ( 2015M571511 ), and the Fundamental Research Funds for the Central Universities ( WF1113014 and 222201514327 ). Authors thank the support from Jiangsu National Synergetic Innovation Center for Advanced Materials (SICAM).

Publisher Copyright:
© 2016 Elsevier B.V.


  • Cancer treatment
  • Chitosan nanoparticles
  • Controlled release
  • Podophyllotoxin
  • pH-sensitivity


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