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Development of Zwitterionic Polypeptide Nanoformulation with High Doxorubicin Loading Content for Targeted Drug Delivery

  • Weifeng Lin
  • , Guanglong Ma
  • , Zhefan Yuan
  • , Haofeng Qian
  • , Liangbo Xu
  • , Elie Sidransky
  • , Shengfu Chen*
  • *Corresponding author for this work
  • Zhejiang University
  • University of Maryland, College Park
  • Nanjing Normal University

Research output: Contribution to journalArticlepeer-review

Abstract

Much attention has been drawn to targeted nanodrug delivery systems due to their high therapeutic efficacy in cancer treatment. In this work, doxorubicin (DOX) was incorporated into a zwitterionic arginyl-glycyl-aspartic acid (RGD)-conjugated polypeptide by an emulsion solvent evaporation technique with high drug loading content (45%) and high drug loading efficiency (95%). This zwitterionic nanoformulation showed excellent colloidal stability at high dilution and in serum. The pH-induced disintegration and enzyme-induced degradation of the nanoformulation were confirmed by dynamic light scattering and gel permeation chromatography. Efficient internalization of DOX in the cells and high antitumor activity in vitro was observed. Compared with the free drug, this nanoformulation showed higher accumulation in tumor and lower systemic toxicity in vivo. The DOX-loaded zwitterionic RGD-conjugated polypeptide vesicles show potential application for targeted drug delivery in the clinic.

Original languageEnglish
Pages (from-to)1273-1283
Number of pages11
JournalLangmuir
Volume35
Issue number5
DOIs
StatePublished - 5 Feb 2019
Externally publishedYes

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

  1. SDG 3 - Good Health and Well-being
    SDG 3 Good Health and Well-being

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