Amphiphilic hyper-branched co-polymer nanoparticles for the controlled delivery of anti-tumor agents

Qinghua Miao, Dongxue Xu, Zhi Wang, Li Xu, Tiewei Wang, Yan Wu, David B. Lovejoy, Danuta S. Kalinowski, Des R. Richardson, Guangjun Nie, Yuliang Zhao

Research output: Contribution to journalArticlepeer-review

49 Scopus citations


In this investigation, we have designed and synthesized an amphiphilic co-polymer with hyper-branched poly(amine-ester) and polylactide (HPAE-co-PLA) to generate nanoparticles (NPs). These have been used to encapsulate a highly active hydrophobic anti-tumor agent, 2-benzoylpyridine 4-ethyl-3-thiosemicarbazone (Bp4eT). Encapsulation in NPs was done in an effort to increase the anti-tumor activity of this agent by facilitating its delivery to tumor cells. We have also examined and optimized the formulation parameters of the NPs that alter their drug-loading capacity and their physical, chemical and biological properties. The resulting NPs exhibited high Bp4eT-loading capacity and substantial stability in aqueous solution. In vitro drug release studies demonstrated a controlled drug release profile with increased release at acidic pH. Anti-tumor proliferation assays showed that both free drug and drug-encapsulated NPs markedly inhibited tumor cell proliferation in a time- and concentration-dependent manner. Direct microscopic observation revealed that the fluorescent NPs were taken up by cells and localized, in part, in organelles consistent with lysosomes. These results demonstrate a feasible application of the amphiphilic hyper-branched co-polymer, HPAE-co-PLA, as nanocarriers for intracellular delivery of potent anti-tumor agents.

Original languageEnglish (US)
Pages (from-to)7364-7375
Number of pages12
Issue number28
StatePublished - Oct 2010


  • Controlled drug release
  • Cytotoxicity
  • Drug delivery
  • Nanoparticle

ASJC Scopus subject areas

  • Biomaterials
  • Bioengineering
  • Ceramics and Composites
  • Mechanics of Materials
  • Biophysics


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