Assembled liposomes of dual podophyllotoxin phospholipid: preparation, characterization and in vivo anticancer activity

Nanomedicine (Lond). 2017 Mar;12(6):657-672. doi: 10.2217/nnm-2016-0396. Epub 2017 Feb 21.

Abstract

Aim: A novel amphiphilic prodrug dual podophyllotoxin (PPT) succinate glycerophosphorylcholine (Di-PPT-GPC) assembled liposomes was developed to improve efficiency of PPT.

Materials & methods: Di-PPT-GPC liposomes were prepared by thin film technique and characterized by dynamic light scattering and cryo-electron microscopy.

Results: In vitro release studies showed that Di-PPT-GPC liposomes could significantly release PPT in weakly acidic environment but had good stability under biological conditions. Methyl tetrazolium assay data revealed that the liposomes have comparable cytotoxicities to free PPT against MCF-7, HeLa and U87 cells. More importantly, in vivo antitumor evaluation indicated that Di-PPT-GPC liposomes exhibited favorable tumor growth inhibition without side effects.

Conclusion: Di-PPT-GPC liposomes might have potential to promote the therapeutic effect of PPT for cancer therapy.

Keywords: anticancer activity; liposomes; podophyllotoxin; prodrug; self-assembly.

MeSH terms

  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / chemistry
  • Cell Proliferation / drug effects
  • HeLa Cells
  • Humans
  • Liposomes / administration & dosage*
  • Liposomes / chemistry
  • MCF-7 Cells
  • Neoplasms / drug therapy*
  • Phospholipids / administration & dosage*
  • Phospholipids / chemistry
  • Podophyllotoxin / administration & dosage*
  • Podophyllotoxin / chemistry

Substances

  • Antineoplastic Agents
  • Liposomes
  • Phospholipids
  • Podophyllotoxin