Liposomes as vehicles for water insoluble platinum-based potential drug: 2-(4-(tetrahydro-2H-pyran-2-yloxy)-undecyl)-propane-1,3-diamminedichloroplatinum(II)

Eur J Med Chem. 2012 Aug:54:567-72. doi: 10.1016/j.ejmech.2012.06.004. Epub 2012 Jun 13.

Abstract

Formulation of liposome delivery system loaded with water insoluble 2-(4-(tetrahydro-2H-pyran-2-yloxy)-undecyl)-propane-1,3-diamminedichloroplatinum(II), LipoTHP-C11 was carried out. The particle size distributions were determined by dynamic light scattering and asymmetrical flow field-flow fractionation indicating size of around 120 nm. Stability study showed that LipoTHP-C11 was stable at 4 °C for more than two months. To test suitability of chosen formulation, LipoTHP-C11 was investigated against several tumor cell lines: H12.1, 1411HP, 518A2, A549, HT-29, MCF-7 and SW1736. Furthermore, toxicity against normal fibroblasts was examined. LipoTHP-C11 may be used as an attractive candidate for further assessment in vivo as antitumor agent.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / administration & dosage*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Humans
  • Inhibitory Concentration 50
  • Liposomes
  • Organoplatinum Compounds / administration & dosage*
  • Organoplatinum Compounds / chemistry
  • Organoplatinum Compounds / pharmacology*
  • Solubility
  • Water / chemistry*

Substances

  • 2-(4-(tetrahydro-2H-pyran-2-yloxy)undecyl)propane-1,3-diamminedichloroplatinum(II)
  • Antineoplastic Agents
  • Liposomes
  • Organoplatinum Compounds
  • Water