4.7 Article

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

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 54, Issue -, Pages 567-572

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.06.004

Keywords

Cisplatin; Platinum(II) complexes; Liposomes; Antitumoral activity; Selectivity

Funding

  1. Ministerium fur Wirtschaft und Arbeit des Landes Sachsen-Anhalt, Deutschland [6003368706]
  2. BioSolutions Halle GmbH

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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 degrees 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. (C) 2012 Elsevier Masson SAS. All rights reserved.

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