Effect of long-term stabilization of cationic liposomes as defibrotide delivery system for antithrombotic activity

Journal Article (Journal Article)

The general goal of this study was to produce cationic liposome formulations suitable for the in vivo administration of defibrotide (DFT) (a DNA-based drug) and to investigate in vitro and in vivo the stability of such a formulation. This article describes the freeze-drying of cationic liposomes using as cryoprotectants different carbohydrates, such as sorbitol, mannitol, and sucrose. Liposome characteristics before and after freeze-drying, such as size, morphology, and ability in complexing a DNA-based drug, have been investigated. The in vitro studies indicate that cationic liposomes sufficiently maintain the initial characteristics after lyophilization and rehydration including the ability to complex DFT. The in vivo data show that lyophilized cationic liposome formulations can be safely stored for at least 3 months. Before in vivo use, liposomes can be rehydrated with DFT solutions, resulting in the formation of stable complexes retaining an in vivo activity comparable to that of the freshly prepared formulation. © 2002 Wiley-Liss, Inc.

Full Text

Duke Authors

Cited Authors

  • Esposito, E; Cortesi, R; Porta, R; Trento, F; Nastruzzi, C

Published Date

  • January 1, 2002

Published In

Volume / Issue

  • 55 / 2

Start / End Page

  • 127 - 138

International Standard Serial Number (ISSN)

  • 0272-4391

Digital Object Identifier (DOI)

  • 10.1002/ddr.10041

Citation Source

  • Scopus