Ultrasound-mediated destabilization and drug release from liposomes comprising dioleoylphosphatidylethanolamine
ForfatterEvjen, Tove Julie; Nilssen, Esben A.; Barnert, Sabine; Schubert, Rolf; Brandl, Martin; Fossheim, Sigrid L
Novel sonosensitive doxorubicin-containing liposomes comprising dioleoylphosphatidylethanolamine (DOPE) as the main lipid constituent were developed and characterized in terms of ultrasound-mediated drug release in vitro. The liposome formulation showed high sonosensitivity; where approximately 95% doxorubicin was released from liposomes after 6 min of 40 kHz US exposure in buffered sucrose solution. This represented a 30% increase in release extent in absolute terms compared to liposomes comprising the saturated lipid analogue distearoylphosphatidylethanolamine (DSPE), and a 9-fold improvement in release extent when compared to standard pegylated liposomal doxorubicin, respectively. Ultrasound release experiments in the presence of serum showed a significantly reduction in sonosensitivity of DSPE-based liposomes, whilst the release properties of DOPE-based liposomes were essentially maintained. Dynamic light scattering measurements and cryo-transmission electron microscopy of DOPE-based liposomes after ultrasound treatment indicated liposome disruption and formation of various lipid structures, corroborating the high release extent. The results point to the potential of DOPE-based liposomes as a new class of drug carriers for ultrasound-mediated drug delivery.
This article is part of Tove Julie Evjen's doctoral thesis. Available in Munin at http://hdl.handle.net/10037/3373
SiteringEuropean Journal of Pharmaceutical Sciences 42(2011) nr. 4 s. 380-386
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