Journal of Pharmaceutical Sciences 2014-07-01

Solid lipid nanoparticles for potential doxorubicin delivery in glioblastoma treatment: preliminary in vitro studies.

Luigi Battaglia, Marina Gallarate, Elena Peira, Daniela Chirio, Elisabetta Muntoni, Elena Biasibetti, Maria Teresa Capucchio, Alberto Valazza, Pier Paolo Panciani, Michele Lanotte, Davide Schiffer, Laura Annovazzi, Valentina Caldera, Marta Mellai, Chiara Riganti

Index: J. Pharm. Sci. 103(7) , 2157-65, (2014)

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Abstract

The major obstacle to glioblastoma pharmacological therapy is the overcoming of the blood-brain barrier (BBB). In literature, several strategies have been proposed to overcome the BBB: in this experimental work, solid lipid nanoparticles (SLN), prepared according to fatty acid coacervation technique, are proposed as the vehicle for doxorubicin (Dox), to enhance its permeation through an artificial model of BBB. The in vitro cytotoxicity of Dox-loaded SLN has been measured on three different commercial and patient-derived glioma cell lines. Dox was entrapped within SLN thanks to hydrophobic ion pairing with negatively charged surfactants, used as counterions. Results indicate that Dox entrapped in SLN maintains its cytotoxic activity toward glioma cell lines; moreover, its permeation through hCMEC/D3 cell monolayer, assumed as a model of the BBB, was increased when the drug was entrapped in SLN. In conclusion, SLN proved to be a promising vehicle for the delivery of Dox to the brain in glioblastoma treatment.© 2014 Wiley Periodicals, Inc. and the American Pharmacists Association.