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Cholesterylbutyrate Solid Lipid Nanoparticles as a Butyric Acid Prodrug
Istituto Auxologico Italiano, IRCCS – Department of Neurology – Ospedale S. Giuseppe, Piancavallo, PO. Box 1 – 28921 Verbania, Italy
University of Torino – Department Anatomy Pharmacology Forensic Medicine – Torino, Italy
Istituto Auxologico Italiano, IRCCS – Department of Neurology – Laboratory of Clinical Neurobiology – Verbania, Italy
Nanovector S.r.l. – Torino, Italy
University of Torino – Departement of Neurosciences – Torino, Italy
* Author to whom correspondence should be addressed.
Received: 4 January 2008; in revised form: 31 January 2008 / Accepted: 1 February 2008 / Published: 1 February 2008
(This article belongs to the Special Issue Prodrugs
Abstract: Cholesterylbutyrate (Chol-but) was chosen as a prodrug of butyric acid.Butyrate is not often used in vivo because its half-life is very short and therefore too largeamounts of the drug would be necessary for its efficacy. In the last few years butyric acid'santi-inflammatory properties and its inhibitory activity towards histone deacetylases havebeen widely studied, mainly in vitro. Solid Lipid Nanoparticles (SLNs), whose lipid matrixis Chol-but, were prepared to evaluate the delivery system of Chol-but as a prodrug and totest its efficacy in vitro and in vivo. Chol-but SLNs were prepared using the microemulsionmethod; their average diameter is on the order of 100-150 nm and their shape is spherical.The antineoplastic effects of Chol-but SLNs were assessed in vitro on different cancer celllines and in vivo on a rat intracerebral glioma model. The anti-inflammatory activity wasevaluated on adhesion of polymorphonuclear cells to vascular endothelial cells. In thereview we will present data on Chol-but SLNs in vitro and in vivo experiments, discussingthe possible utilisation of nanoparticles for the delivery of prodrugs for neoplastic andchronic inflammatory diseases.
Keywords: Cholesterylbutyrate; Solid Lipid Nanoparticles; Butyric Acid; Cancer; Brain Tumours; Inflammatory Diseases.
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MDPI and ACS Style
Brioschi, A.; Zara, G.P.; Calderoni, S.; Gasco, M.R.; Mauro, A. Cholesterylbutyrate Solid Lipid Nanoparticles as a Butyric Acid Prodrug. Molecules 2008, 13, 230-254.
Brioschi A, Zara GP, Calderoni S, Gasco MR, Mauro A. Cholesterylbutyrate Solid Lipid Nanoparticles as a Butyric Acid Prodrug. Molecules. 2008; 13(2):230-254.
Brioschi, Andrea; Zara, Gian P.; Calderoni, Sara; Gasco, Maria R.; Mauro, Alessandro. 2008. "Cholesterylbutyrate Solid Lipid Nanoparticles as a Butyric Acid Prodrug." Molecules 13, no. 2: 230-254.