Cholesterylbutyrate solid lipid nanoparticles as a butyric acid prodrug.
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 large amounts of the drug would be necessary for its efficacy. In the last few years butyric acid's anti-inflammatory properties and its inhibitory activity towards histone deacetylases have been widely studied, mainly in vitro. Solid Lipid Nanoparticles (SLNs), whose lipid matrix is Chol-but, were prepared to evaluate the delivery system of Chol-but as a prodrug and to test its efficacy in vitro and in vivo. Chol-but SLNs were prepared using the microemulsion method; 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 cell lines and in vivo on a rat intracerebral glioma model. The anti-inflammatory activity was evaluated on adhesion of polymorphonuclear cells to vascular endothelial cells. In the review we will present data on Chol-but SLNs in vitro and in vivo experiments, discussing the possible utilisation of nanoparticles for the delivery of prodrugs for neoplastic and chronic inflammatory diseases.
Brioschi
Andrea
A
Istituto Auxologico Italiano, IRCCS - Department of Neurology - Ospedale S. Giuseppe, Piancavallo, PO. Box 1 - 28921 Verbania, Italy. a.brioschi@auxologico.it
Zara
Gian Paolo
GP
Calderoni
Sara
S
Gasco
Maria Rosa
MR
Mauro
Alessandro
A
D000818:Animals; D016923:Cell Death / Q000187:drug effects; D002788:Cholesterol Esters / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D008055:Lipids / Q000737:chemistry* / Q000494:pharmacology; D053758:Nanoparticles / Q000737:chemistry*; D011355:Prodrugs / Q000737:chemistry* / Q000494:pharmacology
D002788:Cholesterol Esters; D008055:Lipids; D011355:Prodrugs; C092211:cholesteryl butanoate