Molecules 2008, 13(2), 230-254; doi:10.3390/molecules13020230

Cholesterylbutyrate Solid Lipid Nanoparticles as a Butyric Acid Prodrug

1,* email, 2, 3, 4 and 1
Received: 4 January 2008; in revised form: 31 January 2008 / Accepted: 1 February 2008 / Published: 1 February 2008
(This article belongs to the collection Prodrugs)
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
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.

AMA Style

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.

Chicago/Turabian Style

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.

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