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 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.
Highlights
Different colloidal drug delivery systems, were developed to overcome physicochemical limitations of potential therapeutical compounds such as poor solubility, low permeability, short half-life, high molecular weight, side effects and systemic toxicity [1, 2]
This drug was chosen to demonstrate that Tobramycin-loaded Solid Lipid Nanoparticles (SLNs) (Tobra-SLNs) are able to pass through the lymph to plasma and to evaluate Tobra-SLNs pharmacokinetics
Intravenous administration: Non-stealth and stealth Doxorubicin-loaded SLNs (Doxo-SLNs) were prepared, the latter containing increasing amounts of stealth agent, and were i.v. administered to rabbits in order to compare their pharmacokinetic in comparison with doxorubicin free solution
Summary
Different colloidal drug delivery systems (including liposomes, dendrimers and polymeric nanoparticles, in addition to Solid Lipid Nanoparticles [SLNs]), were developed to overcome physicochemical limitations of potential therapeutical compounds such as poor solubility, low permeability, short half-life, high molecular weight, side effects and systemic toxicity [1, 2]. A physiologic compound normally present in all mammalian organisms, could be regarded as a prototype of an effective in vitro anti-inflammatory and anti-cancer drug whose clinical use is heavily limited by its poor pharmacokinetic profile [3,4,5,6,7,8,9,10,11]. Cholesterylbutyrate SLNs (Chol-but SLNs), recently prepared and tested in vitro, proved to be an effective and suitable prodrug of butyrate [11,12,13,14,15]. The aims of this review are first to describe the characteristics of SLNs prepared from warm microemulsions, subsequently to analyze the biological properties of butyrate as regards to anti-inflammatory and especially anti-neoplastic, to discuss Chol-but SLNs in vitro and in vivo studies and their potential and future applications
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