Cholesteryl butyrate in solid lipid nanospheres as an alternative approach for butyric acid delivery.

Abstract

BACKGROUND:

Cholesteryl-butyrate chosen as lipid matrix of solid lipid nanospheres (SLNs) could be a suitable pro-drug to deliver butyric acid and overcome one of the most limiting disadvantages of the compound: the short half-life due to a rapid metabolism.

METHODS:

We evaluated the antiproliferative effect, with respect to that of sodium butyrate, of four SLNs (SLN1, SLN2, SLN3 and SLN4) characterized by a different concentration of cholesteryl-butyrate (range, 1.7-30 mM) on NIH-H460, a non-small cell lung carcinoma cell line.

RESULTS:

After 6 days of treatment, all SLN preparations induced a dose-dependent inhibition of NHI-H460 cell growth: the most effective SLN preparation (SLN1) was able to induce a complete growth inhibition already at 0.25 mM, a concentration at which sodium butyrate induced only a 55% inhibition. Fluorescence microscopy showed that 6-coumarin-tagged SLNs were almost completely internalized by cells after 5 min of treatment.

CONCLUSIONS:

The present results indicate that owing to their peculiar characteristics, SLNs could be an interesting alternative approach for butyric acid delivery into tumor cells.

• Authors: C Pellizzaro, D Coradini, S Morel, E Ugazio, M R Gasco, M G Daidone
• Journal: Anticancer research (Anticancer Res) 1999 Sep-Oct Vol. 19 Issue 5B Pg. 3921-5 ISSN: 0250-7005 [Print] Greece
• PMID: 10628332 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Butyrates
• Drug Carriers
• Lipids
• Phosphatidylcholines
• Butyric Acid
• Cholesterol

Topics

• Butyrates (pharmacokinetics)
• Butyric Acid (pharmacokinetics)
• Carcinoma, Non-Small-Cell Lung (metabolism)
• Cell Division (drug effects)
• Cholesterol (pharmacokinetics)
• Dose-Response Relationship, Drug
• Drug Carriers (chemistry, pharmacokinetics)
• Humans
• Lipids (chemistry, pharmacokinetics)
• Lung Neoplasms (metabolism)
• Microscopy, Electron
• Microscopy, Fluorescence
• Phosphatidylcholines (pharmacokinetics)
• Tumor Cells, Cultured