1. Cholesteryl butyrate in solid lipid nanospheres as an alternative approach for butyric acid delivery.
- Author
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Pellizzaro C, Coradini D, Morel S, Ugazio E, Gasco MR, and Daidone MG
- Subjects
- Carcinoma, Non-Small-Cell Lung metabolism, Cell Division drug effects, Dose-Response Relationship, Drug, Humans, Lipids chemistry, Lung Neoplasms metabolism, Microscopy, Electron, Microscopy, Fluorescence, Phosphatidylcholines pharmacokinetics, Tumor Cells, Cultured, Butyrates pharmacokinetics, Butyric Acid pharmacokinetics, Cholesterol pharmacokinetics, Drug Carriers chemistry, Drug Carriers pharmacokinetics, Lipids pharmacokinetics
- 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.
- Published
- 1999