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

Cinzia Pellizzaro, Danila Coradini, Silvia Morel, Elena Ugazio, Maria Rosa Gasco, Maria Grazia Daidone

Research output: Contribution to journalArticlepeer-review

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.

Original languageEnglish
Pages (from-to)3921-3925
Number of pages5
JournalAnticancer Research
Volume19
Issue number5 B
Publication statusPublished - 1999

Keywords

  • Butyrate
  • Cholesteryl-butyrate
  • Drug delivery
  • Lung tumor cells
  • Solid lipid nanospheres

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