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.
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: B Salomone; R Ponti; M R Gasco; E Ugazio; P Quaglino; S Osella-Abate; M G Bernengo Journal: Clin Exp Metastasis Date: 2000 Impact factor: 5.150
Authors: R Minelli; L Serpe; P Pettazzoni; V Minero; G Barrera; Cl Gigliotti; R Mesturini; A C Rosa; P Gasco; N Vivenza; E Muntoni; R Fantozzi; U Dianzani; G P Zara; C Dianzani Journal: Br J Pharmacol Date: 2012-05 Impact factor: 8.739
Authors: R Minelli; S Occhipinti; C L Gigliotti; G Barrera; P Gasco; L Conti; A Chiocchetti; G P Zara; R Fantozzi; M Giovarelli; U Dianzani; C Dianzani Journal: Br J Pharmacol Date: 2013-09 Impact factor: 8.739