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Small R&D Italian company has developed formulations of Solid Lipid Nanoparticles (SLN) to deliver Butyrate ( US6685960).

The company is looking for partners for project development (licensing or cooperation).

Therapeutic target currently under investigation is Brain Tumor as SLN can overcome Blood Brain Barrier (US6419949 - US6238694).

The company has also studied formulation with Doxorubicin and with Paclitaxel, to be developed per se or by exploiting synergetic effect showed when administered with Butyrate SLN.

Cholesteryl butyrate solid lipid nanoparticles (chol-but SLN) have been proposed as a pro-drug to deliver butyric acid. We compared the effects on cell growth, cell-cycle distribution and c-myc expression of chol-but SLN and sodium butyrate (Na-but) in the human leukemic cell lines Jurkat, U937 and HL-60.

In all the cell lines 0.5 and 1.0 mM chol-but SLN provoked a complete block of cell growth. Cell-cycle analysis demonstrated in Jurkat cells that 0.25 mM chol-but SLN caused a pronounced increase of G2/M cells and a decrease of G0/G1 cells, whereas in U937 and HL-60 cells chol-but SLN led to a dose-dependent increase of G0/G1 cells, with a decrease of G2/M cells. In Jurkat and HL-60 cells 0.5 mM chol-but SLN induced a significant increase of sub-G0/G1 apoptotic cells.

Cell growth and cell-cycle distribution were unaffected by the same concentrations of Na-but. A concentration of 0.25 mM chol-but SLN was able to cause a rapid and transient down-regulation of c-myc expression in all the cell lines, whereas 1 mM Na-but caused a slight reduction of c-myc expression only in U937 cells. The results show how chol-but SLN affects the proliferation pattern of both myeloid and lymphoid cells to an extent greater than the natural butyrate (Abstract - Anticancer Drugs. 2004 Jun;15(5):525-36)    

Reference bibliography (Linked to paper when underlined)

• Pellizzaro C.. et Al. - Cholesteryl butyrate in solid lipid nanospheres as an alternative approach for butyric acid delivery - Anticancer Research. 19, 3921-3926 (1999)
• Salomone B. et Al. - In vitro effects of cholesteryl butyrate solid lipid nanospheres as a butyric acid pro-drug on melanoma cells: evaluation of antiproliferative activity and apoptosis induction - Clin.Exper.Metastasis 18, 663-673 (2001)
• Ugazio E. et Al. - The effect  of formulation and concentration of cholesteryl butyrate solid lipid nanospheres (SLN) on NIH-H460 cell proliferation - Eur. J. Pharm. Biopharm.  52 , 197-202(2001)
• Guido M. et Al. - Growth inhibition of glioma cell lines by cholesteryl butyrate in solid lipid nanospheres - Clin. Neuropathol. 19, 151 (2000)
• Serpe L. et Al. - Cholesteril butyrate solid lipid nanoparticles as a butyric acid pro-drug: effects on cell proliferation, cell-cycle distribution and c-myc expression in human leukemic cells - Anti-cancer Drugs. 15(5), 525-36 (2004)
• Serpe L. et Al. - Cytotoxicity of anticancer drugs incorporated in solid lipid nanoparticles on HT-29 colorectal cancer cell line - Eur. J. Pharm. Biopharm, 58, 673-680, (2004)
• Zara G.P. et Al. - Pharmacokinetics and tissue distribution of Idarubicin-loaded Solid Lipid Nanoparticles after duodenal administration to rats.  J. Pharm. Sci. 91, 1024-1033 (2002)
• Zara GP et Al. - Parmacokinetics of doxorubicin incorporated in solid lipid nanospheres (SLN) - Pharmacol Res. 40(3), 281-6 (1999)
• Cavalli R. et Al. - Preparation and characterization of solid lipid nanospheres containing paclitaxel - Eur.J.Pharm.Sci. 10,305-309 (2000)
• Podio V. et Al. - Biodistribution of Stealth and non-stealth solid lipid nanoparticles - J.Pharm.Pharmacol. 52,1057-1063 (2000)
• Fundarò A. et Al. - Stealth and non-stealth solid Lipid Nanoparticles (SLN) carrying doxorubicin: Pharmacokinetics and tissue distribution after IV administration to rats - Pharmacolol. Res. 42, 337-343 (2000)
• Zara G.P. et Al. -  Intravenous administration to rabbits of non-stealth and stealth doxorubicin loaded solid lipid nanoparticles at increasing concentrations of stealth agent: pharmacokinetics and distribution of doxorubicin in brain and in other tissues - J. Drug Targeting 10, 327-335 (2002)

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