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| 1 | Solid lipid nanoparticles delivering anti-inflammatory drugs to treat inflammatory bowel disease: Effects in an in vivo model显示文摘AIM To improve anti-inflammatory activity while reducing drug doses, we developed a nanoformulation carrying dexamethasone and butyrate.METHODS Dexamethasone cholesteryl butyrate-solid lipid nanoparticles(Dx Cb-SLN) were obtained with the warm microemulsion method. The anti-inflammatory activity of this novel nanoformulation has been investigated in vitro(cell adhesion to human vascular endothelial cells and pro-inflammatory cytokine release by lipopolysaccharideinduced polymorphonuclear cells) and in vivo(disease activity index and cytokine plasma concentrations in a dextran sulfate sodium-induced mouse colitis) models. Each drug was also administered separately to compare its effects with those induced by their co-administration in SLN at the same concentrations.RESULTS Dx Cb-SLN at the lowest concentration tested(Dx 2.5 nmol/L and Cb 0.1 μmol/L) were able to exert a more than additive effect compared to the sum of the individual effects of each drug, inducing a significant in vitro inhibition of cell adhesion and a significant decrease of pro-inflammatory cytokine(IL-1β and TNF-α) in both in vitro and in vivo models. Notably, only the Dx Cb nanoformulation administration was able to achieve a significant cytokine decrease compared to the cytokine plasma concentration of the untreated mice with dextran sulfate sodium-induced colitis. Specifically, Dx Cb-SLN induced a IL-1β plasma concentration of 61.77% ± 3.19%, whereas Dx or Cb used separately induced a concentration of 90.0% ± 2.8% and 91.40% ± 7.5%, respectively; Dx Cb-SLN induced a TNF-α plasma concentration of 30.8% ± 8.9%, whereas Dx or Cb used separately induced ones of 99.5% ± 4.9% and 71.1% ± 10.9%, respectively.CONCLUSION Our results indicate that the co-administration of dexamethasone and butyrate by nanoparticles may be beneficial for inflammatory bowel disease treatment. | Chiara Dianzani Federica Foglietta Benedetta Ferrara Arianna Carolina Rosa Elisabetta Muntoni Paolo Gasco Carlo Della Pepa Roberto Canaparo Loredana Serpe | 2017 | World Journal of Gastroenterology2017，23，23： | 3 |
| 2 | Determination of ibuprofen in human plasma by high-performance liquid chromatography:validation and application in pharmacokinetic study显示文摘 | Canaparo R Muntoni E Zara GP | | 0，，04： | 1 |
| 3 | Intracellular accumulation and eytotoxicity of doxorubicin with different pharmaceutical formulations in human cancer cell lines 显示文摘 | Serpe L Guido M Canaparo R | 2006 | J Nanosci Nanotechnol2006，6，910： | 1 |
| 4 | Analysis of CYP2C9*5 in Caucasian, Oriental and black-African populations显示文摘 | Yasar U Aklillu E Canaparo R | 2002 | Eur J Clin Pharmacol2002，58，8： | 1 |
| 5 | Prospective study of the effects of concomitant medications on thiopu- rine metabolism in inflammatory bowel disease显示文摘 | Dapemo M Sostegni R Canaparo R | 2009 | Ali- ment Pharmacol Ther2009，30，8： | 1 |
| 6 | Expression of cytochromes P450 3A and P-glycoprotein in human large intestine in paired tumor and normal samples显示文摘 | Canaparo R Nordmark A Finnstorm N | 2007 | Basic Clin Pharmacol Toxicol2007，100，4： | 1 |
| 7 | Determination of Ibuprofen in Human Plasma by High-Performance Liquid Chromatography: Validation and Application in Pharmacokinetic Study 显示文摘 | Canaparo R Muntoni E Zara G | 2000 | Biomedical Chromatography2000，14，4： | 1 |
| 8 | Innovative formulations for the controlled and site-specific delivery of antiinflammatory drugs显示文摘 | Serpe L Canaparo R Foglietta F | 2013 | CurrPharmDes2013，19，41： | 1 |
| 9 | Expression of CYP3A isoforms and P-glycoprotein in human stomach,jejunum and ileum显示文摘 | Canaparo R Finnstrm N Serpe L | 2007 | Clin Exp Pharmacol Physiol2007，34，11： | 1 |
| 10 | Polymeric nanop- articles enhance the sonodynamic activity of meso-tetrakis (4-sulfonatophenyl) porphyrin in an in vitro neuroblasto- ma model 显示文摘 | Serpe L Canaparo R Varchi G | 2013 | International Journal of Nanomedicine2013，8，： | 1 |
| 11 | Expression of CYP3A isoforms and P-glycoprotein in human stomach,jejunum and ileum显示文摘 | Canaparo R Finnstrom N Serpe L | 2007 | Clin Exp Pharmacol Physiol2007，34，11： | 1 |
| 12 | Dexibuprofen (S +-isomer ibuprofen)reduces gastric damage and improves analgesic and antiinflammatory effects in rodents显示文摘 | BONABELLO A GALMOZZI MR CANAPARO R | 2003 | Anesth Analg2003，97，2： | 1 |
| 13 | Thiopurine S -methyltransferase pharmacogenetics in a large-scale healthy Italian–Caucasian population: differences in enzyme activity显示文摘 | Loredana Serpe Pier Luigi Calvo Elisabetta Muntoni Sergio D&rsquor Antico Mario Giaccone Alessandra Avagnina Maurizio Baldi Cristiana Barbera Franco Curti Angelo Pera Mario Eandi Gian Paolo Zara Roberto Canaparo | 2009 | Pharmacogenomics2009，，11： | 1 |
| 14 | Simultaneous HPLC determination of 5-fluorouraeil and its metabolites in plasma of cancer patients显示文摘 | Casale F Canaparo R Muntoni E | 2002 | Biomed Chromatogr2002，16，7： | 1 |
| 15 | Modulation of butyrate anticancer activity by solid lipid nanoparticle delivery:an in vitro investigation on human breast cancer and leukemia cell lines显示文摘 | Foglietta F Serpe L Canaparo R | 2014 | J Pharm Sci2014，17，2： | 1 |
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