Targeted Antitumoral Dehydrocrotonin Nanoparticles With L-ascorbic Acid 6-stearate.

dc.creatorFrungillo, Lucas
dc.creatorMartins, Dorival
dc.creatorTeixeira, Sérgio
dc.creatorAnazetti, Maristela Conti
dc.creatorMelo, Patrícia da Silva
dc.creatorDurán, Nelson
dc.date2009-Dec
dc.date2015-11-27T13:15:05Z
dc.date2015-11-27T13:15:05Z
dc.date.accessioned2018-03-29T01:08:37Z
dc.date.available2018-03-29T01:08:37Z
dc.identifierJournal Of Pharmaceutical Sciences. v. 98, n. 12, p. 4796-807, 2009-Dec.
dc.identifier1520-6017
dc.identifier10.1002/jps.21760
dc.identifierhttp://www.ncbi.nlm.nih.gov/pubmed/19367621
dc.identifierhttp://repositorio.unicamp.br/jspui/handle/REPOSIP/198262
dc.identifier19367621
dc.identifier.urihttp://repositorioslatinoamericanos.uchile.cl/handle/2250/1298495
dc.descriptionTumoral cells are known to have a higher ascorbic acid uptake than normal cells. Therefore, the aim of this study was to obtain polymeric nanoparticles containing the antitumoral compound trans-dehydrocrotonin (DHC) functionalized with L-ascorbic acid 6-stearate (AAS) to specifically target this system tumoral cells. Nanoparticle suspensions (NP-AAS-DHC) were prepared by the nanoprecipitation method. The systems were characterized for AAS presence by thin-layer chromatography and for drug loading (81-88%) by UV-Vis spectroscopy. To further characterize these systems, in vitro release kinetics, size distribution (100-140 nm) and Zeta potential by photon-correlation spectroscopic method were used. In vitro toxicity against HL60 cells was evaluated by tetrazolium reduction and Trypan blue exclusion assays. Cell death by apoptosis was quantified and characterized by flow cytometry and caspase activity. Zeta potential analyses showed that the system has a negatively charged outer surface and also indicate that AAS is incorporated on the external surface of the nanoparticles. In vitro release kinetics assay showed that DHC loaded in nanoparticles had sustained release behavior. In vitro toxicity assays showed that NP-AAS-DHC suspension was more effective as an antitumoral than free DHC or NP-DHC and increased apoptosis induction by receptor-mediated pathway.
dc.description98
dc.description4796-807
dc.languageeng
dc.relationJournal Of Pharmaceutical Sciences
dc.relationJ Pharm Sci
dc.rightsfechado
dc.rights2009 Wiley-Liss, Inc. and the American Pharmacists Association
dc.sourcePubMed
dc.subjectAntineoplastic Agents, Phytogenic
dc.subjectApoptosis
dc.subjectAscorbic Acid
dc.subjectCaspases
dc.subjectCell Line, Tumor
dc.subjectChromatography, Thin Layer
dc.subjectColoring Agents
dc.subjectDiterpenes, Clerodane
dc.subjectDrug Delivery Systems
dc.subjectElectrochemistry
dc.subjectExcipients
dc.subjectFlow Cytometry
dc.subjectHl-60 Cells
dc.subjectHumans
dc.subjectKinetics
dc.subjectNanoparticles
dc.subjectParticle Size
dc.subjectSpectrophotometry, Ultraviolet
dc.subjectSuspensions
dc.subjectTetrazolium Salts
dc.subjectThiazoles
dc.subjectTrypan Blue
dc.titleTargeted Antitumoral Dehydrocrotonin Nanoparticles With L-ascorbic Acid 6-stearate.
dc.typeArtículos de revistas


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