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Type: Artigo de periódico
Title: Targeted Antitumoral Dehydrocrotonin Nanoparticles With L-ascorbic Acid 6-stearate.
Author: Frungillo, Lucas
Martins, Dorival
Teixeira, Sérgio
Anazetti, Maristela Conti
Melo, Patrícia da Silva
Durán, Nelson
Abstract: Tumoral 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.
Subject: Antineoplastic Agents, Phytogenic
Ascorbic Acid
Cell Line, Tumor
Chromatography, Thin Layer
Coloring Agents
Diterpenes, Clerodane
Drug Delivery Systems
Flow Cytometry
Hl-60 Cells
Particle Size
Spectrophotometry, Ultraviolet
Tetrazolium Salts
Trypan Blue
Citation: Journal Of Pharmaceutical Sciences. v. 98, n. 12, p. 4796-807, 2009-Dec.
Rights: fechado
Identifier DOI: 10.1002/jps.21760
Date Issue: 2009
Appears in Collections:Unicamp - Artigos e Outros Documentos

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