Affordable Access

deepdyve-link
Publisher Website

Targeted antitumoral dehydrocrotonin nanoparticles with L-ascorbic acid 6-stearate.

Authors
  • Frungillo, Lucas
  • Martins, Dorival
  • Teixeira, Sérgio
  • Anazetti, Maristela Conti
  • Melo, Patrícia da Silva
  • Durán, Nelson
Type
Published Article
Journal
Journal of Pharmaceutical Sciences
Publisher
Elsevier
Publication Date
Dec 01, 2009
Volume
98
Issue
12
Pages
4796–4807
Identifiers
DOI: 10.1002/jps.21760
PMID: 19367621
Source
Medline
License
Unknown

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.

Report this publication

Statistics

Seen <100 times