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Nanoliposomes for encapsulation and delivery of the potential antitumoral methyl 6-methoxy-3-(4-methoxyphenyl)-1H-indole-2-carboxylate

Ana S Abreu12*, Elisabete MS Castanheira1, Maria-João RP Queiroz2, Paula MT Ferreira2, Luís A Vale-Silva3 and Eugénia Pinto3

Author Affiliations

1 Centre of Physics (CFUM), University of Minho, Campus de Gualtar, 4710-057 Braga, Portugal

2 Centre of Chemistry (CQ/UM), University of Minho, Campus de Gualtar, 4710-057 Braga, Portugal

3 Laboratory of Microbiology, Faculty of Pharmacy and Centre of Medicinal Chemistry (CEQUIMED), University of Porto, Rua Aníbal Cunha 164, 4050-047 Porto, Portugal

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Nanoscale Research Letters 2011, 6:482  doi:10.1186/1556-276X-6-482

Published: 3 August 2011


A potential antitumoral fluorescent indole derivative, methyl 6-methoxy-3-(4-methoxyphenyl)-1H-indole-2-carboxylate, was evaluated for the in vitro cell growth inhibition on three human tumor cell lines, MCF-7 (breast adenocarcinoma), A375-C5 (melanoma), and NCI-H460 (non-small cell lung cancer), after a continuous exposure of 48 h, exhibiting very low GI50 values for all the cell lines tested (0.25 to 0.33 μM). This compound was encapsulated in different nanosized liposome formulations, containing egg lecithin (Egg-PC), dipalmitoyl phosphatidylcholine (DPPC), dipalmitoyl phosphatidylglycerol (DPPG), DSPC, cholesterol, dihexadecyl phosphate, and DSPE-PEG. Dynamic light scattering measurements showed that nanoliposomes with the encapsulated compound are generally monodisperse and with hydrodynamic diameters lower than 120 nm, good stability and zeta potential values lower than -18 mV. Dialysis experiments allowed to monitor compound diffusion through the lipid membrane, from DPPC/DPPG donor liposomes to NBD-labelled lipid/DPPC/DPPG acceptor liposomes.