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

Abreu AS, Castanheira EM, Queiroz MJ, Ferreira PM, Vale-Silva LA, Pinto E - Nanoscale Res Lett (2011)

Bottom Line: 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.

View Article: PubMed Central - HTML - PubMed

Affiliation: Centre of Physics (CFUM), University of Minho, Campus de Gualtar, 4710-057 Braga, Portugal. anabreu@quimica.uminho.pt.

ABSTRACT
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.

No MeSH data available.


Related in: MedlinePlus

Structure of methyl 6-methoxy-3-(4-methoxyphenyl)-1H-indole-2-carboxylate.
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Figure 1: Structure of methyl 6-methoxy-3-(4-methoxyphenyl)-1H-indole-2-carboxylate.

Mentions: In the present study, the antitumoral activity of the fluorescent indole derivative 1, methyl 6-methoxy-3-(4-methoxyphenyl)-1H-indole-2-carboxylate (Figure 1), previously synthesized by us [10], was tested for the in vitro growth of three human tumor cell lines, showing very low GI50 values. Considering its promising utility as an antitumoral drug, compound 1 was encapsulated in different nanoliposome formulations and the mean size, size distribution, zeta potential, and stability were evaluated, keeping in mind future drug delivery applications using this compound as an anticancer drug.


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

Abreu AS, Castanheira EM, Queiroz MJ, Ferreira PM, Vale-Silva LA, Pinto E - Nanoscale Res Lett (2011)

Structure of methyl 6-methoxy-3-(4-methoxyphenyl)-1H-indole-2-carboxylate.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC3211996&req=5

Figure 1: Structure of methyl 6-methoxy-3-(4-methoxyphenyl)-1H-indole-2-carboxylate.
Mentions: In the present study, the antitumoral activity of the fluorescent indole derivative 1, methyl 6-methoxy-3-(4-methoxyphenyl)-1H-indole-2-carboxylate (Figure 1), previously synthesized by us [10], was tested for the in vitro growth of three human tumor cell lines, showing very low GI50 values. Considering its promising utility as an antitumoral drug, compound 1 was encapsulated in different nanoliposome formulations and the mean size, size distribution, zeta potential, and stability were evaluated, keeping in mind future drug delivery applications using this compound as an anticancer drug.

Bottom Line: 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.

View Article: PubMed Central - HTML - PubMed

Affiliation: Centre of Physics (CFUM), University of Minho, Campus de Gualtar, 4710-057 Braga, Portugal. anabreu@quimica.uminho.pt.

ABSTRACT
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.

No MeSH data available.


Related in: MedlinePlus