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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

Fluorescence spectra of compound 1 in DPPC/DPPG liposomes and NBD-PE labelled DPPC/DPPG liposomes before and after dialysis.
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Figure 3: Fluorescence spectra of compound 1 in DPPC/DPPG liposomes and NBD-PE labelled DPPC/DPPG liposomes before and after dialysis.

Mentions: The NBD-labelled lipids were either labelled at head group (NBD-PE), at position 6 of the fatty acid chain (NBD-C6-HPC) or at position 12 of the fatty acid chain (NBD-C12-HPC). Figure 3 displays (as examples) the emission spectra of compound 1 in DPPC/DPPG donor liposomes and of the NBD-PE/DPPC/DPPG acceptor nanoliposomes, before (t = 0 s) and after (t = 36 h) diffusion of compound 1 through the two dialysis membranes used in the study. After the dialysis assay, the fluorescence of compound 1 in the donor liposomes is notably reduced (Figure 3), and its emission can be detected in the acceptor liposomes solution, showing the diffusion of compound 1 through the dialysis membrane. Besides, due to the energy transfer from compound 1 to NBD, the fluorescence intensity of the latter notably increases (Figure 3). The effect is stronger for the membrane of 12 to 14 KDa.


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)

Fluorescence spectra of compound 1 in DPPC/DPPG liposomes and NBD-PE labelled DPPC/DPPG liposomes before and after dialysis.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

Figure 3: Fluorescence spectra of compound 1 in DPPC/DPPG liposomes and NBD-PE labelled DPPC/DPPG liposomes before and after dialysis.
Mentions: The NBD-labelled lipids were either labelled at head group (NBD-PE), at position 6 of the fatty acid chain (NBD-C6-HPC) or at position 12 of the fatty acid chain (NBD-C12-HPC). Figure 3 displays (as examples) the emission spectra of compound 1 in DPPC/DPPG donor liposomes and of the NBD-PE/DPPC/DPPG acceptor nanoliposomes, before (t = 0 s) and after (t = 36 h) diffusion of compound 1 through the two dialysis membranes used in the study. After the dialysis assay, the fluorescence of compound 1 in the donor liposomes is notably reduced (Figure 3), and its emission can be detected in the acceptor liposomes solution, showing the diffusion of compound 1 through the dialysis membrane. Besides, due to the energy transfer from compound 1 to NBD, the fluorescence intensity of the latter notably increases (Figure 3). The effect is stronger for the membrane of 12 to 14 KDa.

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