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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

Schematic dialysis experiment from DPPC/DPPG liposomes to NBD-labelled lipid/DPPC/DPPG liposomes.
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Figure 2: Schematic dialysis experiment from DPPC/DPPG liposomes to NBD-labelled lipid/DPPC/DPPG liposomes.

Mentions: Taking advantage of the possibility of FRET from the excited compound 1 (donor) to the nitrobenzoxadiazole moiety, the diffusion of compound 1 in dialysis experiments was monitored using this photophysical process. Two different dialysis membranes (6 to 8 KDa or 12 to 14 KDa) were tested. The experiments were carried out at 25°C for 36 h and are schematically illustrated in Figure 2. DPPC/DPPG (1:1) liposomes with encapsulated compound 1 (donor liposomes) were placed at one side of the dialysis membrane (Figure 2, left), while NBD-labelled lipid/DPPC/DPPG liposomes without compound (acceptor liposomes) are placed at the other side (Figure 2, right). After the experiment (36 h), the occurrence of energy transfer (FRET) from compound 1 to NBD, detected in the solution located at the right side, is a proof of compound diffusion from the donor liposomes, passing across the dialysis membrane and incorporation in the membrane of the acceptor liposomes. The phospholipids DPPC and DPPG are the main components of biological membranes and are both in the gel phase at room temperature. This fact is expected to restrain the diffusion of compound 1 and, therefore, if the compound diffuses through the dialysis membrane in this situation, this will be even easier with the lipids that are in the fluid phase.


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)

Schematic dialysis experiment from DPPC/DPPG liposomes to NBD-labelled lipid/DPPC/DPPG liposomes.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

Figure 2: Schematic dialysis experiment from DPPC/DPPG liposomes to NBD-labelled lipid/DPPC/DPPG liposomes.
Mentions: Taking advantage of the possibility of FRET from the excited compound 1 (donor) to the nitrobenzoxadiazole moiety, the diffusion of compound 1 in dialysis experiments was monitored using this photophysical process. Two different dialysis membranes (6 to 8 KDa or 12 to 14 KDa) were tested. The experiments were carried out at 25°C for 36 h and are schematically illustrated in Figure 2. DPPC/DPPG (1:1) liposomes with encapsulated compound 1 (donor liposomes) were placed at one side of the dialysis membrane (Figure 2, left), while NBD-labelled lipid/DPPC/DPPG liposomes without compound (acceptor liposomes) are placed at the other side (Figure 2, right). After the experiment (36 h), the occurrence of energy transfer (FRET) from compound 1 to NBD, detected in the solution located at the right side, is a proof of compound diffusion from the donor liposomes, passing across the dialysis membrane and incorporation in the membrane of the acceptor liposomes. The phospholipids DPPC and DPPG are the main components of biological membranes and are both in the gel phase at room temperature. This fact is expected to restrain the diffusion of compound 1 and, therefore, if the compound diffuses through the dialysis membrane in this situation, this will be even easier with the lipids that are in the fluid phase.

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