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.
Highlights
Anticancer drugs are crucial agents in the global approach to fight cancer
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
Dialysis experiments allowed to follow compound diffusion from dipalmitoyl phosphatidylcholine (DPPC)/dipalmitoyl phosphatidylglycerol (DPPG) donor liposomes to NBD-labelled lipid/DPPC/DPPG acceptor liposomes, through dialysis membranes of 6 to 8 KDa and 12 to 14 KDa. These results may be important for future drug delivery applications using nanoliposomes for the encapsulation and transport of this promising antitumoral compound
Summary
Anticancer drugs are crucial agents in the global approach to fight cancer. Drug-loaded nanoparticles provide a perfect solution to afford higher therapeutic efficacy and/or reducing toxicity and the possibility of targeting cancer tissues. Considering its promising utility as an antitumoral drug, compound 1 was encapsulated in different nanoliposome formulations and the mean size, size hexadecanoyl-sn-glycero-3-phosphocholine (NBD-C12HPC) were obtained from Invitrogen (Carlsbad, CA, USA).
Sign-in/Register to view highlights & summary Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
