Evaluation of Effect of Ligand on Cellular Internalization: A Comparative Study of Nanoparticles and Multifunctional Nanoparticles on MDA-MB-231 Cells
Sanjay K. Jain.
The present work was aimed to develop, explore & compare the use of multifuctional nanoparticles (MNPs) (drug loaded) made
of the conjugate poly (lactide-co-glycolide) (PLGA) - polyethylene glycol (PEG) & – folic acid with PLGA nanoparticles (NPs) (drug
loaded) for targeting solid tumor. For that first optimum cytotoxic concentration of PLGA (polymer) and cisplatin (drug) were optimized
through MTT assay. The optimum size and percent entrapment efficiency were found to be 170±6.5 nm and 74.9±2.3% for PLGA NPs
and 186±4.2 nm and 76.9±3.1% for MNPs. The in vitro cytotoxic activity of MNPs and PLGA NPs were investigated & compared with
drug solution (cisplatin) on MDA-MB-231 breast cancer cells, which revealed that MNPs are more cytotoxic in a time dependent manner.
The rhodamine B isothiocyanate loaded NPs and MNPs were prepared & compared for cell uptake studies which conformed that targeted
NPs (MNPs) were more taken up by the MDA-MB-231 cells. To determine the effect of ligand (folic acid) on internalization, cells
were incubated with MNPs, NPs and 10 fold excess folic acid with MNPs. Results confirmed that the presence of ligand gradually increases
internalization of carriers and exhibited maximum uptake of MNPs whereas, little difference was observed on uptake between
NPs and excess folate treated cells. Results suggesting that MNPs are promising approach for targeting solid tumor & to achieve deeper
Keywords: PLGA poly (lactide-co-glycolide), nanoparticles, multifunctional nanoparticles, cytotoxicity, cell uptake, solid tumor, cisplatin
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