Evaluation of Effect of Ligand on Cellular Internalization: A Comparative Study of Nanoparticles and Multifunctional Nanoparticles on MDA-MB-231 Cells

Author(s): Anand Mahalwar, Arvind Gulbake, Ashish Jain, Satish Shilpi, Bhawna Sharma, Beenu Joshi, Sanjay K. Jain

Journal Name: Current Nanoscience

Volume 8 , Issue 3 , 2012

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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 cellular internalization.

Keywords: PLGA poly (lactide-co-glycolide), nanoparticles, multifunctional nanoparticles, cytotoxicity, cell uptake, solid tumor, cisplatin

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Article Details

Year: 2012
Published on: 10 May, 2012
Page: [432 - 440]
Pages: 9
DOI: 10.2174/157341312800620197
Price: $65

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