Publication Type:

Journal Article


Nanotechnology, Volume 21, Number 28 (2010)



Agricultural products, Apoptotic, article, Biochemistry, Biodegradable polymers, Cancer cells, Cancer-targeting, carrier protein, Carrier Proteins, Cell death, Cell Line, cell proliferation, cell shape, Cell Surface, cell surface receptor, Cellular uptake, chemistry, Chemotherapy, Colloidal Stability, Controlled drug delivery, drug effect, flow cytometry, Fluorescence, fluorescence microscopy, folate binding protein, Folate receptor, folate-binding protein, folic acid, Folic acids, Fourier Transform Infrared, Grape seed extract, human, Humans, Hydrogen-Ion Concentration, In-vitro, infrared spectroscopy, kinetics, Lactic acid, metabolism, methodology, microscopy, Molecular receptors, nanoparticle, Nanoparticles, Nanoprecipitation, neoplasm, Neoplasms, Non-targeted, Nutraceuticals, Organic acids, particle size, pH, pH effects, Physiological pH, Phytomedicines, Phytotherapy, Plants (botany), Poly-lactide-co-glycolide, polyglycolic acid, polylactic acid polyglycolic acid copolymer


The concept of 'green' chemotherapy by employing targeted nanoparticle mediated delivery to enhance the efficacy of phytomedicines is reported. Poly (lactide-co-glycolide) (PLGA) nanoparticles encapsulating a well known nutraceutical namely, grape seed extract (GSE) - 'NanoGSE' - was prepared by a nanoprecipitation technique. The drug-loaded nanoparticles of size ∼ 100nm exhibited high colloidal stability at physiological pH. Molecular receptor targeting of this nanophytomedicine against folate receptor over-expressing cancers was demonstrated invitro by conjugation with a potential cancer targeting ligand, folic acid (FA). Fluorescence microscopy and flow cytometry data showed highly specific cellular uptake of FA conjugated NanoGSE on folate receptor positive cancer cells. Studies were also conducted to investigate the efficiency of targeted (FA conjugated) versus non-targeted (non-FA conjugated) nanoformulations in causing cancer cell death. The IC50 values were lowered by a factor of ∼ 3for FA-NanoGSE compared to the free drug, indicating substantially enhanced bioavailability to the tumor cells, sparing the normal ones. Receptor targeting of FA-NanoGSE resulted in a significant increase in apoptotic index, which was also quantified by flow cytometry and fluorescence microscopy. This invitro study provides a basis for the use of nanoparticle mediated delivery of anticancer nutraceuticals to enhance bioavailability and effectively target cancer by a 'green' approach. © 2010 IOP Publishing Ltd.


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Cite this Research Publication

S. Narayanan, Binulal, N. S., Dr. Ullas Mony, Manzoor, K., Nair, S., and Menon, D., “Folate Targeted Polymeric 'green' Nanotherapy for Cancer”, Nanotechnology, vol. 21, 2010.