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Abstract
Curcumin, the natural anticancer drug and its optimum potential is limited due to
lack of solubility in aqueous solvent, degradation at alkaline pH and poor tissue
absorption. In order to enhance its potency and improve bioavailability, we have synthesized
curcumin loaded nanoparticulate delivery system. Unlike free curcumin, it is readily
dispersed in aqueous medium, showing narrow size distribution 192 nm ranges (as observed
by microscope) with biocompatibility (confocal studies and TNF-alpha assay). Furthermore,
it displayed enhanced stability in phosphate buffer saline by protecting encapsulated
curcumin against hydrolysis and biotransformation. Most importantly, nanoparticulate
curcumin was comparatively more effective than native curcumin against different cancer
cell lines under in vitro condition with time due to enhanced cellular uptake resulting
in reduction of cell viability by inducing apoptosis. Molecular basis of apoptosis
studied by western blotting revealed blockade of nuclear factor kappa B (NFkappaB)
and its regulated gene expression through inhibition of IkappaB kinase and Akt activation.
In mice, nanoparticulate curcumin was more bioavailable and had a longer half-life
than native curcumin as revealed from pharmacokinetics study. Thus, the results demonstrated
nanoparticulate curcumin may be useful as a potential anticancer drug for treatment
of various malignant tumors.
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