INVESTIGATION OF ANTICANCER ACTIVITY ON CURCUMIN DENDRIMERIC NANOFORMULATION

Curcumin (diferuloylmethane) is a polyphenol derivedfrom the plant Curcuma longa, commonly called turmeric. Extensive research over the last 50 years has indicated this polyphenol can both prevent and treat cancer. The anticancer potential of curcumin stems from its ability to suppress proliferation of a wide variety of tumor cells, down-regulatetranscription factors NF-κB, AP-1 and Egr-1; down-regulate theexpression of COX2, LOX, NOS, MMP-9, uPA, TNF,chemokines, cell surface adhesion molecules and cyclin D1;down-regulate growth factor receptors (such as EGFR andHER2); and inhibit the activity of c-Jun N-terminal kinase,protein tyrosine kinases and protein serine/threonine kinases.

One draw-back holding curcumin back is its insolublility in water and therefore has poor absorption and subsequently poor bioavailability.

Dendrimer, being well defined and highly branched macromolecule, their multifunctionality and specific shape have been recognized as powerful tool in drug delivery. Polyamidation (PAMAM) dendrimers consist of core dendr-termini (i.e. DAB-dendr -(NH2)64) is a diaminobutanecore dendritic poly(propylene mine) having 64 primary amine termini, also named as DAB-dendr -(PA)64, where PA stands for polyamine, and its repeating units and terminal groups potent for interaction of oppositely charged component and produces surfactant like effects by forming a nanoparticles for drug delivery. In the context of drug delivery, the use of fatty acids as permeation enhancer limits the metabolism of drug in liver when administered orally and allowed for plasma binding in blood readily. The application f this study could be sustained for oral delivery and improved absorption through gastrointestinal tract for overall enhancement in therapeutic efficacy.

Based on these reports, the present study is designed to overcome pharmacokinetic drawbacks by conjugating with dendrimer and understanding there physicochemical properties of curcumin/dendrimer/fatty acids complex system and to evaluate its suitability for sustaineddrug release, which is further allowed for oral drug delivery for screening as potent anticancer agents by using in vitro and in vivo model.