The therapeutic qualities of the Curcumin compound have been extendedly reported, showing anticancer, antioxidant and anti-inflammatory properties, among others. Nevertheless, dietary curcumin shows poor bioavailability due to its rapid metabolism. However, this obstacle can be overcome in many ways, one is to modify its molecular structure to create a more suitable compound that presents a longer availability within the organism in order to exert its therapeutic action. We have previously reported the cytotoxicity against prostatic and colon cancer cells, and normal peripheral blood mononuclear cells (PBMCs) of Curcumin analogues. Of these, compound (2E,6E)-2,6-bis(3-nitrobenzylidene)cyclohexanone was selected as a good candidate for future development due to its high cytotoxicity against cancer cell lines and relative low toxicity against PBMCs isolated from healthy volunteers, making this analog an excellent candidate for cancer treatment. The purpose of this new research project is to create a suitable drug delivery system to enhance the specific targeting and cytotoxicity of this drug towards cancer cells by achieving a prolonged release of the compound. To this extent, we decided to encapsulate this analog in Poly Lacto-co-Glycolic Acid (PLGA)-based nanoparticles (NPs). This kind of carrier has been reported to be easily absorbed by cells via endocytosis. PLGA-NPs have low toxicity provided by its biodegradable capabilities, degrading into lactic and glycolic acids in the organism, both metabolites of the Krebs' cycle. The formulation of these nanocarriers is achieved by a single emulsion method, and centrifuged to separate the NPs from the medium. The product and the supernatant will be analyzed to determine drug loading and entrapment, morphology and size of the NPs, zeta potential, drug release, and therapeutic potential. We expect that the cytotoxicity against prostatic and colon cancer cell lines of encapsulated drug to be higher than previous tests due to prolonged release of the compound in the cytosol.

Encapsulation of (2E,6E)-2,6-bis(3-nitrobenzylidene)cyclohexanone in PLGA-based nanoparticles

247th National Meeting (2014)

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