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Curcumin: From Extraction to Therapeutic Agent

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Curcumin: From Extraction to Therapeutic Agent ( curcumin-from-extraction-therapeutic-agent )

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Molecules 2014, 19 20102 increase in the anticancer activity due to improved bioavailability of curcumin was reported. Liposomal curcumin was found to be the best for improving the bioavailability of curcumin in cells [96] and products based on liposomal formulations are being marketed for different dietary applications of curcumin. Till recently the word nanocurucmin referred to curcumin-loaded organic formulations only. Since there are already several reviews published on organic nanoformulations, in this review, application of inorganic nano formulations in curcumin delivery is discussed. With the same aim of improving anti-cancer activity of curcumin, in the last few years, researchers have been preparing formulations in which curcumin is bound to novel metal and oxide nanoparticles. Such systems can be easily manipulated for improved delivery, activity and specificity. Mesoporous silica nanoparticles (MSN) are one of the most employed nanosystems for improving the bioavailability of poorly water soluble drugs [99–107]. Due to their ordered nanoporous structures, high surface areas, large pore volumes and high surface densities of hydroxyl groups, MSNs can be functionalized easily. They are biocompatible and they are commonly used in many biomedical applications. Curcumin binds covalently through a silicon-oxygen bond at the diketo moiety (Figure 2). Curcumin-loaded MSNs have been prepared and employed in several studies [99–107]. In these systems, curcumin release could be controlled for even up to several hours along with improvement in the stability and bioavailability of curcumin. Figure 2. Curcumin-bound mesoporous silicon nanoparticles. OH HO H3CO OCH3 H3CO O O- O- O O OOH HO OCH3 OOOO O OCH3 OH -O Si O Si O Si O Si OOOO O- OCH 3 -O Si O Si O Si O Si HO O - - O- OCH3 OH The fluorescence of curcumin is enhanced on MSN conjugation and therefore has the potential to be employed for imaging biomolecules/organelles. Novel cyclodextrin functionalized MSN have been found to be photothermally controlled on exposure to light to release curcumin on demand in zebrafish larve [102]. Large amount of curcumin could be loaded in to spherical microcapsules containing L-lysine, trisodiumcitrate and silica sol (colloidal suspension). These microcapsules could be triggered to release curcumin by adjusting the pH to acidic conditions [103,104]. MSN-curcumin conjugates, increased the cytotoxicity of curcumin in Hela cell lines and also in normal fibroblast cell lines [105]. They also increased photocytotoxicity of curcumin in human oral cancer cells, on exposure to light [106]. Other formulations like guanidine functionalized, and PEGylated MSN-curcumin conjugates showed improved bioavailability and controlled release of curcumin in vitro systems [107]. H3CO HO

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