Cocrystallization in Nutraceuticals
Cocrystal of nutraceuticals alone or in combination with other preventive and/or therapeutic strategies might become effective future drugs against the most common degenerative diseases.
Abstract
light and oxidative enzymes which constitute a serious problem for their bioavailability .This further hamper their formulation and use. At this point their cocrystal can offer an opportunity to overcome all the issues of nutraceuticals and help in the exponential growth of nutraceuticals market.Cocrystal of nutraceuticals alone or in combination with other preventive and/or therapeutic strategies might become effective future drugs against the most common degenerative diseases. Cocrystals are engineered solids based on the concept of different forms having desired properties using hydrogen bonds,pi-pi stacking and van der waals interactions[9] are taken in stoichiometric amounts and ground together using a mortar and pestle, using a ball mill, or using a vibratory mill. Normal grinding time ranges from 30-60 min. It has been reported that cocrystal was first produced by one technique which may be used as seeds to obtain that cocrystal by another method, thus possibly facilitating XRD structure determination via single-crystal growth. In another case, cocrystal structure determination was achieved by preparing only as crystalline powder by grinding [27] Vibrational spectroscopy:-For the characterization of cocrystals molecular motions by use of vibrational spectroscopy are observed. This method includes infrared absorption spectroscopy.Significant changes in the vibrational frequency are observed for the cocrys‐ tals and individual constituents confirming the formation of cocrytals. It can be a very useful technique in differentiaiting cocrystals from salts when a carboxylic acid is involved in hydrogen bonding [37]. It has been reported that in the case of indomethacin and saccharin cocrystals, the O–H stretching of the carboxylic acid group in indomethacin and the N–H stretching of cyclic imide group in saccharin appeared at 3,350.5 and 3,129.1 cm in Indomethacin and saccharin cocrys‐ tals, implied the formation of new phase [38]. It has been reported that the cocrystals of curcumin with resorcinol and pyrogallol were obtained by solvent drop method. Cocrystals of Curcumin–resorcinol and curcumin–pyro‐ gallol were obtained in stoichiometric ratio of 1: 1and were characterized by X-ray diffraction, thermal analysis, FT-IR, FT-Raman, and solid-state 13C NMR spectroscopy. The melting point of the cocrystals was found to be between that of curcumin and the conformer,it has been observed that the lower melting cocrystal was more soluble than higher melting.The dissolu‐ tion studies revealed that the dissolution rates of curcumin–resorcinol and curcumin– pyrogallol in 40% EtOH–water are ~5 and ~12 times faster than that for curcumin [57]. studies. Neutral forms of both compounds cocrystallize in a common P21/c space group of the monoclinic crystal system. Crystal lattice discloses formation of molecular layers, formed by O–H_ _ _O, O–H_ _ _N and C–H_ _ _O-type contacts between genistein and caffeine molecules, while stabilization of the three-dimensional crystal lattice is offered by pi - pi interactions. Dissolution studies showed maximum solubility of the cocrystalline phase in a 50:50 v/v ethanol–water medium, attained 0.861 mg/mL after 8 h, revealing some degree of enhancement as compared to parent genistein, maximum solubility of which was also reached after 8 h and equaled to 0.588 mg/mL [62].