Pure Caffeic Acid Research Articles

Phytophospholipid Complex of Caffeic Acid: Development, In vitro Characterization, and In Vivo Investigation of Antihyperlipidemic and Hepatoprotective Action in Rats

Caffeic acid (CA), a hydroxycinnamic acid possessing a variety of pharmacological activities, has caused a growing interest for the treatment of hyperlipidemia and associated conditions. This work endeavored to develop a novel formulation of CA-Phospholipon® 90H complex (CA-PC) using a solvent evaporation method. Scanning electron microscopy (SEM), differential scanning calorimetry (DSC), Fourier transform infrared spectrophotometry (FTIR), and powder X-ray powder diffraction (PXRD) was carried to confirm the formation of CA-PC. The CA-PC was functionally evaluated in terms of solubility, in vitro and ex vivo drug release, and in vivo bioavailability and efficacy studies. SEM, DSC, FTIR, and XRD studies indicated the physical interaction of CA with Phospholipon® 90H to form a complex. Dynamic light scattering (DLS) studies described particle size of 168 ± 3.9nm with a monodisperse distribution (PDI 0.17) and a negative zeta-potential of - 16.6 ± 2.1mV. The phospholipid complex significantly improved (4.2-fold) the solubility of CA. In vitro and ex vivo dissolution studies of the formulated CA-PC revealed a significantly higher release compared with the pure CA. The pharmacokinetic study of CA-PC in rats demonstrated a significant increase (4.79-fold) in oral bioavailability when compared with pure CA as well. Additionally, a significant improvement in serum lipid profile, serum liver biomarker enzyme levels and, restoration of hepatic tissue architecture to normal, in high-fat diet (HFD) induced hyperlipidemic model was obtained upon CA-PC administration when compared with pure CA. These findings indicated that CA-PC would serve as an effective and promising formulation for CA delivery with improved antihyperlipidemic and hepatoprotective activity.Graphical abstract.

Enhancing the UV A1 screening ability of caffeic acid by encapsulation in layered basic zinc hydroxide matrix

An organic UV screening molecule, caffeic acid (CA), has been stabilised in a zinc basic salt (ZBS) matrix upon intercalative reaction into zinc hydroxide nitrate. According to the X-ray diffraction pattern, the basal spacing of the CA-ZBS nanohybrid is determined to be 10.4Å, which is in agreement with a result of cross-section TEM analysis. FT-IR analysis shows that carboxylate groups in organic anions interact coordinately with zinc atoms on inorganic hydroxide sheets. The resultant CA-ZBS nanohybrid exhibits a superior UV screening ability compared to pure CA molecule.

Oxidative stabilization of cold‐pressed sunflower oil using phenolic compounds of the same seeds

AbstractIt is known that sunflower seeds are rich in phenols, constituting approximately 1–3 g per 100 g of seeds. The principal phenol is chlorogenic acid (CGA), followed by caffeic acid (CA) and lower quantities of several other compounds. On the contrary, it is known that phenols are present only in trace amounts in cold‐pressed sunflower seed oils. In this study, the possibility of improving the oxidative stability of cold‐pressed sunflower oil is evaluated using phenolic substances constitutive of seeds. Phenols, extracted from two different dehulled sunflower seed samples, were identified, measured and added to a cold‐pressed sunflower oil and compared with butylated hydroxyanisole (BHA), pure CGA and pure CA. Raw phenolic extract (RPE) was composed of CGA exclusively, whereas CA was present only in traces in its free form was not present. On the contrary, hydrolysable phenol acids (HPAs) were constituted prevalently from CA, released by CGA alkaline hydrolysis. The stabilization effect on oil oxidation at 110 °C was evaluated as 41% and 118% for RPE and HPAs respectively with respect to the control. At 30 °C, no significant differences were recorded between the two seed extracts. Their antioxidant effect was lower than that at 110 °C and evaluated to be, on average 13%. In comparison with BHA, at 30 °C, both seed extracts were more effective than this synthetic phenol; at 110 °C, the antioxidant effect of RPE and BHA was similar, whereas HPA was significantly more effective than BHA. In conclusion, this study demonstrates that the phenols present in sunflower seeds can be considered natural antioxidants suitable for stabilizing the oxidation of cold‐pressed sunflower oil, at both low and high temperatures. Copyright © 2003 Society of Chemical Industry