Increased Solubility, Dissolution and Physicochemical Studies of Curcumin- Polyvinylpyrrolidone K-30 Solid Dispersions

Authors: Nattha Kaewnopparat, Sanae Kaewnopparat, Amaravadee Jangwang, Daungkhae Maneenaun, Thitima Chuchome, Pharkphoom Panichayupakaranant

Abstract:

Solid dispersions (SD) of curcuminpolyvinylpyrrolidone in the ratio of 1:2, 1:4, 1:5, 1:6, and 1:8 were prepared in an attempt to increase the solubility and dissolution. Solubility, dissolution, powder X-ray diffraction (XRD), differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR) of solid dispersions, physical mixtures (PM) and curcumin were evaluated. Both solubility and dissolution of curcumin solid dispersions were significantly greater than those observed for physical mixtures and intact curcumin. The powder X-ray diffractograms indicated that the amorphous curcumin was obtained from all solid dispersions. It was found that the optimum weight ratio for curcumin:PVP K-30 is 1:6. The 1:6 solid dispersion still in the amorphous from after storage at ambient temperature for 2 years and the dissolution profile did not significantly different from freshly prepared.

Keywords: Curcumin, polyvinylpyrrolidone K-30, solid dispersion, dissolution, physicochemical.

Digital Object Identifier (DOI): doi.org/10.5281/zenodo.1331031

References:

[1] H.P.T. Ammon, and M.A. Wahl, "Pharmacology of curcumin," Planta. Med., vol. 57, pp. 1-7, 1991.
[2] V. Ravindranath, and N. Chandrasekhara, "Absorption and tissue distribution of curcumin in rats," Toxicology, vol. 16(3), pp. 259-265, 1980.
[3] S. Okonogi, T. Oguchi, E. Yonemochi, S. Puttipipatkhachorn and K. Yamamoto, "Improved dissolution of ofloxacin via solid dispersion," Int. J. Pharm., vol. 156, pp.175-180, 1997.
[4] M. Franco, G. Trapani, A. Latrofa, C. Tullio, M.R. Provenzano, M. Serra, M. Muggironi, et al., "Dissolution properties and anticonvulsant activity of phenytoin-polyethylene glycol 6000 and polyvinylpyrrolidone K-30 solid dispersions," Int. J. Pharm., vol. 225, pp. 63-73, 2001.
[5] R.N. Pan, J.H. Chen, and R.R. Chen, "Enhancement of dissolution and bioavailability of piroxicam in solid dispersion systems," Drug. Dev. Ind. Pharm., vol 26(9), pp. 989-994, 2000.
[6] N. Kohri, Y. Yamayoshi, H. Xin, K. Iseki, N. Sato, S. Todo, and K. Miyazaki, "Improving the Oral Bioavailability of Albendazole in Rabbits by the Solid dispersion Technique," J. Pharm. Pharmacol., vol. 51(2), pp. 159-164, 1999.
[7] W.L. Chiou, and S. Riegleman, "Pharmaceutical Applications of Solid Dispersions Dispersion Systems," J. Pharm. Sci., vol 60(9), pp. 1281- 1302, 1971.
[8] A.T.M. Serajuddin, "Solid dispersion of poorly water-soluble drugs: early promises, subsequent problems and recent breakthroughs," J. Pharm. Sci., vol. 88, pp. 1058-1066, 1999.
[9] M.T. Marin, M.V. Margarit, and G.E. Salcedo, "Characterization and solubility study of solid dispersions of flunarizine and polyvinylpyrrolidone," II Farmaco., vol. 57, pp. 723-727, 2002.
[10] V. Tantishaiyakul, N. Kaewnopparat, and S. Ingkatawornwong, "Properties of solid dispersions of piroxicam in polyvinylpyrrolidone," Int. J. Pharm., 181, pp. 143-151, 1999.
[11] H.H. Tonnesen, "Solubility, chemical and photochemical stability of curcumin in surfactant solutions," Pharmazie, vol. 57(12), pp. 820-824, 2002.
[12] J.M. Gines, M.J. Arias, M.A. Holgado, M.F. Arevalo, and A.M. Rabasco, "Dissolution rate study of triamterene-urea solid dispersions," Drug Dev. Ind. Pharm., vol. 20, pp. 2729-2740, 1994.
[13] H. Sekikawa, M. Nakano, and T. Arita, "Inhibitory effect of polyvinylpyrrolidone on the crystallization of drugs," Chem. Pharm. Bull., vol. 6, pp. 118-126, 1978.
[14] V. Tantishaiyakul, N. Kaewnopparat, and S. Ingkatawornwong, "Properties of solid dispersions of piroxicam in polyvinylpyrrolidone K-30," Int. J. Pharm., vol. 143, pp. 59-66, 1996.
[15] Mooter, G., Wuyts, M., Blaton, N., Busson, R., Grobet, P., Augustijns, P., Kinget, R., "Physical stabilisation of amorphous ketoconazole in solid dispersions with polyvinylpyrrolidone K 25,". Eur. J. Pharm. Sci. vol. 12, pp. 261-269, 2001.
[16] L.P. Ruan, B.Y. Yu, G.M. Fu, and D. Zhu, "Improving the solubility of ampelopsin by solid dispersions and inclusion complexes," J. Pharm. Biomed. Anal., vol. 38(3), pp. 457-464, 2005.
[17] G.P. Bettinetti, P. Mura, F. Giordano, and M. Setti, "Thermal behavior and physicochemical properties of naproxen in mixtures with polyvinylpyrrolidone," Thermochimica. Acta., vol. 199, pp. 165-171, 1992.
[18] M. Moneghini, A. Carcano, G. Zingone, B. Perissutti, "Studies in Dissolution Enhancement of Atenolol: Part I," Int. J. Pharm., vol. 175, pp. 177-183, 1998.
[19] J.L. Ford, "The current status of solid dispersions," Pharm. Acta. Helv., vol. 61(3), pp. 69-88, 1986.
[20] J. Akbuga, A. Gursoy, and E. Kendi, "The preparation and stability of fast release furosemide-PVP solid dispersion," Drug Dev. Ind. Pharm., vol. 14, pp. 1439-1464, 1988.