Abstract��
OBJECTIVE To improve the dissolution and bioavailability of curcumin. METHODS Polyvinylpyrrolidone, sodium dodecyl sulfonate, and poloxamer were used as stabilizing agent. Curcumin nanosuspension was prepared by solvent precipitation method combined with high shear homogenization. The prescription was optimized with average particle size, polydispersity index and Zeta potential as indexes. RESULTS The prescription using polyvinylpyrrolidone was the most stable when the mass ratio of curcumin to PVP was 1��2 and the cutting speed was 250 000 rmin-1. The nanoparticles in curcumin nanosuspension were amorphous and spherical with diameter of about 100 nm. The in vitro release experimental showed that the dissolution of curcumin nanosuspension was significantly improved compared with crude curcumin. Characteristic curve fitting showed that the release of curcumin in the nanosuspension could be fitted to zero-order equation. CONCLUSION The prepared curcumin nanosuspension has good sustained release property.
ZHANG Cai-Yun-,
,
YUAN Hui-Ling- etc
.Preparation and in Vitro Dissolution of Curcumin Nanosuspension[J] Chinese Pharmaceutical Journal, 2014,V49(21): 1917-1922
��
[1]
ESATBEYOGLU T, HUEBBE P, ERNST I M, et al. Curcumin from molecule to biological function [J]. Angew Chem Int Ed Engl, 2012, 51(22): 5308-5332.[2] ZHOU H Y, JIANG H X. Effect of curcumin on inhibiting proliferation and inducing apoptosis of gastric cancer cell BGC-823 [J]. Anhui Med Pharm J (����ҽҩ), 2012, 16(6): 749-751.[3] CHENG Y, BIAN Y, XU L, et al.In vitro pharmacokinetic study of curcumin [J]. Anhui Med Pharm J (����ҽҩ), 2011,15(1): 4-6.[4] LIU H Y, WANG H Y, YE S, et al.Research progress of curcumin pharmacological action and mechanism [J]. China J Mod Med (�й��ִ�ҽѧ��־), 2012, 22(6): 48-51.[5] LI Q, JIN J, XU Y. Research advances on the pharmacological effect and clinical application of curcumin [J]. Mod J Integr Tradit Chin West (�ִ�����ҽ�����־), 2012, 21(12): 1366-1368.[6] XIE X Y, CHENG C, LIAO X R, et al. Physical stability of nanosuspensions: Research adavances [J]. J Int Pharm Res (����ҩѧ�о���־), 2011, 38(5): 369-374. [7] JACOBS C, KAYSER O, M�zLLER R H. Production and characterization of mucoadhesive nanosuspensions for the formulation of bupravaquone[J]. Int J Pharm, 2001, 214(1-2): 3-7.[8] SCH�]LER N, KRAUSE K, KAYSER O, et al. Atovaquone nanosuspensions show excellent therapeutic effect in a new murine model of reactivated toxoplasmosis[J]. Antimicrob Agents Ch, 2001, 45(6): 1771-1779.[9] WU Y, LOPER A, LANDIS E, et al. The role of biopharmaceutics in the development of a clinical nanoparticle formulation of MK-0869: A Beagle dog model predicts improved bioavailability and diminished food effect on absorption in human [J]. Int J Pharm, 2004, 285(1-2): 135-146.[10] PETERSEN R. Nanocrystals for use in topical cosmetic formulations and method of production there of W/O, 2008058755(A1) [P]. 2010-02-25.[11] KRAFT W K, STEIGER B, BEUSSINK D, et al. The pharmacokinetics of nebulized nanocrystal budesonide suspension in healthy volunteers [J]. J Clin Pharmacol, 2004, 44(1): 67-72.[12] BI C, WANG Y C, CHEN X P, et al.In-vitro studies on anticancer activity and cellular untake of curcumin nanosuspensions [J]. Tradit Chin Drug Res Clin Pharmacol(��ҩ��ҩ���ٴ�ҩ��), 2013,24(4): 416-420.[13] ZHONG R L, WU J, SONG J, et al. In vivo pharmacokinetics investigation of curcumin nanosuspensions in rats [J]. Chin J Exp Tradit Med Form(�й�ʵ�鷽��ѧ��־), 2013,19(20):137-139.[14] LVOV Y M, PATTEKARI P, ZHANG X, et al. Converting poorly soluble materials into stable aqueous nanocolloids[J]. Langmuir, 2011, 27(3): 1212-1217.[15] ZHANG H, ZHANG L K, YUAN P, et al. Preparation and in vitro release characteristics of curcumin in nanosuspensions [J]. China J Chin Mater Med (�й���ҩ��־), 2011,36(2):132-135. [16] BASNIWAL R K, BUTTAR H S, JAIN V K, et al. Curcumin nanoparticles: Preparation, characterization, and antimicrobial study[J]. J Agric Food Chem, 2011, 59(5):2056-2061.[17] OWEN H, GRAHAM S, WERLING J, et al. Anion effects on electrostatic charging of sterically stabilized, water insoluble drug particles [J]. Int J Pharm, 2009,368(1-2):154-159.[18] GUAN H, OU Y M, LIANG J Y, et al. Preparation of curcumin in solid dispersion and investigation of its dissolution behavior [J]. J Shenyang Pharm Univ (����ҩ�ƴ�ѧѧ��), 2009,26(12):945-950,955.
2014, Vol. 49 
