Preparation and Characterization of Quercetin Nanocrystals

被引:116
作者
Sahoo, N. G. [1 ]
Kakran, M. [1 ]
Shaal, L. A. [2 ]
Li, L. [1 ]
Mueller, R. H. [2 ]
Pal, M. [3 ]
Tan, L. P. [3 ]
机构
[1] Nanyang Technol Univ, Sch Mech & Aerosp Engn, Singapore 639798, Singapore
[2] Free Univ Berlin, Dept Pharm Biopharmaceut & NutriCosmet, D-12169 Berlin, Germany
[3] Nanyang Technol Univ, Sch Mat Sci & Engn, Singapore 639798, Singapore
关键词
antioxidant; crystallinity; dissolution; lyophilization; nanoparticles; particle size; quercetin; x-ray diffractometry; DRUG; NANOSUSPENSIONS; NANOPARTICLES; FLAVONOIDS; RELEASE;
D O I
10.1002/jps.22446
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
This study is to enhance the dissolution rate of a poorly water-soluble drug, quercetin, by fabricating nanocrystals using high-pressure homogenization. The particle size, crystallinity, dissolution, and antioxidant effects of fabricated quercetin nanocrystals have been investigated. Characterization of the original quercetin powder and nanocrystals was carried out by photon correlation spectroscopy (PCS), laser diffraction, scanning electron microscopy, differential scanning calorimetry (DSC), X-ray diffraction, dissolution tester, and so on. A PCS size of about 483nm was obtained for the nanocrystals after 20 cycles of homogenization at 1500 bar. X-ray diffraction and DSC studies revealed that the lyophilized quercetin nanoparticles were crystalline after high-pressure homogenization. The percent dissolution efficiency, relative dissolution, mean dissolution time, difference factor (f(1)), and similarity factor (f(2)) were calculated for the statistical analysis. It was found that the dissolution of the drug nanocrystals was much higher than that of the pure drug at pH 6.8 and 1.2. The antioxidant activity and reducing power of the quercetin nanocrystals were more effective than the original quercetin. (C) 2010 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 100:2379-2390, 2011
引用
收藏
页码:2379 / 2390
页数:12
相关论文
共 42 条
[1]  
Ashish Manigauha Ashish Manigauha, 2009, Journal of Pharmacy Research, V2, P491
[2]   The rutin/β-cyclodextrin interactions in fully aqueous solution:: spectroscopic studies and biological assays [J].
Calabrò, ML ;
Tommasini, S ;
Donato, P ;
Stancanelli, R ;
Raneri, D ;
Catania, S ;
Costa, C ;
Villari, V ;
Ficarra, P ;
Ficarra, R .
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, 2005, 36 (05) :1019-1027
[3]  
Carstensen J.T., 2001, Advanced Pharmaceutical Solids
[4]   Production of griseofulvin nanoparticles using supercritical CO2 antisolvent with enhanced mass transfer [J].
Chattopadhyay, P ;
Gupta, RB .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2001, 228 (1-2) :19-31
[5]   Role of freeze drying in nanotechnology [J].
Chen, Guohua ;
Wang, Wei .
DRYING TECHNOLOGY, 2007, 25 (1-3) :29-35
[6]   In vivo quercitrin anti-inflammatory effect involves release of quercetin, which inhibits inflammation through down-regulation of the NF-κB pathway [J].
Comalada, M ;
Camuesco, D ;
Sierra, S ;
Ballester, I ;
Xaus, J ;
Gálvez, J ;
Zarzuelo, A .
EUROPEAN JOURNAL OF IMMUNOLOGY, 2005, 35 (02) :584-592
[7]   Modeling and comparison of dissolution profiles [J].
Costa, P ;
Manuel, J ;
Lobo, S .
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2001, 13 (02) :123-133
[8]  
DEMIRTURK E, 2005, HACETTEPE U J FACUL, V25, P1
[9]  
DEORE SL, 2009, J PHARM RES, V3, P367
[10]   Preparation and spectral investigation on inclusion complex of β-cyclodextrin with rutin [J].
Ding, HY ;
Chao, JB ;
Zhang, GM ;
Shuang, SM ;
Pan, JH .
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY, 2003, 59 (14) :3421-3429