Formulation optimization and in situ absorption in rat intestinal tract of quercetin-loaded microemulsion

被引：139
作者：
Gao, Yan [1 ]
Wang, Yuqiang [1 ]
Ma, Yukun [2 ]
Yu, Aihua [1 ]
Cai, Fengqun [1 ]
Shao, Wei [1 ]
Zhai, Guangxi [1 ]
机构：
[1] Shandong Univ, Coll Pharm, Dept Pharmaceut, Jinan 250012, Peoples R China
[2] Second Peoples Hosp Jinan, Dept Pharm, Jinan 250001, Peoples R China
来源：
COLLOIDS AND SURFACES B-BIOINTERFACES | 2009年 / 71卷 / 02期
关键词：
Microemulsion; Quercetin; Simplex lattice mixture design; DRUG-DELIVERY SYSTEM; LYMPHATIC TRANSPORT; O/W MICROEMULSION; DESIGN; BIOAVAILABILITY; PERMEABILITY; PERFUSION; DOXORUBICIN; MEMBRANE; RELEASE;
D O I：
10.1016/j.colsurfb.2009.03.005
中图分类号：
Q6 [生物物理学];
学科分类号：
071011 ;
摘要：
A new microemulsion system has been developed to increase the solubility and oral absorption of quercetin, a poorly water-soluble drug. The formulation of quercetin-loaded microemulsion was optimized by a simplex lattice experiment design. The optimized microemulsion formulation consisted of oil (7%, w/w), surfactant (48%, w/w), and cosurfactant (45%, w/w). Under this condition, the mean droplet diameter of microemulsion was 38.9 nm and solubility of quercetin in the microemulsion was 4.138 mg/ml. The in situ absorption property of quercetin-loaded microemulsion in rat intestine was studied and the results showed there was significant difference in absorption parameters such as K-a, t(1/2) and uptake percentages between microemulsion and micelle solution containing quercetin. The study on absorption percentage in different regions of rat intestine attested that the colon had the best permeability, followed by ileum. duodenum in order. It can be concluded that microemulsion can improve the solubility and oral absorption of quercetin, a poorly water-soluble drug. (C) 2009 Elsevier B.V. All rights reserved.
引用
收藏
页码：306 / 314
页数：9
相关论文
共 46 条
  • [1] The novel formulation design of self-emulsifying drug delivery systems (SEDDS) type O/W microemulsion III: The permeation mechanism of a poorly water soluble drug entrapped O/W microemulsion in rat isolated intestinal membrane by the ussing chamber method
    Araya, Hiroshi
    Tomita, Mikio
    Hayashi, Masahiro
    [J]. DRUG METABOLISM AND PHARMACOKINETICS, 2006, 21 (01) : 45 - 53
  • [2] Combination of lipids and emulsifiers enhances the absorption of orally administered quercetin in rats
    Azuma, K
    Ippoushi, K
    Ito, H
    Higashio, H
    Terao, J
    [J]. JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY, 2002, 50 (06) : 1706 - 1712
  • [3] Characterization of jejunal absorption and apical efflux of ropivacaine, lidocaine and bupivacaine in the rat using in situ and in vitro absorption models
    Berggren, S
    Hoogstraate, J
    Fagerholm, U
    Lennernäs, H
    [J]. EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2004, 21 (04) : 553 - 560
  • [4] Biological parametric mapping: A statistical toolbox for multimodality brain image analysis
    Casanova, Ramon
    Srikanth, Ryali
    Baer, Aaron
    Laurienti, Paul J.
    Burdett, Jonathan H.
    Hayasaka, Satoru
    Flowers, Lynn
    Wood, Frank
    Maldjian, Joseph A.
    [J]. NEUROIMAGE, 2007, 34 (01) : 137 - 143
  • [5] ESTIMATING THE MAXIMAL POTENTIAL FOR INTESTINAL LYMPHATIC TRANSPORT OF LIPOPHILIC DRUG MOLECULES
    CHARMAN, WNA
    STELLA, VJ
    [J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1986, 34 (1-2) : 175 - 178
  • [6] A study of microemulsion systems for transdermal delivery of triptolide
    Chen, HB
    Chang, XL
    Weng, T
    Zhao, XZ
    Gao, ZH
    Yang, YJ
    Xu, HB
    Yang, XL
    [J]. JOURNAL OF CONTROLLED RELEASE, 2004, 98 (03) : 427 - 436
  • [7] Chen Q, 2008, NEUROENDOCRINOL LETT, V29, P41
  • [8] Self-microemulsifying drug delivery system (SMEDDS) of vinpocetine:: Formulation development and in vivo assessment
    Chen, Ying
    Li, Gao
    Wu, Xianggen
    Chen, Zhiyu
    Hang, Jiangeng
    Qin, Bei
    Chen, Song
    Wang, Ruihua
    [J]. BIOLOGICAL & PHARMACEUTICAL BULLETIN, 2008, 31 (01) : 118 - 125
  • [9] Validation of an isocratic LC method for determination of quercetin and methylquercetin in topical nanoemulsions
    Fasolo, Daniel
    Schwingel, Liege
    Holzschuh, Maribete
    Bassani, Valquiria
    Teixeira, Helder
    [J]. JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, 2007, 44 (05) : 1174 - 1177
  • [10] Relationship between structural features and in vitro release of doxorubicin from biocompatible anionic microemulsion
    Formariz, T. P.
    Chiavacci, L. A.
    Sarmento, V. H. V.
    Santilli, C. V.
    do Egito, E. S. Tabosa
    Oliveira, A. G.
    [J]. COLLOIDS AND SURFACES B-BIOINTERFACES, 2007, 60 (01) : 28 - 35
12345