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

页码：306 / 314

页数：9

共 46 条

[31]

Li H., 2004, DRUG DEV IND PHARM, V30, P657

[32] Enhancement of gastrointestinal absorption of quercetin by solid lipid nanoparticles [J].

Li, HouLi ;

Zhao, XiaoBin ;

Ma, YuKun ;

Zhai, GuangXi ;

Li, LingBing ;

Lou, HongXiang .

JOURNAL OF CONTROLLED RELEASE, 2009, 133 (03) :238-244

[33]

Li Hua, 2004, Yaoxue Xuebao, V39, P681

[34] Optimization and in situ intestinal absorption of self-microemulsifying drug delivery system of oridonin [J].

Liu, Ying ;

Zhang, Ping ;

Feng, Nianping ;

Zhang, Xin ;

Wu, Shan ;

Zhao, Jihui .

INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2009, 365 (1-2) :136-142

[35] Self-microemulsifying drug delivery system (SMEDDS) improves anticancer effect of oral 9-nitrocamptothecin on human cancer xenografts in nude mice [J].

Lu, Juan-Li ;

Wang, Jian-Cheng ;

Zhao, Shu-Xin ;

Liu, Xiao-Yan ;

Zhao, Hui ;

Zhang, Xuan ;

Zhou, Shu-Feng ;

Zhang, Qiang .

EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 2008, 69 (03) :899-907

[36] Therapeutic and preventive properties of quercetin in experimental arthritis correlate with decreased macrophage inflammatory mediators [J].

Mamani-Matsuda, Maria ;

Kauss, Tina ;

Al-Kharrat, Abir ;

Rambert, Jerome ;

Fawaz, Fawaz ;

Thiolat, Denis ;

Moynet, Daniel ;

Coves, Sara ;

Malvy, Denis ;

Mossalayi, M. Djavad .

BIOCHEMICAL PHARMACOLOGY, 2006, 72 (10) :1304-1310

[37]

MAO SS, 2004, DESIGN EXPT, pCH4

[38] Site of drug absorption after oral administration: Assessment of membrane permeability and luminal concentration of drugs in each segment of gastrointestinal tract [J].

Masaoka, Yoshie ;

Tanaka, Yusuke ;

Kataoka, Makoto ;

Sakuma, Shinji ;

Yamashita, Shinji .

EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2006, 29 (3-4) :240-250

[39] Stable drug encapsulation in micelles and microemulsions [J].

Narang, Ajit S. ;

Delmarre, David ;

Gao, Danchen .

INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2007, 345 (1-2) :9-25

[40] PHARMACEUTICAL INNOVATION BY THE 7 UK-OWNED PHARMACEUTICAL COMPANIES (1964-1985) [J].

PRENTIS, RA ;

LIS, Y ;

WALKER, SR .

BRITISH JOURNAL OF CLINICAL PHARMACOLOGY, 1988, 25 (03) :387-396

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