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Mesoporous carbon with spherical pores as a carrier for celecoxib with needle-like crystallinity: Improve dissolution rate and bioavailability

文献类型：期刊论文

作者Zhu, Wenquan2; Zhao, Qinfu2; Sun, Changshan2; Zhang, Zhiwen1; Jiang, Tongying2; Sun, Jin2; Li, Yaping1; Wang, Siling2
刊名MATERIALS SCIENCE & ENGINEERING C-MATERIALS FOR BIOLOGICAL APPLICATIONS
出版日期2014-06-01
卷号39页码:13-20
关键词Mesoporous carbon Poorly water soluble drug Spherical pore Needle-like crystallinity Dissolution kinetics
ISSN号0928-4931
DOI10.1016/j.msec.2014.02.035
文献子类Article
英文摘要The purposes of this investigation are to design mesoporous carbon (MC) with spherical pore channels and incorporate CEL to it for changing its needlelike crystal form and improving its dissolution and bioavailability. A series of solid-state characterization methods, such as SEM, TEM, DSC and XRD, were employed to systematically investigate the existing status of celecoxib (CEL) within the pore channels of MC. The pore size, pore volume and surface area of samples were characterized by nitrogen physical absorption. Gastric mucosa irritation test was carried out to evaluate the safety of mesoporous carbon as a drug carrier. Dissolution tests and in vivo pharmacokinetic studies were conducted to confirm the improvement in drug dissolution kinetics and oral bioavailability. Uptake experiments were conducted to investigate the mechanism of the improved oral bioavailability. The results of solid state characterization showed that MC was prepared successfully and CEL was incorporated into the mesoporous channels of the MC. The crystallinity of CEL in MC was affected by different loading methods, which involve evaporation method and melting method. The dissolution rate of CEL from MC was found to be significantly higher than that of pure CEL, which attributed to reduced crystallinity of CEL. The gastric mucosa irritation test indicated that the MC caused no harm to the stomach and produced a protective effect on the gastric mucosa. Uptake experiments indicated that MC enhanced the amount of CEL absorbed by Caco-2 cells. Moreover, oral bioavailability of CEL loaded within the MC was approximately 1.59-fold greater than that of commercial CEL. In conclusion, MC was a safe carrier to load water insoluble drug by controlling the crystallinity or crystal form with improvement in drug dissolution kinetics and oral bioavailability. (C) 2014 Elsevier B.V. All rights reserved.
WOS关键词POOR WATER SOLUBILITY ; DRUG-DELIVERY ; ORAL BIOAVAILABILITY ; SILICA NANOPARTICLES ; SOLUBLE DRUGS ; ENHANCEMENT ; RELEASE ; NANOTUBES ; PERMEABILITY ; INCLUSION
资助项目National Basic Research Program of China (973 Program)[2009CB930300] ; National Natural Science Foundation of China[81273449]
WOS研究方向Materials Science
语种英语
WOS记录号WOS:000343949200003
出版者ELSEVIER SCIENCE BV
源URL[http://119.78.100.183/handle/2S10ELR8/277037]  
专题药物制剂研究中心
通讯作者Wang, Siling
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Pharmaceut, Shanghai 201203, Peoples R China
2.Shenyang Pharmaceut Univ, Dept Pharmaceut, Shenyang, Peoples R China;
推荐引用方式
GB/T 7714		 Zhu, Wenquan,Zhao, Qinfu,Sun, Changshan,et al. Mesoporous carbon with spherical pores as a carrier for celecoxib with needle-like crystallinity: Improve dissolution rate and bioavailability[J]. MATERIALS SCIENCE & ENGINEERING C-MATERIALS FOR BIOLOGICAL APPLICATIONS,2014,39:13-20.
APA Zhu, Wenquan.,Zhao, Qinfu.,Sun, Changshan.,Zhang, Zhiwen.,Jiang, Tongying.,...&Wang, Siling.(2014).Mesoporous carbon with spherical pores as a carrier for celecoxib with needle-like crystallinity: Improve dissolution rate and bioavailability.MATERIALS SCIENCE & ENGINEERING C-MATERIALS FOR BIOLOGICAL APPLICATIONS,39,13-20.
MLA Zhu, Wenquan,et al."Mesoporous carbon with spherical pores as a carrier for celecoxib with needle-like crystallinity: Improve dissolution rate and bioavailability".MATERIALS SCIENCE & ENGINEERING C-MATERIALS FOR BIOLOGICAL APPLICATIONS 39(2014):13-20.

入库方式： OAI收割

来源：上海药物研究所

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