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Novel pH-sensitive lipid-polymer composite microspheres of 10-hydroxycamptothecin exhibiting colon-specific biodistribution and reduced systemic absorption

文献类型：期刊论文

作者Gan, Li1; Gao, Yi-Ping1,2; Zhu, Chun-Liu1; Zhang, Xin-Xin1; Gan, Yong1
刊名JOURNAL OF PHARMACEUTICAL SCIENCES
出版日期2013-06
卷号102期号:6页码:1752-1759
关键词colonic drug delivery polymers lipids pH-sensitive 10-hydroxycamptothecin microspheres biodistribution bioavailability
ISSN号0022-3549
DOI10.1002/jps.23499
文献子类Article
英文摘要Novel lipidpolymer composite microspheres (LP-MS) were prepared by combining pH-sensitive polymer Eudragit S100 with solid lipid Compritol 888 ATO for colonic delivery of 10-hydroxycamptothecin (HCPT), and pH-dependent controlled drug release has been achieved. The colon-specific biodistribution and uptake by the mucosal tissue were examined using coumarin-6-marked LP-MS. It is proved that good in vitroin vivo relationship has been achieved, with more drugs being delivered to colon and a higher drug level was maintained for a long period. Moreover, in vivo bioavailability of LP-MS was evaluated with conventional enteric microspheres (enteric MS) as reference. After administration of LP-MS, systemic absorption of HCPT was greatly reduced, with area under the curve from 0 to 24h (AUC024 h, 2.186 +/- 0.27) being significantly lower than that of enteric MS group (6.352 +/- 0.696). In conclusion, the novel pH-sensitive LP-MS has potential for colon-specific drug delivery. (c) 2013 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 102:17521759, 2013
WOS关键词DRUG-DELIVERY ; IN-VITRO ; DESIGN ; 5-FLUOROURACIL ; MICROPARTICLES ; DISSOLUTION ; BEHAVIOR
资助项目National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program"[2012ZX09301001-001] ; National Basic Research Program of China[2009CB930300]
WOS研究方向Pharmacology & Pharmacy ; Chemistry
语种英语
WOS记录号WOS:000319071200010
出版者WILEY
源URL[http://119.78.100.183/handle/2S10ELR8/277606]  
专题药物制剂研究中心
通讯作者Gan, Yong
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China;
2.Xuhui Dist Cent Hosp, Shanghai 200031, Peoples R China
推荐引用方式
GB/T 7714		 Gan, Li,Gao, Yi-Ping,Zhu, Chun-Liu,et al. Novel pH-sensitive lipid-polymer composite microspheres of 10-hydroxycamptothecin exhibiting colon-specific biodistribution and reduced systemic absorption[J]. JOURNAL OF PHARMACEUTICAL SCIENCES,2013,102(6):1752-1759.
APA Gan, Li,Gao, Yi-Ping,Zhu, Chun-Liu,Zhang, Xin-Xin,&Gan, Yong.(2013).Novel pH-sensitive lipid-polymer composite microspheres of 10-hydroxycamptothecin exhibiting colon-specific biodistribution and reduced systemic absorption.JOURNAL OF PHARMACEUTICAL SCIENCES,102(6),1752-1759.
MLA Gan, Li,et al."Novel pH-sensitive lipid-polymer composite microspheres of 10-hydroxycamptothecin exhibiting colon-specific biodistribution and reduced systemic absorption".JOURNAL OF PHARMACEUTICAL SCIENCES 102.6(2013):1752-1759.

入库方式： OAI收割

来源：上海药物研究所

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