| pubmed-article:18656539 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:18656539 | lifeskim:mentions | umls-concept:C0596402 | lld:lifeskim |
| pubmed-article:18656539 | lifeskim:mentions | umls-concept:C0441655 | lld:lifeskim |
| pubmed-article:18656539 | lifeskim:mentions | umls-concept:C1533691 | lld:lifeskim |
| pubmed-article:18656539 | lifeskim:mentions | umls-concept:C1515655 | lld:lifeskim |
| pubmed-article:18656539 | lifeskim:mentions | umls-concept:C0301869 | lld:lifeskim |
| pubmed-article:18656539 | lifeskim:mentions | umls-concept:C0063186 | lld:lifeskim |
| pubmed-article:18656539 | pubmed:issue | 3 | lld:pubmed |
| pubmed-article:18656539 | pubmed:dateCreated | 2008-12-10 | lld:pubmed |
| pubmed-article:18656539 | pubmed:abstractText | 5-Fluorouracil (5-FU) is an antimetabolite with a broad-spectrum activity against solid tumors. However, its very short half-life in plasma circulation greatly limited the in vivo antitumor efficacy and clinical application. The current work aimed to solve this problem as well as to increase 5-FU biodistribution to tumor by covalently conjugating 5-FU to a biocompatible, non-toxic and non-immunogenic drug carrier -N-(2-hydroxypropyl) methacrylamide (HPMA) copolymer. The in vitro cytotoxicity, in vivo biodistribution and therapeutic efficacy of HPMA copolymer-5-FU conjugates (P-FU) were reported. Cytotoxicity was evaluated by using a serial of tumor cells (A549, CT-26, Hela, HepG(2) cells and 5-FU resistant HepG(2) cells). In vivo biodistribution and therapeutic efficacy were investigated in Kunming mice-bearing hepatoma 22 (H(22)). Results indicated that P-FU could increase the cytotoxicity of 5-FU in Hela, HepG(2) and 5-FU resistant HepG(2) cells, while it decreases the cytotoxicity of 5-FU in A549 and CT-26. Both in vitro release profile in plasma and biodistribution study showed that P-FU significantly prolonged the drug plasma circulation time. P-FU also showed an over 3-fold larger area under the concentration-time curve (AUC) in tumor when compared with free drug. Therapeutic evaluation also demonstrated that the treatment with P-FU displayed stronger inhibition of the tumor growth when compared with that of control group (physiologic saline) or 5-FU group at the same dose. All the results suggested that P-FU could increase cytotoxicity of 5-FU in certain cancer cell lines, prolong 5-FU circulation time in vivo, enhance 5-FU distribution to tumor and improve therapeutic efficacy. Therefore, HPMA copolymer is a potential carrier for 5-FU for the effective treatment of cancer. | lld:pubmed |
| pubmed-article:18656539 | pubmed:language | eng | lld:pubmed |
| pubmed-article:18656539 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:18656539 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:18656539 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:18656539 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:18656539 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:18656539 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:18656539 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:18656539 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:18656539 | pubmed:month | Nov | lld:pubmed |
| pubmed-article:18656539 | pubmed:issn | 0939-6411 | lld:pubmed |
| pubmed-article:18656539 | pubmed:author | pubmed-author:ZhangZhi-Rong... | lld:pubmed |
| pubmed-article:18656539 | pubmed:author | pubmed-author:ZhouDanD | lld:pubmed |
| pubmed-article:18656539 | pubmed:author | pubmed-author:HuangYuanY | lld:pubmed |
| pubmed-article:18656539 | pubmed:author | pubmed-author:QinXuanX | lld:pubmed |
| pubmed-article:18656539 | pubmed:author | pubmed-author:FangYuanY | lld:pubmed |
| pubmed-article:18656539 | pubmed:author | pubmed-author:XiangQing-YuQ... | lld:pubmed |
| pubmed-article:18656539 | pubmed:author | pubmed-author:WangMin-TingM... | lld:pubmed |
| pubmed-article:18656539 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:18656539 | pubmed:volume | 70 | lld:pubmed |
| pubmed-article:18656539 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:18656539 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:18656539 | pubmed:pagination | 770-6 | lld:pubmed |
| pubmed-article:18656539 | pubmed:meshHeading | pubmed-meshheading:18656539... | lld:pubmed |
| pubmed-article:18656539 | pubmed:meshHeading | pubmed-meshheading:18656539... | lld:pubmed |
| pubmed-article:18656539 | pubmed:meshHeading | pubmed-meshheading:18656539... | lld:pubmed |
| pubmed-article:18656539 | pubmed:meshHeading | pubmed-meshheading:18656539... | lld:pubmed |
| pubmed-article:18656539 | pubmed:meshHeading | pubmed-meshheading:18656539... | lld:pubmed |
| pubmed-article:18656539 | pubmed:meshHeading | pubmed-meshheading:18656539... | lld:pubmed |
| pubmed-article:18656539 | pubmed:meshHeading | pubmed-meshheading:18656539... | lld:pubmed |
| pubmed-article:18656539 | pubmed:meshHeading | pubmed-meshheading:18656539... | lld:pubmed |
| pubmed-article:18656539 | pubmed:meshHeading | pubmed-meshheading:18656539... | lld:pubmed |
| pubmed-article:18656539 | pubmed:meshHeading | pubmed-meshheading:18656539... | lld:pubmed |
| pubmed-article:18656539 | pubmed:meshHeading | pubmed-meshheading:18656539... | lld:pubmed |
| pubmed-article:18656539 | pubmed:meshHeading | pubmed-meshheading:18656539... | lld:pubmed |
| pubmed-article:18656539 | pubmed:meshHeading | pubmed-meshheading:18656539... | lld:pubmed |
| pubmed-article:18656539 | pubmed:meshHeading | pubmed-meshheading:18656539... | lld:pubmed |
| pubmed-article:18656539 | pubmed:meshHeading | pubmed-meshheading:18656539... | lld:pubmed |
| pubmed-article:18656539 | pubmed:meshHeading | pubmed-meshheading:18656539... | lld:pubmed |
| pubmed-article:18656539 | pubmed:meshHeading | pubmed-meshheading:18656539... | lld:pubmed |
| pubmed-article:18656539 | pubmed:year | 2008 | lld:pubmed |
| pubmed-article:18656539 | pubmed:articleTitle | In vitro cytotoxicity, in vivo biodistribution and antitumor activity of HPMA copolymer-5-fluorouracil conjugates. | lld:pubmed |
| pubmed-article:18656539 | pubmed:affiliation | Key Laboratory of Drug Targeting and Drug Delivery, Ministry of Education, West China School of Pharmacy, Sichuan University, Chengdu, PR China. | lld:pubmed |
| pubmed-article:18656539 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:18656539 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:18656539 | lld:pubmed |
