| In vitro evaluation of a Folate-bovine serum albumin-doxorubicin conjugate. | |
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MedLine Citation:
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PMID: 20001219 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Doxorubicin (DOX) is one of the most effective anticancer drugs. However, its therapeutic effectiveness is greatly hampered by its dose limiting and cumulative cardiotoxic side effects. To overcome these limitations, bioconjugates of DOX were studied using bovine serum albumin (BSA) as a carrier to provide passive tumor targeting by the enhanced permeability and retention (EPR) effect. Folic acid, as an active targeting agent, was linked to BSA to increase the selectivity of the conjugate. In the present study, folate-targeted (Folate-BSA-DOX) conjugates were prepared. In the optimization process, we found that 30 mg of folic acid activated esters reacted with BSA at pH 9.8 for 1 h, the yield was maximum. The qualitative analysis of fluorescent experiments revealed that Folate-BSA-DOX can be specifically delivered to Hela cells and that this unique interaction can be blocked by 1 mM free folic acid. More importantly, the enhanced efficiency of uptake of Folate-BSA-DOX by Hela cells was coupled with the increase of the amount of the conjugate, the incubated time and the conjugated ratio of folic acid. Finally, the quantitative data obtained from the flow cytometry further verified the higher targeting and killing ability of Folate-BSA-DOX to folate receptor positive tumor cells than BSA-DOX. |
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Authors:
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Xiaolan Qu; Chang Yang; Jing Zhang; Nan Ding; Yao Lu; Lei Huang; Guangya Xiang |
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Publication Detail:
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Type: In Vitro; Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Journal of drug targeting Volume: 18 ISSN: 1029-2330 ISO Abbreviation: J Drug Target Publication Date: 2010 Jun |
Date Detail:
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Created Date: 2010-05-06 Completed Date: 2010-08-05 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9312476 Medline TA: J Drug Target Country: England |
Other Details:
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Languages: eng Pagination: 351-61 Citation Subset: IM |
Affiliation:
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School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, China. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Antineoplastic Agents
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administration & dosage,
pharmacology* Doxorubicin / administration & dosage, pharmacology* Drug Evaluation, Preclinical Hela Cells Humans Serum Albumin, Bovine / administration & dosage* Spectrophotometry, Ultraviolet |
| Chemical | |
Reg. No./Substance:
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0/Antineoplastic Agents; 0/Serum Albumin, Bovine; 23214-92-8/Doxorubicin |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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