| In vivo antitumor activity of the folate-conjugated pH-sensitive polymeric micelle selectively releasing adriamycin in the intracellular acidic compartments. | |
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MedLine Citation:
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PMID: 17488066 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Cancer treatment efficacy and safety of the environmentally sensitive polymeric micelle drug carriers were significantly increased by optimizing the number of ligands on their surface. These micelles were designed to target the cancerous tumors through the interaction between folate and its receptors that overexpress on the cancer cell membrane while achieving pH-controlled drug release in the intracellular acidic compartments such as endosomes and lysosomes. In order to elucidate the effects of folate on cytotoxicity, biodistribution, anticancer activity, and pharmacological properties, folate concentration on the surface of the micelles was controlled by precise synthesis of two different amphiphilic block copolymers that self-assemble into spherical micelles, folate-poly(ethylene glycol)-poly(aspartate-hydrazone-adriamycin) with gamma-carboxylic acid activated folate and methoxy-poly(ethylene glycol)-poly(aspartate-hydrazone-adriamycin) without folate. It is of significance that, although folate conjugation induced an extremely small change in tumor accumulation of the micelles, folate-conjugated micelles showed lower in vivo toxicity and higher antitumor activity over a broad range of the dosage from 7.50 to 26.21 mg/kg, which was 5-fold broader than free drugs. |
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Authors:
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Younsoo Bae; Nobuhiro Nishiyama; Kazunori Kataoka |
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Publication Detail:
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Type: Journal Article Date: 2007-05-09 |
Journal Detail:
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Title: Bioconjugate chemistry Volume: 18 ISSN: 1043-1802 ISO Abbreviation: Bioconjug. Chem. Publication Date: 2007 Jul-Aug |
Date Detail:
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Created Date: 2007-07-19 Completed Date: 2007-10-04 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9010319 Medline TA: Bioconjug Chem Country: United States |
Other Details:
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Languages: eng Pagination: 1131-9 Citation Subset: IM |
Affiliation:
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Center for Disease Biology and Integrative Medicine, Graduate School of Medicine, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Antibiotics, Antineoplastic / administration & dosage*, chemistry, pharmacokinetics Cell Survival / drug effects Doxorubicin / administration & dosage*, chemistry, pharmacokinetics Drug Carriers / administration & dosage, chemistry, pharmacokinetics Female Folic Acid / administration & dosage*, chemistry, pharmacokinetics Humans Hydrogen-Ion Concentration KB Cells Mice Mice, Nude Micelles* Neoplasm Transplantation Neoplasms / drug therapy, metabolism Polymers / administration & dosage*, chemistry, pharmacokinetics Tumor Burden / drug effects |
| Chemical | |
Reg. No./Substance:
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0/Antibiotics, Antineoplastic; 0/Drug Carriers; 0/Micelles; 0/Polymers; 23214-92-8/Doxorubicin; 59-30-3/Folic Acid |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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