Abstract | PURPOSE: METHODS: Their binding and cytotoxic activity in vitro, body distribution, and anticancer activity in vivo were evaluated. RESULTS: The results of flow cytometric analysis showed comparable binding of classic and starlike conjugates to the target cells. The in vitro cytotoxic effect was 10-fold higher if cancer cells were exposed to the starlike conjugate compared to the classic one. Biodistribution studies showed that the starlike conjugate remained in a relatively high concentration in blood, whereas the classic conjugate was found in a 6.5-times lower amount. In contrast to the low antitumor activity of free doxorubicin and nontargeted HPMA copolymer- doxorubicin conjugate, both anti-Thy-1.2 targeted conjugates (classic and starlike) cured all mice bearing T-cell lymphoma EL4. On the other hand, starlike conjugates containing anti-CD71/A or anti-CD71/B monoclonals as targeting structures were more effective against human colorectal cancer SW 620 than the classic one. CONCLUSIONS: We have shown that the starlike conjugates are more effective systems for targeted drug delivery and cancer treatment than classic conjugates.
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Authors | Markéta Jelínková, Jirí Strohalm, Tomás Etrych, Karel Ulbrich, Blanka Ríhová |
Journal | Pharmaceutical research
(Pharm Res)
Vol. 20
Issue 10
Pg. 1558-64
(Oct 2003)
ISSN: 0724-8741 [Print] United States |
PMID | 14620507
(Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Antibiotics, Antineoplastic
- Antibodies, Monoclonal
- Methacrylates
- Prodrugs
- Doxorubicin
- hydroxypropyl methacrylate
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Topics |
- Animals
- Antibiotics, Antineoplastic
(chemistry, pharmacokinetics, pharmacology)
- Antibodies, Monoclonal
(chemistry, metabolism)
- Cell Division
(drug effects)
- Cell Line, Tumor
- Colorectal Neoplasms
(drug therapy)
- Doxorubicin
(chemistry, pharmacokinetics, pharmacology)
- Humans
- In Vitro Techniques
- Lymphoma, T-Cell
(drug therapy)
- Methacrylates
(chemistry, pharmacology)
- Mice
- Mice, Inbred BALB C
- Mice, Inbred C57BL
- Molecular Structure
- Neoplasm Transplantation
- Prodrugs
(chemistry, pharmacology)
- Tissue Distribution
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