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Journal of Bioactive and Compatible Polymers
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Poly(Ethylene Glycol)-Doxorubicin Conjugates with pH-Controlled Activation

Michal Pechar

Institute of Macromolecular Chemistry, Academy of Sciences of the Czech Republic, 162 06 Prague 6, Czech Republic, pechar{at}imc.cas.cz

Alena Braunová

Institute of Macromolecular Chemistry, Academy of Sciences of the Czech Republic, 162 06 Prague 6, Czech Republic

Karel Ulbrich

Institute of Macromolecular Chemistry, Academy of Sciences of the Czech Republic, 162 06 Prague 6, Czech Republic

Markéta Jelínková

Institute of Microbiology, Academy of Sciences of the Czech Republic, 142 20 Prague 4, Czech Republic

Blanka Ríhová

Institute of Microbiology, Academy of Sciences of the Czech Republic, 142 20 Prague 4, Czech Republic

The synthesis and physico-chemical characterisation of a biodegradable multiblock polymer drug carrier based on poly(ethylene glycol) (PEG) is described. The blocks of PEG (M w 2,000) are connected by an enzymatically degradable tripeptide derivative consisting of one lysine and two glutamic acid residues. Doxorubicin (Dox), was attached to the polymer carrier via a hydrazone bond susceptible to acid hydrolysis at pH 5.0. Human immunoglobulin (IgG) was covalently linked to the polymer-Dox conjugate by the reaction of 2-pyridyldisulfanyl groups of the polymer with thiol groups of the antibody modified with 2-iminothiolane. The resulting antibody-polymer-drug conjugates were characterised by size-exclusion chromatography, UV/VIS spectrophotometry, electrophoresis and amino acid analysis. All polymers studied (both with and without IgG) showed high anti-proliferative activity against concanavalin A-stimulated murine splenocytes and various cancer cell lines in vitro. The polymer-Dox conjugate (without IgG) exhibited a significant anti-tumor efficacy against murine EL4 T-cell lymphoma and human colorectal carcinoma SW620 in vivo.

Key Words: biodegradable polymer • drug delivery systems • drug release • drug carrier • hydrophilic polymers • cancer therapy • doxorubicin • poly(ethylene glycol)

Journal of Bioactive and Compatible Polymers, Vol. 20, No. 4, 319-341 (2005)
DOI: 10.1177/0883911505055161
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