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PEGylated immunoliposomes directed against brain astrocytes
V P Chekhonin1, Yu A Zhirkov, O I Gurina
1Laboratory of Immunochemistry, Serbsky National Research Centre for Social and Forensic Psychiatry, Moscow, Russia. chekhonin@aport.ru
Polyethylene glycol (PEG)ylated (stealth) immunoliposomes directed against human gliofibrillary acidic protein (GFAP) were prepared by coupling the thiolated monoclonal anti-GFAP antibodies with a maleimide derivative of phosphatidyl ethanolamine of the liposomal membrane. Experiments with cell cultures demonstrated specific and competitive binding of these immunoliposomes to embryonic rat brain astrocytes. Administered intravenously into rats, the immunoliposomes displayed typical kinetics with elimination half-lives of 8-15 hr. Being incapable of penetrating the unimpaired blood-brain barrier (BBB), these immunoliposomes, nevertheless, may be useful in delivering drugs to glial brain tumors (which continue to express GFAP) or to other pathological loci in the brain with a partially disintegrated BBB.
Polyethylene glycol (PEG)ylated (stealth) immunoliposomes directed against human gliofibrillary acidic protein (GFAP) were prepared by coupling the thiolated monoclonal anti-GFAP antibodies with a maleimide derivative of phosphatidyl ethanolamine of the liposomal membrane. Experiments with cell cultures demonstrated specific and competitive binding of these immunoliposomes to embryonic rat brain astrocytes. Administered intravenously into rats, the immunoliposomes displayed typical kinetics with elimination half-lives of 8-15 hr. Being incapable of penetrating the unimpaired blood-brain barrier (BBB), these immunoliposomes, nevertheless, may be useful in delivering drugs to glial brain tumors (which continue to express GFAP) or to other pathological loci in the brain with a partially disintegrated BBB.
