Use of block copolymers of poly(ortho esters) and poly (ethylene glycol) micellar carriers as potential tumour targeting systems.
Amphiphilic AB and ABA block copolymers have been prepared from poly (ortho esters) and poly (ethylene glycol). Such block copolymers readily form micellar dispersions in water, or buffers. The CMC is in the range of 3 x 10(-4)-5 x 10(-4) g/l which is a value low enough to assure retention of micelle integrity upon intravenous injection. The size, as determined by dynamic light scattering was in the 40-70 nm range. The micelles can be stored in lyophilized form for at lest 8 months and easily reconstituted to the original properties. The micelles are stable in PBS at pH 7.4 and 37 degrees C for 3 days and in a citrate buffer at pH 5.5 and 37 degrees C for 2 h. Stability in the presence of bovine serum albumin depends on the structure of the block copolymer and especially the length of the POE block.
Toncheva
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Laboratory of Organic Chemistry, University of Gent, 281 Gent, B-9000 Krigslaan, Belgium.
Schacht
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Ng
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Barr
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Heller
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D004337:Drug Carriers; D004355:Drug Stability; D006863:Hydrogen-Ion Concentration; D009682:Magnetic Resonance Spectroscopy; D008823:Micelles; D008970:Molecular Weight; D009369:Neoplasms / Q000188:drug therapy / Q000378:metabolism*; D010316:Particle Size; D011091:Polyesters / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*; D012710:Serum Albumin, Bovine / Q000737:chemistry
D004337:Drug Carriers; D008823:Micelles; D011091:Polyesters; D012710:Serum Albumin, Bovine; D011092:Polyethylene Glycols