Use of Block Copolymers of Poly(Ortho Esters) and Poly (Ethylene Glycol) Micellar Carriers as Potential Tumour Targeting Systems

Use of Block Copolymers of Poly(Ortho Esters) and Poly (Ethylene Glycol) Micellar Carriers as Potential Tumour Targeting Systems
July 2003
V. Toncheva A1, E. Schacht A1, S.Y. Ng A2, J. Barr A2, J. Heller A2
A1 Laboratory of Organic Chemistry University of Gent 281 Gent B-9000 Krigslaan Belgium
A2 AP Pharma 123 Saginaw Drive 94063 Redwood City CA USA
Journal of Drug Targeting Volume 11, Number 6 / July 2003 Pages: 345 - 353
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Abstract:
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 ? 10
-4
-5 ? 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?C for 3 days and in a citrate buffer at pH 5.5 and 37?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.