Biodegradable ion-exchange microspheres based on modified polylysines

摘要: Poly-L-lysine was synthesized via a triethylamine initiated ring-opening polymerization of Z-L-lysine-N'~-carboxyanhydride, followed by deprotection the E-amino group. Subsequently polylysine sulfamated using pyridinium-sulfate complex to obtain polymers with varying degrees sulfamation ranging from 0 100%. Cytotoxicity these materials tested tetrazolium metabolism (MTI') assays B16F10 and P388 cell lines. polylysines degree 80% higher significantly reduced as compared native polylysines. In both lines, LDso than 5 mg/ml, which highest dose tested. lower 0.1 mg/ml in case 0.01 cells. Sulfamated were used prepare microspheres (SPLMS). The stabilized glutaraldehyde or oxidized dextran crosslinking agent. swelling ratio (defined V~wollen/Vdr~ed) SPLMS aqueous media decreased increasing ionic strength crosslink density. pH (ranging 3 11) had no influence on SPLMS. maximal approximately 35 (SPLMS crosslinked 0.5% distilled water). could be loaded adriamycin up payload 60%, not influenced method. release controlled medium: drug released non-ionic medium such water, while phosphate buffered saline. This effect change applied microsphere suspension 5% glucose solution, does contain free adriamycin. would only after intra-arterial administration this suspension, due to the presence blood.