Novel biodegradable polyester poly(propylene succinate): synthesis and application in the preparation of solid dispersions and nanoparticles of a water-soluble drug.
Poly(propylene succinate) (PPSu) polymers of average molecular weights from 2,800 to 13,100 g/mol were synthesized and characterized with regard to crystallinity, thermal properties, and cytocompatibility. Higher molecular weight samples exhibited lower degree of crystallinity and melted at lower temperatures. Melting of the polymer appeared to begin at 38 degrees C. PPSu cytocompatibility was investigated based on human umbilical vein endothelial cells viability in the presence of increasing concentrations of polymer, and it was found that PPSu exhibited comparable cytocompatibility with poly(DL-lactide). The feasibility of applying PPSu as a drug carrier was shown for the first time, as solid dispersions and nanoparticles of sodium fluvastatin based in PPSu were prepared. Drug release rates decreased with increasing the molecular weight of PPSu in both solid dispersions and nanoparticles. For dispersions prepared from PPSu of the same molecular weight, drug release rates increased with drug loading. It appears that PPSu applicability as a drug carrier warrants further consideration.
Bikiaris
Dimitrios N
DN
Laboratory of Organic Chemical Technology, Chemistry Department, Aristotle University of Thessaloniki, Thessaloniki, Greece. dbic@chem.auth.gr
Papageorgiou
George Z
GZ
Papadimitriou
Sofia A
SA
Karavas
Evangelos
E
Avgoustakis
Konstantinos
K
D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D002626:Chemistry, Pharmaceutical; D003460:Crystallization; D004337:Drug Carriers; D004339:Drug Compounding; D042783:Endothelial Cells / Q000187:drug effects / Q000473:pathology; D005229:Fatty Acids, Monounsaturated / Q000737:chemistry*; D005240:Feasibility Studies; D000077340:Fluvastatin; D006801:Humans; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors / Q000737:chemistry*; D007211:Indoles / Q000737:chemistry*; D007700:Kinetics; D008970:Molecular Weight; D053758:Nanoparticles; D011091:Polyesters / Q000737:chemistry* / Q000633:toxicity; D012995:Solubility; D013678:Technology, Pharmaceutical / Q000379:methods; D044366:Transition Temperature
D004337:Drug Carriers; D005229:Fatty Acids, Monounsaturated; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D007211:Indoles; D011091:Polyesters; C541439:poly(propylene succinate); D000077340:Fluvastatin