RESUMO
The polyester- and poly(ester-carbonate)-paclitaxel conjugates with low molecular weight were synthesized using dicyclohexylcarbodiimide (DCC) and dimethylaminopyridine (DMAP) as catalysts. Polymeric matrices were obtained by ring-opening polymerization of É-caprolactone (CL), rac-lactide (rac-LA), l-lactide (LLA) and trimethylene carbonate (TMC). The macromolecular conjugates were characterized by using spectroscopic techniques, such as (1)H, (13)C NMR and FTIR. The degree of degradation of polyester- and poly(ester-carbonate)-paclitaxel conjugates was tested in vitro under different conditions. The preliminary results of drug release were discussed.
Assuntos
Antineoplásicos Fitogênicos/química , Dioxanos/síntese química , Portadores de Fármacos , Paclitaxel/química , Poliésteres/síntese química , Caproatos/química , Catálise , Preparações de Ação Retardada , Dicicloexilcarbodi-Imida/química , Dioxanos/química , Liberação Controlada de Fármacos , Lactonas/química , Piridinas/químicaRESUMO
The controlled release of 5-fluorouracil (5FU) from aliphatic poly(amide urethane)s (PURs) was studied in vitro. Linear PUR conjugates were prepared by the reaction between oligo(É-caprolactone) (PCL), oligolactide (PLA), copolymers of É-caprolactone (CL) and rac-lactide (rac-LA), dihydroxy(polyethylene adipate) (OEDA) with 1,6-diisocyanatohexane (HDI). Release of 5FU from PURs was found to depend on the nature of oligoester units and consist of soft and hard segments.
Assuntos
Antimetabólitos Antineoplásicos/administração & dosagem , Preparações de Ação Retardada/química , Fluoruracila/administração & dosagem , Poliuretanos/química , Antimetabólitos Antineoplásicos/química , Fluoruracila/químicaRESUMO
New polymeric conjugates were prepared coupling ofloxacin to two-, three-, four and six-arm, star-shaped poly(É-caprolactone) and polylactide. The homopolymers were synthesized via ring-opening polymerization of É-caprolactone, l-lactide and rac-lactide in the presence of glycerol, penthaerythritol, dipentaerythritol and poly(ethylene glycol) as initiators and stannous octoate as a catalyst. The conjugates were characterized by GPC, MALDI-TOF MS, NMR, IR and viscosity methods. Content of Sn has been investigated in polymers by electrothermal atomic absorption spectrometry. Toxicity of monomers, initiators and polymers were evaluated with bacterial luminescence test and two protozoan assays. The in vitro release of ofloxacin from obtained conjugates in pH 7 was investigated.
