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Amphiphilic polyaspartamide copolymer-based micelles for rivastigmine delivery to neuronal cells

2012

A novel polysorbate-80 (PS(80))-attached amphiphilic copolymer comprising a hydrophilic α,β-poly(N-2-hydroxyethyl)-D,L-aspartamide (PHEA) backbone and hydrophobic squalenyl-C(17) (Sq(17)) portions was synthesized and characterized; the formation of polymeric micelles was also evaluated. Rivastigmine free-base (Riv), a hydrophobic drug employed to treat Alzheimer's disease, was chosen as model drug to investigate micelle's ability to incorporate hydrophobic molecules and target them to neuronal cells. Micelle formation was studied through analyses including fluorescence spectroscopy and 2D (1)H-NMR NOESY experiments. Finally, the capacity of Riv-loaded micelles, versus free drug, to penetrat…

Materials sciencePhenylcarbamatesPharmaceutical ScienceRivastigminepolyaspartamide micelles rivastigmine drug delivery neuronal cellsMicelleFluorescence spectroscopyHydrophobic effectMiceNeuroblastomachemistry.chemical_compoundDrug Delivery SystemsCell Line TumorAmphiphileCopolymerAnimalsHumansOrganic chemistryParticle SizeMicellesAlkylNeuronschemistry.chemical_classificationPolysorbateDrug CarriersGeneral MedicineHydrophobeNeuroprotective AgentsSpectrometry FluorescencechemistryBiophysicsPeptidesHydrophobic and Hydrophilic InteractionsDrug Delivery
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