title: Biodegradable paclitaxel-loaded microparticles prepared from novel block copolymers: influence of polymer composition on drug encapsulation and release.
abstract: This study covers the preparation of microspheres for the controlled and targeted release of paclitaxel, using novel degradable polymers as carrier materials. Paclitaxel-loaded microspheres were prepared by oil-in-water single-emulsion solvent extraction/evaporation technique by using a series of polyurethanes and a block copolymer; the physicochemical properties of these polymers were modulated by changing nature and composition of their structural units. The obtained microparticles showed a regular morphology and properties (diameter: 1-100 µm; resuspension index: 18.8-100%; encapsulation efficiency: 26.6-97.2%) depending on polymer hydrophilicity and emulsifier used. In vitro release curves showed in all cases almost zero-order kinetics after an initial low burst effect (from 1 to 8.4%), which is required to minimize the drug side effects. This work also proposes a novel strategy to combine a controlled and a targeted release through the functionalization of the polymer matrix with peptide sequences. An RGD-functionalized polyurethane was used to successfully prepare paclitaxel-loaded microparticles. Studies on the preparation of polymer microspheres are reported.
authors.affiliation: Department of Mechanical and AerospaceEngineering, Politecnico di Torino, Torino, Italy.
authors.forename: Susanna
authors.initials: S
authors.lastname: Sartori
authors.forename: Andrea
authors.initials: A
authors.lastname: Caporale
authors.forename: Alfonsina
authors.initials: A
authors.lastname: Rechichi
authors.forename: Domenico
authors.initials: D
authors.lastname: Cufari
authors.forename: Caterina
authors.initials: C
authors.lastname: Cristallini
authors.forename: Niccoletta
authors.initials: N
authors.lastname: Barbani
authors.forename: Paolo
authors.initials: P
authors.lastname: Giusti
authors.forename: Gianluca
authors.initials: G
authors.lastname: Ciardelli
mesh_terms: D003692:Delayed-Action Preparations; D004337:Drug Carriers / Q000737:chemistry*; D057927:Hydrophobic and Hydrophilic Interactions; D008863:Microspheres; D009842:Oligopeptides / Q000737:chemistry*; D017239:Paclitaxel / Q000737:chemistry*; D010316:Particle Size; D011140:Polyurethanes / Q000737:chemistry*
chemical_list: D003692:Delayed-Action Preparations; D004337:Drug Carriers; D009842:Oligopeptides; D011140:Polyurethanes; C047981:arginyl-glycyl-aspartic acid; D017239:Paclitaxel