Biodegradable paclitaxel-loaded microparticles prepared from novel block copolymers: influence of polymer composition on drug encapsulation and release

作者：Sartori Susanna; Caporale Andrea; Rechichi Alfonsina; Cufari Domenico; Cristallini Caterina; Barbani Niccoletta; Giusti Paolo; Ciardelli Gianluca^*

来源：Journal of Peptide Science, 2013, 19(4): 205-213.

DOI：10.1002/psc.2491

• tailor-made polymers
• biodegradable polymers
• polymer synthesis
• molecular engineering
• nanomaterials

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: 1100 mu m; resuspension index: 18.8100%; encapsulation efficiency: 26.697.2%) 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.

• 出版日期2013-4