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Biodegradable paclitaxel‐loaded microparticles prepared from novel block copolymers: influence of polymer composition on drug encapsulation and release
Author(s) -
Sartori Susanna,
Caporale Andrea,
Rechichi Alfonsina,
Cufari Domenico,
Cristallini Caterina,
Barbani Niccoletta,
Giusti Paolo,
Ciardelli Gianluca
Publication year - 2013
Publication title -
journal of peptide science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.475
H-Index - 66
eISSN - 1099-1387
pISSN - 1075-2617
DOI - 10.1002/psc.2491
Subject(s) - polymer , copolymer , microparticle , controlled release , emulsion , chemical engineering , polyurethane , materials science , drug delivery , chemistry , paclitaxel , polymer chemistry , nanotechnology , organic chemistry , engineering , medicine , surgery , chemotherapy
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. Copyright © 2013 European Peptide Society and John Wiley & Sons, Ltd.