Production and Characterization of Chitosan-Polyanion Nanoparticles by Polyelectrolyte Complexation Assisted by High-Intensity Sonication for the Modified Release of Methotrexate

A promising strategy to improve the effectivity of anticancer treatment and decrease its side effects is to modulate drug release by using nanoparticulates (NPs) as carriers. In this study, methotrexate-loaded chitosan−polyanion nanoparticles were produced by polyelectrolyte complexation a...

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Main Authors: Yhors Ciro (Author), John Rojas (Author), Maria J. Alhajj (Author), Gustavo A. Carabali (Author), Constain H. Salamanca (Author)
Format: Book
Published: MDPI AG, 2020-01-01T00:00:00Z.
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Summary:A promising strategy to improve the effectivity of anticancer treatment and decrease its side effects is to modulate drug release by using nanoparticulates (NPs) as carriers. In this study, methotrexate-loaded chitosan&#8722;polyanion nanoparticles were produced by polyelectrolyte complexation assisted by high-intensity sonication, using several anionic polymers, such as the sodium and potassium salts of poly(maleic acid-<i>alt</i>-ethylene) and poly(maleic acid-<i>alt</i>-octadecene), here named PAM-2 and PAM-18, respectively. Such NPs were analyzed and characterized according to particle size, polydispersity index, zeta potential and encapsulation efficiency. Likewise, their physical stability was tested at 4 &#176;C and 40 &#176;C in order to evaluate any change in the previously mentioned particle parameters. The in vitro methotrexate release was assessed at a pH of 7.4, which simulated physiological conditions, and the data were fitted to the heuristic models of order one, Higuchi, Peppas&#8722;Sahlin and Korsmeyer&#8722;Peppas. The results revealed that most of the MTX-chitosan&#8722;polyanion NPs have positive zeta potential values, sizes &lt;280 nm and monodisperse populations, except for the NPs formed with PAM-18 polyanions. Further, the NPs showed adequate physical stability, preventing NP&#8722;NP aggregation. Likewise, these carriers modified the MTX release by an anomalous mechanism, where the NPs formed with PAM-2 polymer led to a release mechanism controlled by diffusion and relaxation, whereas the NPs formed with PAM-18 led to a mainly diffusion-controlled release mechanism.
Item Description:1424-8247
10.3390/ph13010011