Antonio O. Costa, Claure N. Lunardi and Anderson J. Gomes* Pages 63 - 75 ( 13 )
Purpose: This study assesses the kinetics of the anti-tumor drug chlorambucil (CLB) incorporated into PLGA nanoparticles (NP-CLB) with and without the presence of the O-stearoyl mannose (OEM) functionalizing agent (NP-CLBMAN).Methods: OEM was synthesized and used in the NP-CLB-MAN formulation. The nanoparticles were characterized by dynamic light scattering, electrophoretic light scattering, scanning electron microscopy, and Fourier-transform infrared spectroscopy. Results: The nanoparticles presented an encapsulation efficiency greater than 61% and a PdI between 0.186–0.217. The mean size was 185 nm for NP-CLB and 220 nm for NPCLB- MAN, and the zeta potential values were -17.7 mV for NP-CLB and -14.2 mV for NP- CLB-MAN. Scanning electron microscopy showed that NPs with OEM have a surface with a different shape, and FTIR analyses showed binding of CLB to the drug delivery system, as well as functionalization with OEM. In vitro release studies showed a biphasic release profile for both systems, and they were analyzed considering the mathematical Korsmeyer-Peppas, first-order, and Fick diffusion models, and the combination of the first-order and Fick diffusion models. Conclusion: The experimental results obtained for the release of CLB were better described using a combination of the first order and Fick diffusion mathematical models.
PLGA, nanoparticles, o-stearoyl mannose, chlorambucil, mathematical modeling.
Instituto Federal do Acre, Av. Brasil, 920 - Xavier Maia, Rio Branco, 69903-068, AC, Laboratory of Photochemistry and Nanobiotechnology, University of Brasília, Centro Metropolitano, Conjunto A, lote 01, Brasilia, 72220-275, DF, Laboratory of Photochemistry and Nanobiotechnology, University of Brasília, Centro Metropolitano, Conjunto A, lote 01, Brasilia, 72220-275, DF