Title:Kinetic Evaluation of Anti-tumor Chlorambucil Release from O-stearoyl Mannose PLGA Nanoparticles
Volume: 10
Issue: 1
Author(s): Antonio O. Costa, Claure N. Lunardi and Anderson J. Gomes*
Affiliation:
- Laboratory of Photochemistry and Nanobiotechnology, University of Brasília, Centro Metropolitano, Conjunto A, lote 01, Brasilia, 72220-275, DF,Brazil
Keywords:
PLGA, nanoparticles, o-stearoyl mannose, chlorambucil, mathematical modeling.
Abstract:
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.