Antonio O Costa, Claure N Lunardi and Anderson J Gomes*
PURPOSE: The aim of this study was to assess the pharmacokinetics of the anti-tumor drug chlorambucil (CLB) was incorporated into PLGA nanoparticles (NP-CLB) without and with the presence of the O-stearoyl mannose (OEM) functionalizing agent (NP-CLB-MAN). METHOD: 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 FTIR. 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 NP-CLB-MAN, and the zeta potential of-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 show the 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, which were analyzed considering the mathematical models of Korsmeyer-Peppas, first order, diffusion of Fick, 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 the combination of the first order and Fick diffusion mathematical models.
PLGA, Mathematical modeling., Nanoparticles, O-stearoyl mannose, chlorambucil
Federal Institute of Acre, Av. Brasil, 920 - Xavier Maia, Rio Branco, 69903-068, AC, Laboratory of Photochem- istry and Nanobiotechnology,, University of Brasília, Centro Metropolitano, Conjunto A, lote 01, Brasilia, 72220-275, DF, Laboratory of Photochem- istry and Nanobiotechnology,, University of Brasília, Centro Metropolitano, Conjunto A, lote 01, Brasilia, 72220-275, DF