Release of chlorambucil from mannose-functionalized PLGA nanoparticles

What is it about?

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-CLB-MAN). 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.

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Photo by L N on Unsplash

Photo by L N on Unsplash

Why is it important?

We describe the release profile of chlorambucil in vitro at pH 7.4 and which mathematical model best describes how chlorambucil is released into the tested medium. These data can be useful for the dosage in a future application of the presented formulation.

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