Preparation and characterization of dithiocarbazate Schiff base–loaded poly(lactic acid) nanoparticles and analytical validation for drug quantification

Colloid and Polymer Science(2019)

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Abstract
Dithiocarbazate Schiff bases have been reported as a class of compounds that exhibit a wide range of pharmacological activities against neglected diseases such as malaria, trypanosomiasis, and tuberculosis. This work reports the encapsulation of the 1-(S-benzyldithiocarbazate)-3-methyl-5-phenyl-pyrazole (DTC) into biodegradable polymeric nanoparticles (NPs) of poly(lactic acid) (PLA) aiming potential drug delivery application. The DTC-loaded PLA-NPs were prepared by the single-nanoemulsification method using the poly(vinyl alcohol) (PVA) as a surfactant. The nanostructured system was characterized mainly by dynamic light scattering (DLS), electrophoretic light scattering (ELS), and transmission electron microscopy (TEM). The NPs show good colloidal stability exhibiting mean hydrodynamic diameter 157 ± 5 nm and zeta potential − 36 ± 3 mV. The encapsulation efficiency and drug loading were 52 ± 14% and 4.8 ± 1.5%, respectively. The quantifications of DTC and residual PVA in the NPs were performed by UV-Vis absorption spectroscopy. The analytical methods were validated according to regulatory agencies. Both quantification analytical curves showed good precision, in repeatability (intra-day) and intermediate (inter-day), and also good accuracy with low values of detection and quantification. The new nanostructured system, DTC-loaded PLA-NPs, shows advantages to improve stability and to overcome water solubility problems of the dithiocarbazate Schiff bases aiming potential drug delivery applications. Graphical abstract .
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Key words
Azomethine, Pyrazole, Emulsion polymerization, Nanostructured system, Colloidal system
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