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

• Published in: Colloid and polymer science Vol. 297; no. 11-12; pp. 1465 - 1475
• Main Authors: de Menezes, Thacilla Ingrid, de Oliveira Costa, Rebeca, Sanches, Rute Nazaré Fernandes, de Oliveira Silva, Denise, Santos, Rodrigo Luis Silva Ribeiro
• Format: Journal Article
• Language: English
• Published: Berlin/Heidelberg Springer Berlin Heidelberg 01-12-2019; Springer Nature B.V
• Subjects: Biodegradability; Characterization and Evaluation of Materials; Chemistry; Chemistry and Materials Science; Complex Fluids and Microfluidics; Drug delivery systems; Encapsulation; Food Science; Imines; Malaria; Mathematical analysis; Nanoparticles; Nanostructure; Nanotechnology and Microengineering; Original Contribution; Photon correlation spectroscopy; Physical Chemistry; Polylactic acid; Polymer Sciences; Polyvinyl alcohol; Pyrazole; Regulatory agencies; Scattering; Soft and Granular Matter; Stability; Tuberculosis; Zeta potential; Nanostructured system; Colloidal system; Emulsion polymerization; Pyrazole; Azomethine
• ISSN: 0303-402X; 1435-1536
• DOI: 10.1007/s00396-019-04572-9

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.
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