Increased in vitro leishmanicidal activity of octyl gallate loaded poly(methyl methacrylate) nanoparticles

Abstract

The current paucity of effective and affordable drugs for the treatment of leishmaniasis renders the search for new therapeutic alternatives a priority. Gallic acid-related compounds display anti-parasitic activities and their incorporation into drug carrier systems, such as polymeric nanoparticles may be a viable alternative for leishmaniasis treatment. Therefore, this study focused on the synthesis and characterization of octyl gallate (G8) loaded poly(methyl methacrylate) (PMMA) nanoparticles via miniemulsion polymerization in order to increase the leishmanicidal activity of this compound. G8 loaded PMMA nanoparticles presented a spherical morphology with a mean size of 108 nm, a negatively charged surface (−33 ± 5 mV) and high encapsulation efficiency (83% ± 5). Fourier-transform infrared spectroscopy and X-ray diffraction analysis confirmed that G8 was encapsulated in PMMA nanoparticles and presented a biphasic release profile. The G8 loaded PMMA nanoparticles did not present cytotoxic effect on human red blood cells. G8 loaded PMMA nanoparticles displayed a leishmanicidal activity almost three times higher than free G8 while the cytotoxic activity against human THP-1 cells remained unchanged.

Graphical Abstract

Keywords:

• Octyl gallate
• Leishmania amazonensis
• miniemulsion polymerization
• polymeric nanoparticles
• poly(methyl methacrylate)

Acknowledgements

The authors thank the financial support from CNPq (Conselho Nacional de Desenvolvimento Científico e Tecnológico), CAPES (Coordenação de Aperfeiçoamento de Pessoal de Nível Superior) and TEM analysis from Laboratório Central de Microscopia Eletrônica of Federal University of Santa Catarina (LCME/UFSC).

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This work was supported by CNPq (Conselho Nacional de Desenvolvimento Científico e Tecnológico) and CAPES (Coordenação de Aperfeiçoamento de Pessoal de Nível Superior).