Study of antimycobacterial, cytotoxic, and mutagenic potential of polymeric nanoparticles of copper (II) complex

Abstract

This study aimed to encapsulate and characterise a potential anti-tuberculosis copper complex (CuCl₂(INH)₂.H₂O:I1) into polymeric nanoparticles (PNs) of polymethacrylate copolymers (Eudragit®, Eu) developed by nanoprecipitation method. NE30D, S100 and, E100 polymers were tested. The physicochemical characterisations were performed by DLS, TEM, FTIR, encapsulation efficiency and, in vitro release studies. Encapsulation of I1 in PN-NE30D, PN-E100, and PN-S100 was 26.3%, 94.5%, 22.6%, respectively. The particle size and zeta potentials were 82.3 nm and −24.5 mV for PNs-NE30D, 304.4 nm and +18.7 mV for PNs-E100, and 517.9 nm and −6.9 mV for PNs-S100, respectively. All PDIs were under 0.5. The formulations showed an I1 controlled release at alkaline pH with 29.7% from PNs-NE30D, 7.9% from PNs-E100 and, 28.1% from PNs-S100 at 1 h incubation. PNs were stable for at least 3 months. Particularly, PNs-NE30D demonstrated moderate inhibition of M. tuberculosis and low cytotoxic activity. None of the PNs induced mutagenicity.

Keywords:

• Copper(II) complexes
• mutagenicity
• resazurin assay
• polymeric matrices
• Eudragit®

Disclosure statement

The authors declare no conflict of interest.

Additional information

Funding

This work was supported by “Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP n° 2017/16278–9 and 2013/09265–7)” and “Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)”, Brazilian state and federal agencies and by Universidad Nacional de La Plata (Grant X701, Subsidio Jóvenes Investigadores 2017) and Agencia Nacional de Promoción Científica y Técnica (ANPCyT, PICT2016-4597, PICT2017-2251) of Argentina to GRC and GAI. Also, we appreciate the donation of Eudragit^® samples to Etilfarma^® (Buenos Aires, Argentina).