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

Made available in DSpace on 2022-04-29T08:38:47Z (GMT). No. of bitstreams: 0 Previous issue date: 2022-01-01 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. Department of Biological Sciences and Health University of Araraquara (UNIARA) Department of Drugs and Medicines School of Pharmaceutical Sciences São Paulo State University (UNESP) Nanobiotechnology Laboratory Institute of Biological Sciences Department of Genetics and Morphology University of Brasilia Department of Biological Sciences School of Pharmaceutical Sciences São Paulo State University (UNESP) Facultad de Ciencias Exactas Departmento de Química CINDEFI Laboratorio de Nanobiomateriales Universidad Nacional de La Plata–CONICET (CCT La Plata) Max Planck Laboratory for Structural Biology Chemistry and Molecular Biophysics of Rosario (MPLbioR UNR-MPIbpC) Partner Laboratory of the Max Planck Institute for Biophysical Chemistry (MPIbpC MPG) Universidad Nacional de Rosario Centro de Estudios Interdisciplinarios (CEI) Laboratorio de Química Fina (UNL-CONICET) Universidad Nacional del Litoral (UNL) INTEC Department of Drugs and Medicines School of Pharmaceutical Sciences São Paulo State University (UNESP) Department of Biological Sciences School of Pharmaceutical Sciences São Paulo State University (UNESP)