Artemether-loaded polymeric lipid-core nanocapsules reduce cell viability and alter the antioxidant status of U-87 MG cells

Abstract

Glioblastomas are tumors that present a high mortality rate. Artemether (ART) is a lactone with antitumor properties, demonstrating low bioavailability and water solubility. In the present study, we developed lipid-core nanocapsules (LNC) containing pequi oil (Caryocar brasiliense Cambess) as the oily core for ART-loaded LNCs (LNC_ART) and evaluated their effect on human glioblastoma cells (U-87 MG). LNCs were developed by interfacial deposition of a preformed polymer, followed by physicochemical characterization. LNC_ART revealed a diameter of 0.216 µm, polydispersity index of 0.161, zeta potential of −12.0 mV, and a pH of 5.53. Furthermore, mitochondrial viability, proliferation, total antioxidant status, and antioxidant enzyme activity were evaluated. ART reduced cell viability after 24 h and proliferation after 48 h of treatment at concentrations equal to or above 40 µg . mL⁻¹. LNC_ART, at 1.25 µg . mL⁻¹, reduced these parameters after 24 h of treatment. Furthermore, superoxide dismutase (SOD) activity was elevated, while glutathione reductase (GR) activity was reduced. These findings suggest that ART loaded into LNC may be a promising alternative to improve its pharmacological action and possible application as a therapeutic agent for glioblastoma.

Graphical Abstract

Keywords:

• Polymeric lipid-core nanocapsules
• Caryocar brasiliense Cambess
• artemether
• human glioblastoma
• cell viability
• antioxidant status

Acknowledgments

The authors thank Prof. Thais Leite Nascimento for her comments and review of the manuscript.

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This work was financed in part by Cordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES), J.P. received a CAPES Fellow (Bolsa de Mestrado); Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq); Universidade Federal de Mato Grosso (UFMT); and Fundação de Amparo à Pesquisa do Estado de Mato Grosso (FAPEMAT).