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

Pharm Dev Technol. 2022 Oct;27(8):892-903. doi: 10.1080/10837450.2022.2128819. Epub 2022 Oct 3.

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 (LNCART) 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. LNCART 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. LNCART, 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.

Keywords: Caryocar brasiliense Cambess; Polymeric lipid-core nanocapsules; antioxidant status; artemether; cell viability; human glioblastoma.

MeSH terms

  • Antioxidants / pharmacology
  • Artemether
  • Cell Survival
  • Glioblastoma* / drug therapy
  • Humans
  • Lipids / chemistry
  • Nanocapsules* / chemistry
  • Polymers

Substances

  • Nanocapsules
  • Antioxidants
  • Artemether
  • Lipids
  • Polymers