Desenvolvimento de nanopartículas lipídicas sólidas de palmitoestearato de glicerila contendo beta-cariofileno para o potencial uso no tratamento de Glioblastoma.

Abstract

Glioblastoma (GB) is the most aggressive glioma and is difficult to treat, considering its location and pathophysiology. In this context, nanotechnology proves to be a strategy to carry pharmaceutically active ingredients (APIs) in order to overcome the limitations imposed by the blood–brain barrier, delivering such APIs to the cancer target site, thus contributing to the therapy of malignant brain neoplasms. Given this, this monograph developed the production of Solid Lipid Nanoparticles (SLNs), based on glyceryl palmitostearate and capable of carrying β-caryophyllene (BCP), a terpene that interacts with CB2 receptors, widely present in glial cells, could act on critical glioblastoma processes such as proliferation, differentiation, and cell survival. Therefore, BCP-loaded SLNs would mitigate disease progression or could act as treatment and/or combination therapy with antineoplastic agents. The general objective was to produce SLNs of glyceryl palmitostearate containing BCP aiming at biopharmaceutical applicability, especially antioxidant, anticancer, and neuroprotective. For this, different production methods were evaluated (solvent evaporation, phase inversion by composition, and melt-emulsification), in addition to the influence of variation in formulation components (lipid concentration, surfactant, and types of co-solvent), standardization studies (temperature and time), as well as physicochemical characterization assays, preliminary stability, and in vitro antioxidant activity (DPPH radical scavenging method). The results demonstrated that the developed particles showed a drug loading capacity of 5.3%, stability during the studied period (6 weeks), and antioxidant potential with 98% DPPH scavenging, indicating a promising nanosystem for the treatment of brain cancers.