In this study, we developed
curcumin-loaded
lipid-core
nanocapsules (C-LNCs) in an attempt to improve the antiglioma activity of this
polyphenol. C-LNC showed nanotechnological properties such as nanometric mean size (196 nm), 100% encapsulation efficiency, polydispersity index below 0.1, and negative zeta potential. The in vitro release assays demonstrated a controlled release of
curcumin from
lipid-core
nanocapsules. In C6 and U251MG
gliomas, C-LNC promoted a biphasic delivery of
curcumin: the first peak occurred early in the treatment (1-3h), whereas the onset of the second phase occurred after 48 h. In C6 cells, the cytotoxicity of C-LNC was comparable to non-encapsulated
curcumin only after 96 h, whereas C-LNCs were more cytotoxic than non-encapsulated
curcumin after 24h of incubation in U251MG. Induction of G2/M arrest and autophagy were observed in C-LNC as well as in free-
curcumin treatments. In rats bearing C6
gliomas, C-LNC (1.5mg/kg/day, i.p.) decreased the
tumor size and malignance and prolonged animal survival when compared to same dose of non-encapsulated drug. In addition,
serum markers of tissue toxicity and histological parameters were not altered. Considered overall, the data suggest that the nanoencapsulation of
curcumin in LNC is an important strategy to improve its pharmacological efficacy in the treatment of
gliomas.