Curcumin-loaded lipid-core nanocapsules as a strategy to improve pharmacological efficacy of curcumin in glioma treatment

• Published in: European journal of pharmaceutics and biopharmaceutics 2013-02, Vol.83 (2), p.156-167
• Main Authors: Zanotto-Filho, Alfeu, Coradini, Karine, Braganhol, Elizandra, Schröder, Rafael, de Oliveira, Cláudia Melo, Simões-Pires, André, Battastini, Ana Maria Oliveira, Pohlmann, Adriana Raffin, Guterres, Sílvia Stanisçuaski, Forcelini, Cassiano Mateus, Beck, Ruy Carlos Ruver, Moreira, José Cláudio Fonseca
• Format: Article
• Language: English
• Subjects: Animals; Autophagy - drug effects; Cell Line, Tumor; Curcumin; Curcumin - administration & dosage; Drug delivery; G2 Phase Cell Cycle Checkpoints - drug effects; Glioma; Glioma - drug therapy; In vivo; Lipid-core nanocapsules; Lipids - administration & dosage; Male; Nanocapsules - administration & dosage; Particle Size; Rats; Rats, Wistar
• ISSN: 0939-6411; 1873-3441
• DOI: 10.1016/j.ejpb.2012.10.019

Curcumin-loaded lipid-core nanocapsules reduce tumor size in animal model of glioma. 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 (196nm), 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 48h. In C6 cells, the cytotoxicity of C-LNC was comparable to non-encapsulated curcumin only after 96h, 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.