title: Curcumin-loaded lipid-core nanocapsules as a strategy to improve pharmacological efficacy of curcumin in glioma treatment.
abstract: 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.
authors.affiliation: Departamento de Bioquímica, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre, Rio Grande do Sul, Brazil.
authors.forename: Alfeu
authors.initials: A
authors.lastname: Zanotto-Filho
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre, Brazil.
authors.forename: Karine
authors.initials: K
authors.lastname: Coradini
authors.affiliation: Centro de Ciências Químicas, Farmacêuticas e de Alimentos, Universidade Federal de Pelotas (UFPel), Pelotas, Rio Grande do Sul, Brazil.
authors.forename: Elizandra
authors.initials: E
authors.lastname: Braganhol
authors.affiliation: Departamento de Bioquímica, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre, Rio Grande do Sul, Brazil.
authors.forename: Rafael
authors.initials: R
authors.lastname: Schröder
authors.affiliation: Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul (UFRGS),Porto Alegre,Brazil.
authors.forename: Cláudia Melo
authors.initials: CM
authors.lastname: de Oliveira
authors.affiliation: Departamento de Bioquímica, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre, Rio Grande do Sul, Brazil.
authors.forename: André
authors.initials: A
authors.lastname: Simões-Pires
authors.affiliation: Departamento de Bioquímica, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre, Rio Grande do Sul, Brazil.
authors.forename: Ana Maria Oliveira
authors.initials: AM
authors.lastname: Battastini
authors.affiliation: Departamento de Química Orgânica, Instituto de Química, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre, Rio Grande do Sul, Brazil.
authors.forename: Adriana Raffin
authors.initials: AR
authors.lastname: Pohlmann
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre, Brazil.
authors.forename: Sílvia Stanisçuaski
authors.initials: SS
authors.lastname: Guterres
authors.affiliation: Hospital São Vicente de Paulo, Faculdade de Medicina da Universidade de Passo Fundo (UPF), Passo Fundo, Rio Grande do Sul, Brazil.
authors.forename: Cassiano Mateus
authors.initials: CM
authors.lastname: Forcelini
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre, Brazil. Electronic address: ruy.beck@ufrgs.br.
authors.forename: Ruy Carlos Ruver
authors.initials: RC
authors.lastname: Beck
authors.affiliation: Departamento de Bioquímica, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre, Rio Grande do Sul, Brazil.
authors.forename: José Cláudio Fonseca
authors.initials: JC
authors.lastname: Moreira
mesh_terms: D000818:Animals; D001343:Autophagy / Q000187:drug effects; D045744:Cell Line, Tumor; D003474:Curcumin / Q000008:administration & dosage*; D059565:G2 Phase Cell Cycle Checkpoints / Q000187:drug effects; D005910:Glioma / Q000188:drug therapy*; D008055:Lipids / Q000008:administration & dosage*; D008297:Male; D053769:Nanocapsules / Q000008:administration & dosage*; D010316:Particle Size; D051381:Rats; D017208:Rats, Wistar
chemical_list: D008055:Lipids; D053769:Nanocapsules; D003474:Curcumin