title: Curcumin-loaded lipid and polymeric nanocapsules stabilized by nonionic surfactants: an in vitro and In vivo antitumor activity on B16-F10 melanoma and macrophage uptake comparative study.
abstract: Curcumin is a polyphenol obtained from the plant Curcuma longa (called turmeric) that displays several pharmacological activities, including anti-inflammatory, antioxidant, antimicrobial and antitumoral activity, but clinical use has been limited by its poor solubility in water and, consequently, minimal systemic bioavailability. We have therefore formulated the drug into nanocarrier systems in an attempt to improve its therapeutic properties. This study evaluates the effect of intraperitoneally administered nanocapsules containing curcumin on subcutaneous melanoma in mice inoculated with B16-F10 cells, and on the cytotoxicity activity against B16-F10 cells in vitro. Phagocytic uptake of formulations was also evaluated upon incubation with macrophage J774 cells by fluorescence microscopy. Lipid and polymeric nanocapsules were prepared by the phase inversion and nanoprecipitation methods, respectively. The uptake of the lipid nanocapsules prepared using Solutol HS15 was significantly reduced in J774 cells. Curcumin, as free drug or as drug-loaded nanocapsules, was administrated at a dose of 6 mg/kg twice a week for 21 days. Free drug and curcumin-loaded nanocapsules significantly reduced tumor volume (P < 0.05 vs. control), but no difference was found in the antitumor activity displayed by lipid and polymeric nanocapsules. This assumption was supported by the in vitro study, in which free curcumin as well as loaded into nanocapsules caused significant reduction of cell viability in a concentration- and time-dependent manner.
authors.affiliation: Departamento de Ciências Farmacêuticas, Centro de Ciências da Saúde, Universidade Federal de Santa Catarina, Campus Trindade, Florianópolis, 88040-970, Brazil.
authors.forename: Leticia
authors.initials: L
authors.lastname: Mazzarino
authors.forename: Luís F C
authors.initials: LF
authors.lastname: Silva
authors.forename: Juliana C
authors.initials: JC
authors.lastname: Curta
authors.forename: Marley A
authors.initials: MA
authors.lastname: Licínio
authors.forename: Aline
authors.initials: A
authors.lastname: Costa
authors.forename: Leticia K
authors.initials: LK
authors.lastname: Pacheco
authors.forename: Jarbas M
authors.initials: JM
authors.lastname: Siqueira
authors.forename: Jorge
authors.initials: J
authors.lastname: Montanari
authors.forename: Eder
authors.initials: E
authors.lastname: Romero
authors.forename: Jamil
authors.initials: J
authors.lastname: Assreuy
authors.forename: Maria C
authors.initials: MC
authors.lastname: Santos-Silva
authors.forename: Elenara
authors.initials: E
authors.lastname: Lemos-Senna
mesh_terms: D000818:Animals; D001692:Biological Transport / Q000187:drug effects; D045744:Cell Line, Tumor; D003474:Curcumin / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D004355:Drug Stability; D007477:Ions; D008081:Liposomes; D008264:Macrophages / Q000187:drug effects* / Q000276:immunology / Q000378:metabolism*; D008546:Melanoma, Experimental / Q000188:drug therapy; D051379:Mice; D008810:Mice, Inbred C57BL; D053769:Nanocapsules / Q000737:chemistry; D010316:Particle Size; D013501:Surface-Active Agents / Q000737:chemistry
chemical_list: D007477:Ions; D008081:Liposomes; D053769:Nanocapsules; D013501:Surface-Active Agents; D003474:Curcumin