title: Lipid-Core Nanocapsules Improved Antiedematogenic Activity of Tacrolimus in Adjuvant-Induced Arthritis Model.
abstract: Despite significant technological advances, rheumatoid arthritis remains an incurable disease with great impact on the life quality of patients. We studied the encapsulation of tacrolimus in lipidcore nanocapsules (TAC-LNC) as a strategy to enhance its systemic anti-arthritic properties. TAC-LNC presented unimodal distribution of particles with z-average diameter of 212 +/- 11, drug content close to the theoretical value (0.80 mg mL(-1)), and 99.43% of encapsulation efficiency. An in vitro sustained release was determined for TAC-LNC with anomalous transport mechanism (n = 0.61). In vivo studies using an arthritis model induced by Complete Freund's Adjuvant demonstrated that the animals treated with TAC-LNC presented a significantly greater inhibition of paw oedema after intraperitoneal administration. Furthermore, the encapsulation of TAC in lipid-core nanocapsules was potentially able to prevent hyperglycemia in the animals. In conclusion, TAC-LNC was prepared with 100% yield of nanoscopic particles having satisfactory characteristics for systemic use. This formulation represents a promising strategy to the treatment of rheumatoid arthritis in the near future.
authors.forename: Rossana B
authors.initials: RB
authors.lastname: Friedrich
authors.forename: Karine
authors.initials: K
authors.lastname: Coradini
authors.forename: Francisco N
authors.initials: FN
authors.lastname: Fonseca
authors.forename: Silvia S
authors.initials: SS
authors.lastname: Guterres
authors.forename: Ruy C R
authors.initials: RC
authors.lastname: Beck
authors.forename: Adriana R
authors.initials: AR
authors.lastname: Pohlmann
mesh_terms: D000818:Animals; D001169:Arthritis, Experimental / Q000139:chemically induced / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D007166:Immunosuppressive Agents / Q000737:chemistry / Q000494:pharmacology; D008055:Lipids / Q000737:chemistry / Q000494:pharmacology; D008297:Male; D053769:Nanocapsules / Q000737:chemistry*; D010316:Particle Size; D051381:Rats; D017208:Rats, Wistar; D016559:Tacrolimus / Q000737:chemistry / Q000494:pharmacology
chemical_list: D007166:Immunosuppressive Agents; D008055:Lipids; D053769:Nanocapsules; D016559:Tacrolimus