title: Nanoencapsulation of usnic acid: An attempt to improve antitumour activity and reduce hepatotoxicity.
abstract: Despite the recognised antiproliferative and antitumour properties of usnic acid, its therapeutic application has yet to be introduced. In fact, the high hepatotoxicity and low water solubility of usnic acid have somewhat restricted its practical use in anticancer therapy. The aim of this study was therefore to investigate the antitumour activity of usnic acid encapsulated into nanocapsules prepared with lactic co-glycolic acid polymer. Usnic acid-loaded nanocapsules were obtained using the interfacial deposition of a preformed polymer. The antitumour activity was confirmed on an ascitic tumour (Sarcoma-180) implanted in Swiss mice and estimated by means of the tumour inhibition. The results of antitumour activity confirmed that the encapsulation of usnic acid into PLGA-nanocapsules produced a 26.4% increase in tumour inhibition as compared with the standard free usnic acid treatment. Vacuolization of hepatocytes and a mild lymphocytic infiltration in portal spaces were observed in animals treated with free usnic acid. However, this hepatotoxicity was substantially reduced when animals were treated with usnic acid-loaded nanocapsules. No histological changes were noticed in the kidneys or spleen of animals treated either with usnic acid or usnic acid-loaded nanocapsules. These results suggest that nanoencapsulation may be a way of enabling usnic acid to be used in chemotherapy.
authors.affiliation: Universidade Federal de Pernambuco (UFPE), Laboratório de Imunopatologia Keizo-Asami, Brazil.
authors.forename: Noemia Pereira
authors.initials: NP
authors.lastname: da Silva Santos
authors.forename: Silene Carneiro
authors.initials: SC
authors.lastname: Nascimento
authors.forename: Marcela Silvestre Outtes
authors.initials: MS
authors.lastname: Wanderley
authors.forename: Nicodemos Teles
authors.initials: NT
authors.lastname: Pontes-Filho
authors.forename: José Figueiredo
authors.initials: JF
authors.lastname: da Silva
authors.forename: Célia Maria Machado Barbosa
authors.initials: CM
authors.lastname: de Castro
authors.forename: Eugênia Cristina
authors.initials: EC
authors.lastname: Pereira
authors.forename: Nicácio Henrique
authors.initials: NH
authors.lastname: da Silva
authors.forename: Neli Kika
authors.initials: NK
authors.lastname: Honda
authors.forename: Nereide Stela
authors.initials: NS
authors.lastname: Santos-Magalhães
mesh_terms: D000818:Animals; D001572:Benzofurans / Q000008:administration & dosage / Q000627:therapeutic use* / Q000633:toxicity; D045744:Cell Line, Tumor; D056486:Chemical and Drug Induced Liver Injury / Q000097:blood / Q000209:etiology / Q000517:prevention & control*; D018450:Disease Progression; D004339:Drug Compounding / Q000379:methods*; D007274:Injections, Intraperitoneal; D019344:Lactic Acid / Q000737:chemistry; D008099:Liver / Q000187:drug effects / Q000473:pathology; D008297:Male; D051379:Mice; D049329:Nanostructures / Q000737:chemistry*; D011100:Polyglycolic Acid / Q000737:chemistry; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers / Q000737:chemistry; D012510:Sarcoma 180 / Q000188:drug therapy*; D016019:Survival Analysis
chemical_list: D001572:Benzofurans; D011108:Polymers; C073339:usnic acid; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid