title: Antitumoral activity and toxicity of PEG-coated and PEG-folate-coated pH-sensitive liposomes containing ¹⁵⁹Gd-DTPA-BMA in Ehrlich tumor bearing mice.
abstract: In the present study, PEG-coated pH-sensitive and PEG-folate-coated pH-sensitive liposomes containing the ¹⁵⁹Gd-DTPA-BMA were prepared and radiolabeled through neutron activation technique, aiming to study the in vivo antitumoral activity and toxicity on mice bearing a previously-developed solid Ehrlich tumor. The treatment efficacy was verified through tumoral volume increase and histomorphometry studies. The toxicity of formulations was investigated through animal weight variations, as well as hematological and biochemical tests. The results showed that after 31 days of treatment, animals treated with radioactive formulations had a lower increase in tumor volume and a significantly higher percentage of necrosis compared with controls revealed by histomorphometry studies. Furthermore, mice treated with radioactive formulations exhibited lower weight gain without significant hematological or biochemical changes, except for toxicity to hepatocytes which requires more detailed studies. From the results obtained to date, we believe that the radioactive formulations can be considered potential therapeutic agents for cancer.
authors.affiliation: Universidade Federal de Minas Gerais - Avenida Presidente Antônio Carlos, 6627 - Pampulha - 31270-901 - Belo Horizonte, Minas Gerais, Brazil.
authors.forename: Daniel Crístian Ferreira
authors.initials: DC
authors.lastname: Soares
authors.forename: Valbert Nascimento
authors.initials: VN
authors.lastname: Cardoso
authors.forename: André Luís Branco
authors.initials: AL
authors.lastname: de Barros
authors.forename: Cristina Maria
authors.initials: CM
authors.lastname: de Souza
authors.forename: Geovanni Dantas
authors.initials: GD
authors.lastname: Cassali
authors.forename: Mônica Cristina
authors.initials: MC
authors.lastname: de Oliveira
authors.forename: Gilson Andrade
authors.initials: GA
authors.lastname: Ramaldes
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000009:adverse effects / Q000627:therapeutic use; D002286:Carcinoma, Ehrlich Tumor / Q000473:pathology / Q000532:radiotherapy*; D056486:Chemical and Drug Induced Liver Injury / Q000473:pathology / Q000503:physiopathology; D016503:Drug Delivery Systems / Q000009:adverse effects; D005260:Female; D005492:Folic Acid / Q000031:analogs & derivatives* / Q000737:chemistry; D005682:Gadolinium; D019786:Gadolinium DTPA / Q000008:administration & dosage* / Q000009:adverse effects / Q000627:therapeutic use; D006863:Hydrogen-Ion Concentration; D007928:Lethal Dose 50; D008081:Liposomes; D008099:Liver / Q000473:pathology / Q000503:physiopathology / Q000528:radiation effects; D051379:Mice; D009336:Necrosis; D011092:Polyethylene Glycols / Q000737:chemistry*; D011868:Radioisotopes; D019275:Radiopharmaceuticals / Q000008:administration & dosage* / Q000009:adverse effects / Q000627:therapeutic use; D013499:Surface Properties; D047368:Tumor Burden / Q000528:radiation effects; D015430:Weight Gain / Q000528:radiation effects
chemical_list: D000970:Antineoplastic Agents; D008081:Liposomes; D011868:Radioisotopes; D019275:Radiopharmaceuticals; C552831:poly(ethylene glycol)-folate; D011092:Polyethylene Glycols; C064925:gadodiamide; D005492:Folic Acid; D005682:Gadolinium; D019786:Gadolinium DTPA