title: Multicompartimental nanoparticles for co-encapsulation and multimodal drug delivery to tumor cells and neovasculature.
abstract: OBJECTIVE
  The purpose of this work was the development of a multicompartimental nanocarrier for the simultaneous encapsulation of paclitaxel (PTX) and genistein (GEN), associating antiangiogenic and cytotoxic properties in order to potentiate antitumoral activity.
  
  
  METHODS
  Polymeric nanocapsules containing PTX were obtained by interfacial deposition of preformed polymer and coated with a phospholipid bilayer entrapping GEN. Physical-chemical and morphological characteristics were characterized, including size and size distribution, drug entrapment efficiency and drug release profile. In vivo studies were performed in EAT bearing Swiss mice.
  
  
  RESULTS
  Entrapment efficiency for both drugs in the nanoparticles was approximately 98%. Average particle diameter was 150 nm with a monomodal distribution. In vitro assays showed distinct temporal drug release profiles for each drug. The dose of 0.2 mg/kg/day of PTX resulted in 11% tumor inhibition, however the association of 12 mg/kg/day of GEN promoted 44% tumor inhibition and a 58% decrease in VEGF levels.
  
  
  CONCLUSIONS
  Nanoparticles containing GEN and PTX with a temporal pattern of drug release indicated that the combined effect of cytotoxic and antiangiogenic drugs present in the formulation contributed to the overall enhanced antitumor activity of the nanomedicine.
authors.affiliation: Laboratório de Nanotecnologia Farmacêutica e Sistemas de Liberação de Fármacos-FarmaTec, Faculdade de Farmácia, Universidade Federal de Goiás, Goiânia, GO, Brazil.
authors.forename: Lívia Palmerston
authors.initials: LP
authors.lastname: Mendes
authors.forename: Marilisa Pedroso Nogueira
authors.initials: MP
authors.lastname: Gaeti
authors.forename: Paulo Henrique Marcelino
authors.initials: PH
authors.lastname: de Ávila
authors.forename: Marcelo
authors.initials: M
authors.lastname: de Sousa Vieira
authors.forename: Bruna
authors.initials: B
authors.lastname: Dos Santos Rodrigues
authors.forename: Renato Ivan
authors.initials: RI
authors.lastname: de Ávila Marcelino
authors.forename: Lílian Cristina Rosa
authors.initials: LC
authors.lastname: Dos Santos
authors.forename: Marize Campos
authors.initials: MC
authors.lastname: Valadares
authors.forename: Eliana Martins
authors.initials: EM
authors.lastname: Lima
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000627:therapeutic use*; D001808:Blood Vessels / Q000378:metabolism*; D002851:Chromatography, High Pressure Liquid; D016503:Drug Delivery Systems; D019833:Genistein / Q000008:administration & dosage / Q000627:therapeutic use; D008297:Male; D051379:Mice; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles; D009374:Neoplasms, Experimental / Q000188:drug therapy* / Q000473:pathology; D017239:Paclitaxel / Q000008:administration & dosage / Q000627:therapeutic use
chemical_list: D000970:Antineoplastic Agents; D019833:Genistein; D017239:Paclitaxel