title: Bromelain-Functionalized Multiple-Wall Lipid-Core Nanocapsules: Formulation, Chemical Structure and Antiproliferative Effect Against Human Breast Cancer Cells (MCF-7).
abstract: This study was conducted a promising approach to surface functionalization developed for lipid-core nanocapsules and the merit to pursue new strategies to treat solid tumors.
  
  
  
  Bromelain-functionalized multiple-wall lipid-core nanocapsules (Bro-MLNC-Zn) were produced by self-assembling following three steps of interfacial reactions. Physicochemical and structural characteristics, in vitro proteolytic activity (casein substrate) and antiproliferative activity (breast cancer cells, MCF-7) were determined.
  
  
  
  Bro-MLNC-Zn had z-average diameter of 135 nm and zeta potential of +23 mV. The complex is formed by a Zn-N chemical bond and a chelate with hydroxyl and carboxyl groups. Bromelain complexed at the nanocapsule surface maintained its proteolytic activity and showed anti-proliferative effect against human breast cancer cells (MCF-7) (72.6 ± 1.2% at 1.250 μg mL-1and 65.5 ± 5.5% at 0.625 μg mL-1). Comparing Bro-MLNC-Zn and bromelain solution, the former needed a dose 160-folds lower than the latter for a similar effect. Tripan blue dye assay corroborated the results.
  
  
  
  The surface functionalization approach produced an innovative formulation having a much higher anti-proliferative effect than the bromelain solution, even though both in vitro proteolytic activity were similar, opening up a great opportunity for further studies in nanomedicine.
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga, 2752, Porto Alegre, 90610-000, RS, Brazil. catipadilha@yahoo.com.br.|Departamento de Química Orgânica, Instituto de Química, Universidade Federal do Rio Grande do Sul, Porto Alegre, 91501-970, RS, Brazil. catipadilha@yahoo.com.br.
authors.forename: Catiúscia P
authors.initials: CP
authors.lastname: Oliveira
authors.affiliation: Programa de Pós-Graduação em Química, Instituto de Química, Universidade Federal do Rio Grande do Sul, Av. Bento Gonçalves, 9500, Porto Alegre, 91501-970, RS, Brazil.
authors.forename: Willian A
authors.initials: WA
authors.lastname: Prado
authors.affiliation: Programa de Pós-Graduação em Química, Instituto de Química, Universidade Federal do Rio Grande do Sul, Av. Bento Gonçalves, 9500, Porto Alegre, 91501-970, RS, Brazil.
authors.forename: Vladimir
authors.initials: V
authors.lastname: Lavayen
authors.affiliation: Programa de Pós-Graduação em Química, Instituto de Química, Universidade Federal do Rio Grande do Sul, Av. Bento Gonçalves, 9500, Porto Alegre, 91501-970, RS, Brazil.
authors.forename: Sabrina L
authors.initials: SL
authors.lastname: Büttenbender
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga, 2752, Porto Alegre, 90610-000, RS, Brazil.
authors.forename: Aline
authors.initials: A
authors.lastname: Beckenkamp
authors.affiliation: Programa de Pós-Graduação em Química, Instituto de Química, Universidade Federal do Rio Grande do Sul, Av. Bento Gonçalves, 9500, Porto Alegre, 91501-970, RS, Brazil.
authors.forename: Bruna S
authors.initials: BS
authors.lastname: Martins
authors.affiliation: Programa de Pós-Graduação em Química, Instituto de Química, Universidade Federal do Rio Grande do Sul, Av. Bento Gonçalves, 9500, Porto Alegre, 91501-970, RS, Brazil.
authors.forename: Diogo S
authors.initials: DS
authors.lastname: Lüdtke
authors.affiliation: Programa de Pós-Graduação em Química, Instituto de Química, Universidade Federal do Rio Grande do Sul, Av. Bento Gonçalves, 9500, Porto Alegre, 91501-970, RS, Brazil.
authors.forename: Leandra F
authors.initials: LF
authors.lastname: Campo
authors.affiliation: Programa de Pós-Graduação em Química, Instituto de Química, Universidade Federal do Rio Grande do Sul, Av. Bento Gonçalves, 9500, Porto Alegre, 91501-970, RS, Brazil.
authors.forename: Fabiano S
authors.initials: FS
authors.lastname: Rodembusch
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga, 2752, Porto Alegre, 90610-000, RS, Brazil.
authors.forename: Andréia
authors.initials: A
authors.lastname: Buffon
authors.affiliation: Faculdade de Ciências Farmacêuticas, Universidade de São Paulo, Av. Prof. Lineu Prestes, 580, São Paulo, 05434-070, SP, Brazil.
authors.forename: Adalberto
authors.initials: A
authors.lastname: Pessoa
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga, 2752, Porto Alegre, 90610-000, RS, Brazil.
authors.forename: Silvia S
authors.initials: SS
authors.lastname: Guterres
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga, 2752, Porto Alegre, 90610-000, RS, Brazil. adriana.pohlmann@ufrgs.br.|Departamento de Química Orgânica, Instituto de Química, Universidade Federal do Rio Grande do Sul, Porto Alegre, 91501-970, RS, Brazil. adriana.pohlmann@ufrgs.br.|Programa de Pós-Graduação em Química, Instituto de Química, Universidade Federal do Rio Grande do Sul, Av. Bento Gonçalves, 9500, Porto Alegre, 91501-970, RS, Brazil. adriana.pohlmann@ufrgs.br.
authors.forename: Adriana R
authors.initials: AR
authors.lastname: Pohlmann
mesh_terms: D001943:Breast Neoplasms / Q000188:drug therapy*; D001963:Bromelains / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004337:Drug Carriers / Q000737:chemistry; D005260:Female; D006801:Humans; D008055:Lipids / Q000737:chemistry*; D061986:MCF-7 Cells; D053769:Nanocapsules / Q000737:chemistry*; D050997:Nanomedicine / Q000379:methods; D010316:Particle Size
chemical_list: D004337:Drug Carriers; D008055:Lipids; D053769:Nanocapsules; D001963:Bromelains
keywords: MCF-7 human breast cancer cells; bromelain; lipid-core nanocapsules; metal-chitosan complex; surface-functionalized nanoparticles