title: Efficacy of DOPE/DC-cholesterol liposomes and GCPQ micelles as AZD6244 nanocarriers in a 3D colorectal cancer in vitro model.
abstract: OBJECTIVE
  In this work, we use cationic organic nanocarriers as chemotherapy delivery platforms and test them in a colorectal cancer 3D in vitro model.
  
  
  METHODS
  We used 3beta-(N-[N',N'-dimethylaminoethane]carbamoyl])cholesterol (DC-chol) and dioleoylphosphatidylethanolamine (DOPE) liposomes and N-palmitoyl-N-monomethyl-N,N-dimethyl-N,N,N-trimethyl-6-O-glycolchitosan (GCPQ) micelles, to deliver AZD6244, a MEK inhibitor, to HCT116 cells cultured as monolayers and in 3D in vitro cancer models (tumoroids).
  
  
  RESULTS
  Nanoparticle-mediated drug delivery was superior to the free drug in monolayer experiments and despite their therapeutic effect being hindered by poor diffusion through the cancer mass, GCPQ micelles were also superior in tumoroids.
  
  
  CONCLUSIONS
  These results support the role of nanoparticles in improving drug delivery and highlight the need to include 3D cancer models in early phases of drug development.
authors.affiliation: Cancer Nanotechnology Group, University College London, Division of Surgery & Interventional Science, Royal Free Campus, London, NW3 2PF, UK.
authors.forename: Víctor
authors.initials: V
authors.lastname: López-Dávila
authors.affiliation: Cancer Nanotechnology Group, University College London, Division of Surgery & Interventional Science, Royal Free Campus, London, NW3 2PF, UK.|Institute of Orthopaedics & Musculoskeletal Sciences, University College London, Division of Surgery & Interventional Science, Stanmore Campus, HA7 4LP, UK.
authors.forename: Tarig
authors.initials: T
authors.lastname: Magdeldin
authors.affiliation: Cancer Nanotechnology Group, University College London, Division of Surgery & Interventional Science, Royal Free Campus, London, NW3 2PF, UK.
authors.forename: Hazel
authors.initials: H
authors.lastname: Welch
authors.affiliation: Department of Biomedical Sciences, Faculty of Science & Technology, University of Westminster, 115 New Cavendish Street, London, W1W 6UW, UK.
authors.forename: Miriam Victoria
authors.initials: MV
authors.lastname: Dwek
authors.affiliation: School of Pharmacy, University College London, 29-39 Brunswick Square, London, WC1N 1AX, UK.
authors.forename: Ijeoma
authors.initials: I
authors.lastname: Uchegbu
authors.affiliation: Cancer Nanotechnology Group, University College London, Division of Surgery & Interventional Science, Royal Free Campus, London, NW3 2PF, UK.
authors.forename: Marilena
authors.initials: M
authors.lastname: Loizidou
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage*; D001562:Benzimidazoles / Q000008:administration & dosage*; D002784:Cholesterol / Q000008:administration & dosage*; D015179:Colorectal Neoplasms / Q000188:drug therapy* / Q000473:pathology; D004337:Drug Carriers; D006801:Humans; D066298:In Vitro Techniques; D008081:Liposomes; D008823:Micelles
chemical_list: C517975:AZD 6244; D000970:Antineoplastic Agents; D001562:Benzimidazoles; D004337:Drug Carriers; D008081:Liposomes; D008823:Micelles; D002784:Cholesterol
keywords: 3D culture; AZD6244; artificial cancer mass; chemotherapy; colorectal cancer; drug delivery; liposomes; micelles; tumoroids