title: Drug delivery by polymeric micelles: an in vitro and in vivo study to deliver lipophilic substances to colonocytes and selectively target inflamed colon.
abstract: Colitis is the term used for chronic inflammatory bowel diseases at substantially increased risk of developing a form of colorectal cancer (CRC) known as colitis-associated cancer. In our study we synthesized core-shell polymeric micelles obtained by self-assembly of block copolymers for high efficiency delivery of anti-inflammatory and anti-cancer compounds to colonocytes and colon mucosa. We achieved an efficient intracellular delivery of these hydrophobic compounds (prednisone, retinoic acid and doxorubicin) to cultured colonocytes without cellular toxicity. The efficacy of retinoic acid and doxorubicin administration was significantly increased using these nanosized carriers. Moreover, these polymeric micelles have been shown to overcome the multidrug resistance efflux mechanism effectively delivering doxorubicin to multidrug-resistant colon cancer cells. These nanocarriers are also suitable for selective in vivo delivery of lipophilic drugs by enema administration to the inflamed colon tissue, specifically targeting the inflamed mucosa.
  
  
  BACKGROUND
  This team of investigators studied polymeric micelles as highly efficient drug delivery systems enabling intracellular delivery of hydrophobic compounds (prednisone, retinoic acid, and doxorubicin) to cultured colonocytes without cellular toxicity, also demonstrating beneficial in vivo effects.
authors.affiliation: Department of Clinical Medicine, University of Bologna, Bologna, Italy.
authors.forename: Maria Chiara
authors.initials: MC
authors.lastname: Valerii
authors.forename: Massimo
authors.initials: M
authors.lastname: Benaglia
authors.forename: Cinzia
authors.initials: C
authors.lastname: Caggiano
authors.forename: Alessio
authors.initials: A
authors.lastname: Papi
authors.forename: Antonio
authors.initials: A
authors.lastname: Strillacci
authors.forename: Giorgia
authors.initials: G
authors.lastname: Lazzarini
authors.forename: Massimo
authors.initials: M
authors.lastname: Campieri
authors.forename: Paolo
authors.initials: P
authors.lastname: Gionchetti
authors.forename: Fernando
authors.initials: F
authors.lastname: Rizzello
authors.forename: Enzo
authors.initials: E
authors.lastname: Spisni
mesh_terms: D000818:Animals; D003092:Colitis / Q000150:complications / Q000188:drug therapy* / Q000473:pathology; D003106:Colon / Q000166:cytology / Q000187:drug effects*; D003110:Colonic Neoplasms / Q000150:complications / Q000188:drug therapy* / Q000473:pathology; D004317:Doxorubicin / Q000008:administration & dosage; D016503:Drug Delivery Systems; D018432:Drug Resistance, Multiple / Q000187:drug effects; D006801:Humans; D051379:Mice; D008823:Micelles; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry; D011108:Polymers / Q000008:administration & dosage* / Q000737:chemistry; D011241:Prednisone / Q000008:administration & dosage; D014212:Tretinoin / Q000008:administration & dosage
chemical_list: D008823:Micelles; D011108:Polymers; D014212:Tretinoin; D004317:Doxorubicin; D011241:Prednisone