title: Design, synthesis and evaluation of biotin decorated inulin-based polymeric micelles as long-circulating nanocarriers for targeted drug delivery.
abstract: Here, long-circulating behaviors of Inulin-based nanomicelles are demonstrated for the first time in vivo. We show the synthesis and evaluation of biotin (BIO)-decorated polymeric INVITE micelles constituted of substances of natural origin, Inulin (INU) and Vitamin E (VITE), as long-circulating carriers for receptor-mediated targeted drug delivery. The resulting INVITE or INVITE-BIO micelles, nanometrically sized, did not reveal any cytotoxicity after 24h of incubation with Caco-2 cells. Moreover, in vitro studies on Caco-2 cells monolayers indicated that the transport of INVITE-BIO micelles was faster than surface unmodified INVITE micelles. In vivo optical imaging studies evidenced that, upon intravenous administration, INVITE-BIO micelles were quantitatively present in the body up to 48h. Instead, after oral administration, the micelles were not found in the systemic circulation but eliminated with the normal intestinal content. In conclusion, INVITE-BIO micelles may enhance drug accumulation in tumor-cells over-expressing the receptor for biotin through receptor mediated endocytosis.
authors.affiliation: Department of Pharmacy-Drug Sciences, University of Bari "Aldo Moro", Bari, Italy.
authors.forename: Delia
authors.initials: D
authors.lastname: Mandracchia
authors.affiliation: Veneto Institute of Oncology IOV-IRCCS, Padua, Italy; Department of Surgery, Oncology and Gastroenterology, University of Padua, Padua, Italy.
authors.forename: Antonio
authors.initials: A
authors.lastname: Rosato
authors.affiliation: Department of Pharmacy-Drug Sciences, University of Bari "Aldo Moro", Bari, Italy.
authors.forename: Adriana
authors.initials: A
authors.lastname: Trapani
authors.affiliation: Department of Drug Sciences, University of Pavia, Pavia, Italy.
authors.forename: Theodora
authors.initials: T
authors.lastname: Chlapanidas
authors.affiliation: Veneto Institute of Oncology IOV-IRCCS, Padua, Italy.
authors.forename: Isabella Monia
authors.initials: IM
authors.lastname: Montagner
authors.affiliation: Department of Drug Sciences, University of Pavia, Pavia, Italy.
authors.forename: Sara
authors.initials: S
authors.lastname: Perteghella
authors.affiliation: CNR-IFN Bari, Bari, Italy.
authors.forename: Cinzia
authors.initials: C
authors.lastname: Di Franco
authors.affiliation: Department of Drug Sciences, University of Pavia, Pavia, Italy.
authors.forename: Maria Luisa
authors.initials: ML
authors.lastname: Torre
authors.affiliation: Department of Pharmacy-Drug Sciences, University of Bari "Aldo Moro", Bari, Italy.
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Trapani
authors.affiliation: Department of Drug Sciences, University of Pavia, Pavia, Italy. Electronic address: giuseppe.tripodo@unipv.it.
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Tripodo
mesh_terms: D000818:Animals; D001710:Biotin / Q000737:chemistry / Q000493:pharmacokinetics*; D018938:Caco-2 Cells; D004337:Drug Carriers / Q000737:chemistry / Q000493:pharmacokinetics*; D016503:Drug Delivery Systems; D005260:Female; D006801:Humans; D007444:Inulin / Q000737:chemistry / Q000493:pharmacokinetics*; D008807:Mice, Inbred BALB C; D008823:Micelles; D061848:Optical Imaging; D014810:Vitamin E / Q000737:chemistry / Q000493:pharmacokinetics*
chemical_list: D004337:Drug Carriers; D008823:Micelles; D014810:Vitamin E; D001710:Biotin; D007444:Inulin
keywords: Biotin; Cancer; Inulin; Micelle; Optical imaging; Vitamin E