title: Evaluation of thermoresponsive properties and biocompatibility of polybenzofulvene aggregates for leuprolide delivery.
abstract: In this study, a polybenzofulvene derivative named poly-6-MOEG-9-BF3k, was evaluated as polymeric material for the production of injectable thermoresponsive nano-aggregates able to load low molecular weight peptidic drug, like the anticancer leuprolide. Thermoresponsive behavior of poly-6-MOEG-9-BF3k was studied in aqueous media by evaluating scattering intensity variations by means of DLS in function of temperature. Zeta potential measurements and SEM observations were also carried out. Moreover, critical aggregation temperature of the poly-6-MOEG-9-BF3k polymer was evaluated by pyrene fluorescence analysis. Then, the ability of prepared thermoresponsive aggregates to protect this model oligopeptide drug and regulate its release rate in function of external temperature was evaluated in vitro. Finally, biocompatibility of poly-6-MOEG-9-BF3k aggregates was tested in vitro on a healthy cell line (human bronchial epithelial cell; 16-HBE) and in vivo on rat animal model upon subcutaneous administration.
authors.affiliation: Department of Scienze e Tecnologie Molecolari e Biomolecolari, Laboratory of Biocompatible Polymers, University of Palermo, Via Archirafi, 32 90129 Palermo, Italy. mariano.licciardi@unipa.it
authors.forename: Mariano
authors.initials: M
authors.lastname: Licciardi
authors.forename: Giovanni
authors.initials: G
authors.lastname: Amato
authors.forename: Andrea
authors.initials: A
authors.lastname: Cappelli
authors.forename: Marco
authors.initials: M
authors.lastname: Paolino
authors.forename: Germano
authors.initials: G
authors.lastname: Giuliani
authors.forename: Beatrice
authors.initials: B
authors.lastname: Belmonte
authors.forename: Carla
authors.initials: C
authors.lastname: Guarnotta
authors.forename: Giovanna
authors.initials: G
authors.lastname: Pitarresi
authors.forename: Gaetano
authors.initials: G
authors.lastname: Giammona
mesh_terms: D000818:Animals; D018931:Antineoplastic Agents, Hormonal / Q000008:administration & dosage* / Q000737:chemistry; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D004337:Drug Carriers / Q000008:administration & dosage* / Q000737:chemistry; D006801:Humans; D007192:Indenes / Q000008:administration & dosage* / Q000737:chemistry; D016729:Leuprolide / Q000008:administration & dosage* / Q000737:chemistry; D008297:Male; D008855:Microscopy, Electron, Scanning; D049329:Nanostructures / Q000008:administration & dosage* / Q000737:chemistry / Q000648:ultrastructure; D011108:Polymers / Q000008:administration & dosage* / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar; D012867:Skin / Q000033:anatomy & histology / Q000187:drug effects; D013696:Temperature
chemical_list: D018931:Antineoplastic Agents, Hormonal; D004337:Drug Carriers; D007192:Indenes; D011108:Polymers; C578962:poly-6-MOEG-9-BF3k; D016729:Leuprolide