title: pH-sensitive niosomes: Effects on cytotoxicity and on inflammation and pain in murine models.
abstract: pH-sensitive nonionic surfactant vesicles (niosomes) by polysorbate-20 (Tween-20) or polysorbate-20 derivatized by glycine (added as pH sensitive agent), were developed to deliver Ibuprofen (IBU) and Lidocaine (LID). For the physical-chemical characterization of vesicles (mean size, size distribution, zeta potential, vesicle morphology, bilayer properties and stability) dynamic light scattering (DLS), small angle X-ray scattering and fluorescence studies were performed. Potential cytotoxicity was evaluated on immortalized human keratinocyte cells (HaCaT) and on immortalized mouse fibroblasts Balb/3T3. In vivo antinociceptive activity (formalin test) and anti-inflammatory activity tests (paw edema induced by zymosan) in murine models were performed on drug-loaded niosomes. pH-sensitive niosomes were stable in the presence of 0 and 10% fetal bovine serum, non-cytotoxic and able to modify IBU or LID pharmacological activity in vivo. The synthesis of stimuli responsive surfactant, as an alternative to add pH-sensitive molecules to niosomes, could represent a promising delivery strategy for anesthetic and anti-inflammatory drugs.
authors.affiliation: a Fondazione Istituto Italiano di Tecnologia , Center for Life Nano Science@Sapienza , Rome , Italy.
authors.forename: Federica
authors.initials: F
authors.lastname: Rinaldi
authors.affiliation: b Department of Medical Biotechnologies and Traslational Medicine , University of Milan , Milan , Italy.
authors.forename: Elena
authors.initials: E
authors.lastname: Del Favero
authors.affiliation: b Department of Medical Biotechnologies and Traslational Medicine , University of Milan , Milan , Italy.
authors.forename: Valeria
authors.initials: V
authors.lastname: Rondelli
authors.affiliation: c Department of Therapeutic Research and Medicine Evaluation , Istituto Superiore di Sanità , Rome , Italy.
authors.forename: Stefano
authors.initials: S
authors.lastname: Pieretti
authors.affiliation: d Consumers and Reference Materials, Consumer Products Safety Unit (F.2) , European Commission, Directorate General Joint Research Centre Directorate F - Health , ISPRA , Varese , Italy.
authors.forename: Alessia
authors.initials: A
authors.lastname: Bogni
authors.affiliation: d Consumers and Reference Materials, Consumer Products Safety Unit (F.2) , European Commission, Directorate General Joint Research Centre Directorate F - Health , ISPRA , Varese , Italy.
authors.forename: Jessica
authors.initials: J
authors.lastname: Ponti
authors.affiliation: d Consumers and Reference Materials, Consumer Products Safety Unit (F.2) , European Commission, Directorate General Joint Research Centre Directorate F - Health , ISPRA , Varese , Italy.
authors.forename: François
authors.initials: F
authors.lastname: Rossi
authors.affiliation: e Department of Pharmacy , University "G. d'Annunzio" , Chieti , Italy.
authors.forename: Luisa
authors.initials: L
authors.lastname: Di Marzio
authors.affiliation: f Interregional Research Center for Food Safety & Health (IRC-FSH), Campus Universitario "S. Venuta", University of Catanzaro "Magna Græcia" , Catanzaro , Italy.|g Department of Health Sciences , Campus Universitario "S. Venuta", University of Catanzaro "Magna Græcia" , Catanzaro , Italy.
authors.forename: Donatella
authors.initials: D
authors.lastname: Paolino
authors.affiliation: h Department of Drug Chemistry and Technology , University of Rome "Sapienza" , Rome , Italy.
authors.forename: Carlotta
authors.initials: C
authors.lastname: Marianecci
authors.affiliation: h Department of Drug Chemistry and Technology , University of Rome "Sapienza" , Rome , Italy.
authors.forename: Maria
authors.initials: M
authors.lastname: Carafa
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000494:pharmacology*; D041702:BALB 3T3 Cells; D002478:Cells, Cultured; D004195:Disease Models, Animal; D005347:Fibroblasts / Q000187:drug effects; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007052:Ibuprofen / Q000008:administration & dosage / Q000494:pharmacology*; D007249:Inflammation / Q000188:drug therapy*; D008012:Lidocaine / Q000008:administration & dosage / Q000494:pharmacology*; D008081:Liposomes / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology; D051379:Mice; D010146:Pain / Q000188:drug therapy*; D010147:Pain Measurement; D013501:Surface-Active Agents / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D008081:Liposomes; D013501:Surface-Active Agents; D008012:Lidocaine; D007052:Ibuprofen
keywords: anti-nociceptive/anti-inflammatory activity; cytotoxicity; ibuprofen; lidocaine; pH-sensitive niosomes