pH-sensitive niosomes: Effects on cytotoxicity and on inflammation and pain in murine models
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 distributio...
Main Authors: | , , , , , , , , , , |
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Format: | Article |
Language: | English |
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Taylor & Francis Group
2017-01-01
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Series: | Journal of Enzyme Inhibition and Medicinal Chemistry |
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Online Access: | http://dx.doi.org/10.1080/14756366.2016.1268607 |
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author | Federica Rinaldi Elena Del Favero Valeria Rondelli Stefano Pieretti Alessia Bogni Jessica Ponti François Rossi Luisa Di Marzio Donatella Paolino Carlotta Marianecci Maria Carafa |
author_facet | Federica Rinaldi Elena Del Favero Valeria Rondelli Stefano Pieretti Alessia Bogni Jessica Ponti François Rossi Luisa Di Marzio Donatella Paolino Carlotta Marianecci Maria Carafa |
author_sort | Federica Rinaldi |
collection | DOAJ |
description | 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. |
first_indexed | 2024-12-18T08:22:28Z |
format | Article |
id | doaj.art-b0d81602fdc14a12b913256a07b4610e |
institution | Directory Open Access Journal |
issn | 1475-6366 1475-6374 |
language | English |
last_indexed | 2024-12-18T08:22:28Z |
publishDate | 2017-01-01 |
publisher | Taylor & Francis Group |
record_format | Article |
series | Journal of Enzyme Inhibition and Medicinal Chemistry |
spelling | doaj.art-b0d81602fdc14a12b913256a07b4610e2022-12-21T21:14:42ZengTaylor & Francis GroupJournal of Enzyme Inhibition and Medicinal Chemistry1475-63661475-63742017-01-0132153854610.1080/14756366.2016.12686071268607pH-sensitive niosomes: Effects on cytotoxicity and on inflammation and pain in murine modelsFederica Rinaldi0Elena Del Favero1Valeria Rondelli2Stefano Pieretti3Alessia Bogni4Jessica Ponti5François Rossi6Luisa Di Marzio7Donatella Paolino8Carlotta Marianecci9Maria Carafa10Center for Life Nano Science@SapienzaUniversity of MilanUniversity of MilanIstituto Superiore di SanitàEuropean Commission, Directorate General Joint Research Centre Directorate F – HealthEuropean Commission, Directorate General Joint Research Centre Directorate F – HealthEuropean Commission, Directorate General Joint Research Centre Directorate F – HealthUniversity “G. d’Annunzio”Interregional Research Center for Food Safety & Health (IRC-FSH), Campus Universitario “S. Venuta”, University of Catanzaro “Magna Græcia”University of Rome “Sapienza”University of Rome “Sapienza”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.http://dx.doi.org/10.1080/14756366.2016.1268607pH-sensitive niosomeslidocaineibuprofencytotoxicityanti-nociceptive/anti-inflammatory activity |
spellingShingle | Federica Rinaldi Elena Del Favero Valeria Rondelli Stefano Pieretti Alessia Bogni Jessica Ponti François Rossi Luisa Di Marzio Donatella Paolino Carlotta Marianecci Maria Carafa pH-sensitive niosomes: Effects on cytotoxicity and on inflammation and pain in murine models Journal of Enzyme Inhibition and Medicinal Chemistry pH-sensitive niosomes lidocaine ibuprofen cytotoxicity anti-nociceptive/anti-inflammatory activity |
title | pH-sensitive niosomes: Effects on cytotoxicity and on inflammation and pain in murine models |
title_full | pH-sensitive niosomes: Effects on cytotoxicity and on inflammation and pain in murine models |
title_fullStr | pH-sensitive niosomes: Effects on cytotoxicity and on inflammation and pain in murine models |
title_full_unstemmed | pH-sensitive niosomes: Effects on cytotoxicity and on inflammation and pain in murine models |
title_short | pH-sensitive niosomes: Effects on cytotoxicity and on inflammation and pain in murine models |
title_sort | ph sensitive niosomes effects on cytotoxicity and on inflammation and pain in murine models |
topic | pH-sensitive niosomes lidocaine ibuprofen cytotoxicity anti-nociceptive/anti-inflammatory activity |
url | http://dx.doi.org/10.1080/14756366.2016.1268607 |
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