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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.

SUBMITTER: Rinaldi F 

PROVIDER: S-EPMC6010110 | biostudies-literature | 2017 Dec

REPOSITORIES: biostudies-literature

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pH-sensitive niosomes: Effects on cytotoxicity and on inflammation and pain in murine models.

Rinaldi Federica F   Del Favero Elena E   Rondelli Valeria V   Pieretti Stefano S   Bogni Alessia A   Ponti Jessica J   Rossi François F   Di Marzio Luisa L   Paolino Donatella D   Marianecci Carlotta C   Carafa Maria M  

Journal of enzyme inhibition and medicinal chemistry 20171201 1


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 wa  ...[more]

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