Mucoadhesive, Thermoreversible Hydrogel, Containing Tetracaine-Loaded Nanostructured Lipid Carriers for Topical, Intranasal Needle-Free Anesthesia

Recent advances have been reported for needle-free local anesthesia in maxillary teeth by administering a nasal spray of tetracaine (TTC) and oxymetazoline, without causing pain, fear, and stress. This work aimed to assess whether a TTC-loaded hybrid system could reduce cytotoxicity, promote sustain...

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Autores principales: Giovana Maria Fioramonti Calixto, Bruno Vilela Muniz, Simone R. Castro, Jaiza Samara Macena de Araujo, Klinger de Souza Amorim, Lígia N. M. Ribeiro, Luiz Eduardo Nunes Ferreira, Daniele Ribeiro de Araújo, Eneida de Paula, Michelle Franz-Montan
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Publicado: MDPI AG 2021
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Acceso en línea:https://doaj.org/article/47407dbe31b5403ca40d04eb1642c9de
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spelling oai:doaj.org-article:47407dbe31b5403ca40d04eb1642c9de2021-11-25T18:40:27ZMucoadhesive, Thermoreversible Hydrogel, Containing Tetracaine-Loaded Nanostructured Lipid Carriers for Topical, Intranasal Needle-Free Anesthesia10.3390/pharmaceutics131117601999-4923https://doaj.org/article/47407dbe31b5403ca40d04eb1642c9de2021-10-01T00:00:00Zhttps://www.mdpi.com/1999-4923/13/11/1760https://doaj.org/toc/1999-4923Recent advances have been reported for needle-free local anesthesia in maxillary teeth by administering a nasal spray of tetracaine (TTC) and oxymetazoline, without causing pain, fear, and stress. This work aimed to assess whether a TTC-loaded hybrid system could reduce cytotoxicity, promote sustained permeation, and increase the anesthetic efficacy of TTC for safe, effective, painless, and prolonged analgesia of the maxillary teeth in dental procedures. The hybrid system based on TTC (4%) encapsulated in nanostructured lipid carriers (NLC) and incorporated into a thermoreversible hydrogel of poloxamer 407 (TTC<sub>NLC-HG4%</sub>) displayed desirable rheological, mechanical, and mucoadhesive properties for topical application in the nasal cavity. Compared to control formulations, the use of TTC<sub>NLC-HG4%</sub> slowed in vitro permeation of the anesthetic across the nasal mucosa, maintained cytotoxicity against neuroblastoma cells, and provided a three-fold increase in analgesia duration, as observed using the tail-flick test in mice. The results obtained here open up perspectives for future clinical evaluation of the thermoreversible hybrid hydrogel, which contains TTC-loaded NLC, with the aim of creating an effective, topical, intranasal, needle-free anesthesia for use in dentistry.Giovana Maria Fioramonti CalixtoBruno Vilela MunizSimone R. CastroJaiza Samara Macena de AraujoKlinger de Souza AmorimLígia N. M. RibeiroLuiz Eduardo Nunes FerreiraDaniele Ribeiro de AraújoEneida de PaulaMichelle Franz-MontanMDPI AGarticlenanostructured lipid carriersthermoreversible hydrogelnasal administrationmucoadhesiontopical anesthesiatetracainePharmacy and materia medicaRS1-441ENPharmaceutics, Vol 13, Iss 1760, p 1760 (2021)
institution DOAJ
collection DOAJ
language EN
topic nanostructured lipid carriers
thermoreversible hydrogel
nasal administration
mucoadhesion
topical anesthesia
tetracaine
Pharmacy and materia medica
RS1-441
spellingShingle nanostructured lipid carriers
thermoreversible hydrogel
nasal administration
mucoadhesion
topical anesthesia
tetracaine
Pharmacy and materia medica
RS1-441
Giovana Maria Fioramonti Calixto
Bruno Vilela Muniz
Simone R. Castro
Jaiza Samara Macena de Araujo
Klinger de Souza Amorim
Lígia N. M. Ribeiro
Luiz Eduardo Nunes Ferreira
Daniele Ribeiro de Araújo
Eneida de Paula
Michelle Franz-Montan
Mucoadhesive, Thermoreversible Hydrogel, Containing Tetracaine-Loaded Nanostructured Lipid Carriers for Topical, Intranasal Needle-Free Anesthesia
description Recent advances have been reported for needle-free local anesthesia in maxillary teeth by administering a nasal spray of tetracaine (TTC) and oxymetazoline, without causing pain, fear, and stress. This work aimed to assess whether a TTC-loaded hybrid system could reduce cytotoxicity, promote sustained permeation, and increase the anesthetic efficacy of TTC for safe, effective, painless, and prolonged analgesia of the maxillary teeth in dental procedures. The hybrid system based on TTC (4%) encapsulated in nanostructured lipid carriers (NLC) and incorporated into a thermoreversible hydrogel of poloxamer 407 (TTC<sub>NLC-HG4%</sub>) displayed desirable rheological, mechanical, and mucoadhesive properties for topical application in the nasal cavity. Compared to control formulations, the use of TTC<sub>NLC-HG4%</sub> slowed in vitro permeation of the anesthetic across the nasal mucosa, maintained cytotoxicity against neuroblastoma cells, and provided a three-fold increase in analgesia duration, as observed using the tail-flick test in mice. The results obtained here open up perspectives for future clinical evaluation of the thermoreversible hybrid hydrogel, which contains TTC-loaded NLC, with the aim of creating an effective, topical, intranasal, needle-free anesthesia for use in dentistry.
format article
author Giovana Maria Fioramonti Calixto
Bruno Vilela Muniz
Simone R. Castro
Jaiza Samara Macena de Araujo
Klinger de Souza Amorim
Lígia N. M. Ribeiro
Luiz Eduardo Nunes Ferreira
Daniele Ribeiro de Araújo
Eneida de Paula
Michelle Franz-Montan
author_facet Giovana Maria Fioramonti Calixto
Bruno Vilela Muniz
Simone R. Castro
Jaiza Samara Macena de Araujo
Klinger de Souza Amorim
Lígia N. M. Ribeiro
Luiz Eduardo Nunes Ferreira
Daniele Ribeiro de Araújo
Eneida de Paula
Michelle Franz-Montan
author_sort Giovana Maria Fioramonti Calixto
title Mucoadhesive, Thermoreversible Hydrogel, Containing Tetracaine-Loaded Nanostructured Lipid Carriers for Topical, Intranasal Needle-Free Anesthesia
title_short Mucoadhesive, Thermoreversible Hydrogel, Containing Tetracaine-Loaded Nanostructured Lipid Carriers for Topical, Intranasal Needle-Free Anesthesia
title_full Mucoadhesive, Thermoreversible Hydrogel, Containing Tetracaine-Loaded Nanostructured Lipid Carriers for Topical, Intranasal Needle-Free Anesthesia
title_fullStr Mucoadhesive, Thermoreversible Hydrogel, Containing Tetracaine-Loaded Nanostructured Lipid Carriers for Topical, Intranasal Needle-Free Anesthesia
title_full_unstemmed Mucoadhesive, Thermoreversible Hydrogel, Containing Tetracaine-Loaded Nanostructured Lipid Carriers for Topical, Intranasal Needle-Free Anesthesia
title_sort mucoadhesive, thermoreversible hydrogel, containing tetracaine-loaded nanostructured lipid carriers for topical, intranasal needle-free anesthesia
publisher MDPI AG
publishDate 2021
url https://doaj.org/article/47407dbe31b5403ca40d04eb1642c9de
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