Combining amino amide salts in mucoadhesive films enhances needle-free buccal anesthesia in adults.
Identifieur interne : 000126 ( Main/Exploration ); précédent : 000125; suivant : 000127Combining amino amide salts in mucoadhesive films enhances needle-free buccal anesthesia in adults.
Auteurs : Renê Oliveira Do Couto [Brésil] ; Camila Cubayachi [Brésil] ; Paulo Linares Calefi [Brésil] ; Renata Fonseca Vianna Lopez [Brésil] ; Vinícius Pedrazzi [Brésil] ; Cristiane Masetto De Gaitani [Brésil] ; Osvaldo De Freitas [Brésil]Source :
- Journal of controlled release : official journal of the Controlled Release Society [ 1873-4995 ] ; 2017.
Descripteurs français
- KwdFr :
- Adhésivité (MeSH), Adulte (MeSH), Amides (administration et posologie), Anesthésie (MeSH), Anesthésiques locaux (administration et posologie), Animaux (MeSH), Femelle (MeSH), Humains (MeSH), Lidocaïne (administration et posologie), Muqueuse de la bouche (métabolisme), Muqueuse oesophagienne (MeSH), Mâle (MeSH), Prilocaïne (administration et posologie), Sels (administration et posologie), Suidae (MeSH), Systèmes de délivrance de médicaments (MeSH), Études croisées (MeSH).
- MESH :
- administration et posologie : Amides, Anesthésiques locaux, Lidocaïne, Prilocaïne, Sels.
- métabolisme : Muqueuse de la bouche.
- Adhésivité, Adulte, Anesthésie, Animaux, Femelle, Humains, Muqueuse oesophagienne, Mâle, Suidae, Systèmes de délivrance de médicaments, Études croisées.
English descriptors
- KwdEn :
- Adhesiveness (MeSH), Adult (MeSH), Amides (administration & dosage), Anesthesia (MeSH), Anesthetics, Local (administration & dosage), Animals (MeSH), Cross-Over Studies (MeSH), Drug Delivery Systems (MeSH), Esophageal Mucosa (MeSH), Female (MeSH), Humans (MeSH), Lidocaine (administration & dosage), Male (MeSH), Mouth Mucosa (metabolism), Prilocaine (administration & dosage), Salts (administration & dosage), Swine (MeSH).
- MESH :
- chemical , administration & dosage : Amides, Anesthetics, Local, Lidocaine, Prilocaine, Salts.
- metabolism : Mouth Mucosa.
- Adhesiveness, Adult, Anesthesia, Animals, Cross-Over Studies, Drug Delivery Systems, Esophageal Mucosa, Female, Humans, Male, Swine.
Abstract
Needle-phobia is usually a great concern in dentistry, and the replacement of painful injections by patient-friendly needle-free topical formulations would bring several advantages in dental practice worldwide. In this pursuit, the effects of combining prilocaine hydrochloride (PCL) and lidocaine hydrochloride (LCL) in different proportions in mucoadhesive films on their in vitro permeation and retention through porcine esophageal mucosa was studied. Complementarily, the permeation and retention of isolated LCL was investigated. The in vitro model used for evaluating buccal anesthetic penetration and retention in buccal epithelium was validated. In addition, the feasibility of a novel in vivo model to evaluate the painful sensation due to puncture "needle-shaped" gum jaw of adults at shallow and deep levels was demonstrated. The in vivo clinical survey revealed the efficiency of the films, which had onset of anesthesia at 5min, peak of anesthetic effect within 15 and 25min and anesthesia duration of 50min after being placed in maxillary sites. The in vitro drug flux, permeability coefficient and retention in the epithelium significantly correlated with in vivo onset, peak and extent of shallow and deep anesthetic effect. At shallow level, the permeation of LCL has shown to be closely related to the onset of anesthesia, while the penetration of PCL has a significant impact in the peak of anesthetic effect. Concerning the deep level, the penetration of PCL is required to attain the onset of anesthetic effect. The total amount of drug retained in the epithelium showed to modulate the extent of both shallow and deep anesthesia. Thus, the combination of LCL and PCL in mucoadhesive films may offer dentists and their patients a safe improvement for pain management during dental procedures.
DOI: 10.1016/j.jconrel.2017.09.039
PubMed: 28974451
Affiliations:
Links toward previous steps (curation, corpus...)
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sortKey="Calefi, Paulo Linares" sort="Calefi, Paulo Linares" uniqKey="Calefi P" first="Paulo Linares" last="Calefi">Paulo Linares Calefi</name><affiliation wicri:level="4"><nlm:affiliation>University of São Paulo, School of Dentistry of Ribeirão Preto, Ribeirão Preto, SP, Brazil.</nlm:affiliation><country xml:lang="fr">Brésil</country><wicri:regionArea>University of São Paulo, School of Dentistry of Ribeirão Preto, Ribeirão Preto, SP</wicri:regionArea><placeName><region type="state">État de São Paulo</region><settlement type="city">São Paulo</settlement></placeName><orgName type="university">Université de São Paulo</orgName></affiliation></author><author><name sortKey="Lopez, Renata Fonseca Vianna" sort="Lopez, Renata Fonseca Vianna" uniqKey="Lopez R" first="Renata Fonseca Vianna" last="Lopez">Renata Fonseca Vianna Lopez</name><affiliation wicri:level="4"><nlm:affiliation>University of São Paulo, School of Pharmaceutical Sciences of Ribeirão Preto, Ribeirão Preto, SP, 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type="university">Université de São Paulo</orgName></affiliation></author><author><name sortKey="De Gaitani, Cristiane Masetto" sort="De Gaitani, Cristiane Masetto" uniqKey="De Gaitani C" first="Cristiane Masetto" last="De Gaitani">Cristiane Masetto De Gaitani</name><affiliation wicri:level="4"><nlm:affiliation>University of São Paulo, School of Pharmaceutical Sciences of Ribeirão Preto, Ribeirão Preto, SP, Brazil.</nlm:affiliation><country xml:lang="fr">Brésil</country><wicri:regionArea>University of São Paulo, School of Pharmaceutical Sciences of Ribeirão Preto, Ribeirão Preto, SP</wicri:regionArea><placeName><region type="state">État de São Paulo</region><settlement type="city">São Paulo</settlement></placeName><orgName type="university">Université de São Paulo</orgName></affiliation></author><author><name sortKey="De Freitas, Osvaldo" sort="De Freitas, Osvaldo" uniqKey="De Freitas O" first="Osvaldo" last="De Freitas">Osvaldo De Freitas</name><affiliation wicri:level="4"><nlm:affiliation>University of São Paulo, School of Pharmaceutical Sciences of Ribeirão Preto, Ribeirão Preto, SP, Brazil.</nlm:affiliation><country xml:lang="fr">Brésil</country><wicri:regionArea>University of São Paulo, School of Pharmaceutical Sciences of Ribeirão Preto, Ribeirão Preto, SP</wicri:regionArea><placeName><region type="state">État de São Paulo</region><settlement type="city">São Paulo</settlement></placeName><orgName type="university">Université de São Paulo</orgName></affiliation></author></analytic><series><title level="j">Journal of controlled release : official journal of the Controlled Release Society</title><idno type="eISSN">1873-4995</idno><imprint><date when="2017" type="published">2017</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Adhesiveness (MeSH)</term><term>Adult (MeSH)</term><term>Amides (administration & dosage)</term><term>Anesthesia (MeSH)</term><term>Anesthetics, Local (administration & dosage)</term><term>Animals (MeSH)</term><term>Cross-Over Studies (MeSH)</term><term>Drug Delivery Systems (MeSH)</term><term>Esophageal Mucosa (MeSH)</term><term>Female (MeSH)</term><term>Humans (MeSH)</term><term>Lidocaine (administration & dosage)</term><term>Male (MeSH)</term><term>Mouth Mucosa (metabolism)</term><term>Prilocaine (administration & dosage)</term><term>Salts (administration & dosage)</term><term>Swine (MeSH)</term></keywords><keywords scheme="KwdFr" xml:lang="fr"><term>Adhésivité (MeSH)</term><term>Adulte (MeSH)</term><term>Amides (administration et posologie)</term><term>Anesthésie (MeSH)</term><term>Anesthésiques locaux (administration et posologie)</term><term>Animaux (MeSH)</term><term>Femelle (MeSH)</term><term>Humains (MeSH)</term><term>Lidocaïne (administration et posologie)</term><term>Muqueuse de la bouche (métabolisme)</term><term>Muqueuse oesophagienne (MeSH)</term><term>Mâle (MeSH)</term><term>Prilocaïne (administration et posologie)</term><term>Sels (administration et posologie)</term><term>Suidae (MeSH)</term><term>Systèmes de délivrance de médicaments (MeSH)</term><term>Études croisées (MeSH)</term></keywords><keywords scheme="MESH" type="chemical" qualifier="administration & dosage" xml:lang="en"><term>Amides</term><term>Anesthetics, Local</term><term>Lidocaine</term><term>Prilocaine</term><term>Salts</term></keywords><keywords scheme="MESH" qualifier="administration et posologie" xml:lang="fr"><term>Amides</term><term>Anesthésiques locaux</term><term>Lidocaïne</term><term>Prilocaïne</term><term>Sels</term></keywords><keywords scheme="MESH" qualifier="metabolism" xml:lang="en"><term>Mouth Mucosa</term></keywords><keywords scheme="MESH" qualifier="métabolisme" xml:lang="fr"><term>Muqueuse de la bouche</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Adhesiveness</term><term>Adult</term><term>Anesthesia</term><term>Animals</term><term>Cross-Over Studies</term><term>Drug Delivery Systems</term><term>Esophageal Mucosa</term><term>Female</term><term>Humans</term><term>Male</term><term>Swine</term></keywords><keywords scheme="MESH" xml:lang="fr"><term>Adhésivité</term><term>Adulte</term><term>Anesthésie</term><term>Animaux</term><term>Femelle</term><term>Humains</term><term>Muqueuse oesophagienne</term><term>Mâle</term><term>Suidae</term><term>Systèmes de délivrance de médicaments</term><term>Études croisées</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Needle-phobia is usually a great concern in dentistry, and the replacement of painful injections by patient-friendly needle-free topical formulations would bring several advantages in dental practice worldwide. In this pursuit, the effects of combining prilocaine hydrochloride (PCL) and lidocaine hydrochloride (LCL) in different proportions in mucoadhesive films on their in vitro permeation and retention through porcine esophageal mucosa was studied. Complementarily, the permeation and retention of isolated LCL was investigated. The in vitro model used for evaluating buccal anesthetic penetration and retention in buccal epithelium was validated. In addition, the feasibility of a novel in vivo model to evaluate the painful sensation due to puncture "needle-shaped" gum jaw of adults at shallow and deep levels was demonstrated. The in vivo clinical survey revealed the efficiency of the films, which had onset of anesthesia at 5min, peak of anesthetic effect within 15 and 25min and anesthesia duration of 50min after being placed in maxillary sites. The in vitro drug flux, permeability coefficient and retention in the epithelium significantly correlated with in vivo onset, peak and extent of shallow and deep anesthetic effect. At shallow level, the permeation of LCL has shown to be closely related to the onset of anesthesia, while the penetration of PCL has a significant impact in the peak of anesthetic effect. Concerning the deep level, the penetration of PCL is required to attain the onset of anesthetic effect. The total amount of drug retained in the epithelium showed to modulate the extent of both shallow and deep anesthesia. Thus, the combination of LCL and PCL in mucoadhesive films may offer dentists and their patients a safe improvement for pain management during dental procedures.</div></front></TEI><pubmed><MedlineCitation Status="MEDLINE" Owner="NLM"><PMID Version="1">28974451</PMID><DateCompleted><Year>2018</Year><Month>07</Month><Day>27</Day></DateCompleted><DateRevised><Year>2018</Year><Month>07</Month><Day>27</Day></DateRevised><Article PubModel="Print-Electronic"><Journal><ISSN IssnType="Electronic">1873-4995</ISSN><JournalIssue CitedMedium="Internet"><Volume>266</Volume><PubDate><Year>2017</Year><Month>Nov</Month><Day>28</Day></PubDate></JournalIssue><Title>Journal of controlled release : official journal of the Controlled Release Society</Title><ISOAbbreviation>J Control Release</ISOAbbreviation></Journal><ArticleTitle>Combining amino amide salts in mucoadhesive films enhances needle-free buccal anesthesia in adults.</ArticleTitle><Pagination><MedlinePgn>205-215</MedlinePgn></Pagination><ELocationID EIdType="pii" ValidYN="Y">S0168-3659(17)30883-0</ELocationID><ELocationID EIdType="doi" ValidYN="Y">10.1016/j.jconrel.2017.09.039</ELocationID><Abstract><AbstractText>Needle-phobia is usually a great concern in dentistry, and the replacement of painful injections by patient-friendly needle-free topical formulations would bring several advantages in dental practice worldwide. In this pursuit, the effects of combining prilocaine hydrochloride (PCL) and lidocaine hydrochloride (LCL) in different proportions in mucoadhesive films on their in vitro permeation and retention through porcine esophageal mucosa was studied. Complementarily, the permeation and retention of isolated LCL was investigated. The in vitro model used for evaluating buccal anesthetic penetration and retention in buccal epithelium was validated. In addition, the feasibility of a novel in vivo model to evaluate the painful sensation due to puncture "needle-shaped" gum jaw of adults at shallow and deep levels was demonstrated. The in vivo clinical survey revealed the efficiency of the films, which had onset of anesthesia at 5min, peak of anesthetic effect within 15 and 25min and anesthesia duration of 50min after being placed in maxillary sites. The in vitro drug flux, permeability coefficient and retention in the epithelium significantly correlated with in vivo onset, peak and extent of shallow and deep anesthetic effect. At shallow level, the permeation of LCL has shown to be closely related to the onset of anesthesia, while the penetration of PCL has a significant impact in the peak of anesthetic effect. Concerning the deep level, the penetration of PCL is required to attain the onset of anesthetic effect. The total amount of drug retained in the epithelium showed to modulate the extent of both shallow and deep anesthesia. Thus, the combination of LCL and PCL in mucoadhesive films may offer dentists and their patients a safe improvement for pain management during dental procedures.</AbstractText><CopyrightInformation>Copyright © 2017 Elsevier B.V. All rights reserved.</CopyrightInformation></Abstract><AuthorList CompleteYN="Y"><Author ValidYN="Y"><LastName>do Couto</LastName><ForeName>Renê Oliveira</ForeName><Initials>RO</Initials><AffiliationInfo><Affiliation>The State University of Londrina, Department of Pharmaceutical Sciences, Londrina, PR, Brazil. Electronic address: rocouto@uel.br.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>Cubayachi</LastName><ForeName>Camila</ForeName><Initials>C</Initials><AffiliationInfo><Affiliation>University of São Paulo, School of Pharmaceutical Sciences of Ribeirão Preto, Ribeirão Preto, SP, Brazil.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>Calefi</LastName><ForeName>Paulo Linares</ForeName><Initials>PL</Initials><AffiliationInfo><Affiliation>University of São Paulo, School of Dentistry of Ribeirão Preto, Ribeirão Preto, SP, Brazil.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>Lopez</LastName><ForeName>Renata Fonseca Vianna</ForeName><Initials>RFV</Initials><AffiliationInfo><Affiliation>University of São Paulo, School of Pharmaceutical Sciences of Ribeirão Preto, Ribeirão Preto, SP, Brazil.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>Pedrazzi</LastName><ForeName>Vinícius</ForeName><Initials>V</Initials><AffiliationInfo><Affiliation>University of São Paulo, School of Dentistry of Ribeirão Preto, Ribeirão Preto, SP, Brazil.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>De Gaitani</LastName><ForeName>Cristiane Masetto</ForeName><Initials>CM</Initials><AffiliationInfo><Affiliation>University of São Paulo, School of Pharmaceutical Sciences of Ribeirão Preto, Ribeirão Preto, SP, Brazil.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>de Freitas</LastName><ForeName>Osvaldo</ForeName><Initials>O</Initials><AffiliationInfo><Affiliation>University of São Paulo, School of Pharmaceutical Sciences of Ribeirão Preto, Ribeirão Preto, SP, Brazil.</Affiliation></AffiliationInfo></Author></AuthorList><Language>eng</Language><PublicationTypeList><PublicationType UI="D016428">Journal Article</PublicationType><PublicationType UI="D016449">Randomized Controlled Trial</PublicationType></PublicationTypeList><ArticleDate DateType="Electronic"><Year>2017</Year><Month>09</Month><Day>30</Day></ArticleDate></Article><MedlineJournalInfo><Country>Netherlands</Country><MedlineTA>J Control Release</MedlineTA><NlmUniqueID>8607908</NlmUniqueID><ISSNLinking>0168-3659</ISSNLinking></MedlineJournalInfo><ChemicalList><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance UI="D000577">Amides</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance UI="D000779">Anesthetics, Local</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance UI="D012492">Salts</NameOfSubstance></Chemical><Chemical><RegistryNumber>046O35D44R</RegistryNumber><NameOfSubstance UI="D011318">Prilocaine</NameOfSubstance></Chemical><Chemical><RegistryNumber>98PI200987</RegistryNumber><NameOfSubstance UI="D008012">Lidocaine</NameOfSubstance></Chemical></ChemicalList><CitationSubset>IM</CitationSubset><MeshHeadingList><MeshHeading><DescriptorName UI="D000268" MajorTopicYN="N">Adhesiveness</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D000328" MajorTopicYN="N">Adult</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D000577" MajorTopicYN="N">Amides</DescriptorName><QualifierName UI="Q000008" MajorTopicYN="Y">administration & dosage</QualifierName></MeshHeading><MeshHeading><DescriptorName UI="D000758" MajorTopicYN="N">Anesthesia</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D000779" MajorTopicYN="N">Anesthetics, Local</DescriptorName><QualifierName UI="Q000008" MajorTopicYN="Y">administration & dosage</QualifierName></MeshHeading><MeshHeading><DescriptorName UI="D000818" MajorTopicYN="N">Animals</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D018592" MajorTopicYN="N">Cross-Over Studies</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D016503" MajorTopicYN="Y">Drug Delivery Systems</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D000071041" MajorTopicYN="N">Esophageal Mucosa</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D005260" MajorTopicYN="N">Female</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D006801" MajorTopicYN="N">Humans</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D008012" MajorTopicYN="N">Lidocaine</DescriptorName><QualifierName UI="Q000008" MajorTopicYN="Y">administration & dosage</QualifierName></MeshHeading><MeshHeading><DescriptorName UI="D008297" MajorTopicYN="N">Male</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D009061" MajorTopicYN="N">Mouth Mucosa</DescriptorName><QualifierName UI="Q000378" MajorTopicYN="Y">metabolism</QualifierName></MeshHeading><MeshHeading><DescriptorName UI="D011318" MajorTopicYN="N">Prilocaine</DescriptorName><QualifierName UI="Q000008" MajorTopicYN="Y">administration & dosage</QualifierName></MeshHeading><MeshHeading><DescriptorName UI="D012492" MajorTopicYN="N">Salts</DescriptorName><QualifierName UI="Q000008" MajorTopicYN="Y">administration & dosage</QualifierName></MeshHeading><MeshHeading><DescriptorName UI="D013552" MajorTopicYN="N">Swine</DescriptorName></MeshHeading></MeshHeadingList></MedlineCitation><PubmedData><History><PubMedPubDate PubStatus="received"><Year>2017</Year><Month>08</Month><Day>10</Day></PubMedPubDate><PubMedPubDate PubStatus="accepted"><Year>2017</Year><Month>09</Month><Day>29</Day></PubMedPubDate><PubMedPubDate PubStatus="pubmed"><Year>2017</Year><Month>10</Month><Day>5</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="medline"><Year>2018</Year><Month>7</Month><Day>28</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="entrez"><Year>2017</Year><Month>10</Month><Day>5</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate></History><PublicationStatus>ppublish</PublicationStatus><ArticleIdList><ArticleId IdType="pubmed">28974451</ArticleId><ArticleId IdType="pii">S0168-3659(17)30883-0</ArticleId><ArticleId IdType="doi">10.1016/j.jconrel.2017.09.039</ArticleId></ArticleIdList></PubmedData></pubmed><affiliations><list><country><li>Brésil</li></country><region><li>Paraná (État)</li><li>État de São Paulo</li></region><settlement><li>São Paulo</li></settlement><orgName><li>Université de São Paulo</li></orgName></list><tree><country name="Brésil"><region name="Paraná (État)"><name sortKey="Do Couto, Rene Oliveira" sort="Do Couto, Rene Oliveira" uniqKey="Do Couto R" first="Renê Oliveira" last="Do Couto">Renê Oliveira Do Couto</name></region><name sortKey="Calefi, Paulo Linares" sort="Calefi, Paulo Linares" uniqKey="Calefi P" first="Paulo Linares" last="Calefi">Paulo Linares Calefi</name><name sortKey="Cubayachi, Camila" sort="Cubayachi, Camila" uniqKey="Cubayachi C" first="Camila" last="Cubayachi">Camila Cubayachi</name><name sortKey="De Freitas, Osvaldo" sort="De Freitas, Osvaldo" uniqKey="De Freitas O" first="Osvaldo" last="De Freitas">Osvaldo De Freitas</name><name sortKey="De Gaitani, Cristiane Masetto" sort="De Gaitani, Cristiane Masetto" uniqKey="De Gaitani C" first="Cristiane Masetto" last="De Gaitani">Cristiane Masetto De Gaitani</name><name sortKey="Lopez, Renata Fonseca Vianna" sort="Lopez, Renata Fonseca Vianna" uniqKey="Lopez R" first="Renata Fonseca Vianna" last="Lopez">Renata Fonseca Vianna Lopez</name><name sortKey="Pedrazzi, Vinicius" sort="Pedrazzi, Vinicius" uniqKey="Pedrazzi V" first="Vinícius" last="Pedrazzi">Vinícius Pedrazzi</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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