Combining amino amide salts in mucoadhesive films enhances needle-free buccal anesthesia in adults

Autor(es)

do Couto, Rene Oliveira ^[1] ; Cubayachi, Camila ^[2] ; Calefi, Paulo Linares ^[3] ; Vianna Lopez, Renata Fonseca ^[2] ; Pedrazzi, Vinicius ^[3] ; De Gaitani, Cristiane Masetto ^[2] ; de Freitas, Osvaldo ^[2]

Afiliação do(s) autor(es)

^[1] Univ Estadual Londrina, Dept Pharmaceut Sci, Ave Robert Koch 60, BR-86038350 Londrina, PR - Brazil

^[2] Univ Sao Paulo, Sch Pharmaceut Sci Ribeirao Preto, Ribeirao Preto, SP - Brazil

^[3] Univ Sao Paulo, Sch Dent Ribeirao Preto, Ribeirao Preto, SP - Brazil

• Tipo de documento: Artigo Científico
• Fonte: JOURNAL OF CONTROLLED RELEASE; v. 266, p. 205-215, NOV 28 2017.
• Citações Web of Science: 5

Resumo

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 5 min, peak of anesthetic effect within 15 and 25 min and anesthesia duration of 50 min 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. (AU)

• Processo FAPESP: 12/07251-6 - Desenvolvimento de plataforma com sistemas mucoadesivos para liberação de fármacos na cavidade bucal
• Beneficiário: Osvaldo de Freitas
• Modalidade de apoio: Auxílio à Pesquisa - Regular
• Processo FAPESP: 12/05644-0 - Desenvolvimento de sistemas semi-sólidos mucoadesivos para liberação de anestésico e aplicação de iontoforese na cavidade bucal
• Beneficiário: Camila Cubayachi
• Modalidade de apoio: Bolsas no Brasil - Mestrado
• Processo FAPESP: 13/12174-3 - Estudo de polímeros reabsorvíveis: efeito da degradação e erosão na liberação de corantes
• Beneficiário: Renê Oliveira Do Couto
• Modalidade de apoio: Bolsas no Exterior - Estágio de Pesquisa - Doutorado
• Processo FAPESP: 14/22451-7 - Sistemas de liberação sustentada e direcionada de fármacos para o tecido epitelial
• Beneficiário: Renata Fonseca Vianna Lopez
• Modalidade de apoio: Auxílio à Pesquisa - Temático
• Processo FAPESP: 12/06167-1 - Desenvolvimento de filmes mucoadesivos para liberação de fármacos anestésicos na cavidade bucal
• Beneficiário: Renê Oliveira Do Couto
• Modalidade de apoio: Bolsas no Brasil - Doutorado