Needle-free buccal anesthesia using iontophoresis and amino amide salts combined in a mucoadhesive formulation

Author(s)

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

Affiliation

^[1] Univ Sao Paulo, Sch Pharmaceut Sci Ribeirao Preto, BR-14040903 Ribeirao Preto, SP - Brazil

^[2] Univ Sao Paulo, Sch Dent Ribeirao Preto, BR-14040903 Ribeirao Preto, SP - Brazil

• Document type: Journal article
• Source: COLLOIDS AND SURFACES B-BIOINTERFACES; v. 136, p. 1193-1201, DEC 1 2015.
• Web of Science Citations: 12

Abstract

Iontophoresis is a strategy to increase the penetration of drugs through biological membranes; however, its use has been underexplored in mucosa. The aim of this work was to investigate the influence of iontophoresis in the mucosal penetration of prilocaine hydrochloride (PCL) and lidocaine hydrochloride (LCL), which are largely used in dentistry as local anesthetics, when combined in the same formulation. Semisolid hydrogels containing these drugs either alone or in combination were developed at two different pHs (7.0 and 5.8) and presented adequate mechanical and mucoadhesive properties for buccal administration. The distribution coefficients between the mucosa and the formulations (D-m/f) and the in vitro mucosa permeation and retention rates were evaluated for both PCL and LCL. At pH 7.0, the combination of the drugs decreased the D-m/f of PCL by approximately 3-fold but did not change the D-m/f of LCL; iontophoresis increased the permeation rate of PCL by 12-fold and did not significantly change LCL flux compared with the passive permeation rate of the combined drugs. Combining the drugs also resulted in an increase in both PCL (86-fold) and LCL (12-fold) accumulation in the mucosa after iontophoresis at pH 7.0 compared with iontophoresis of the isolated drugs. Therefore, applying iontophoresis to a semisolid formulation of this drug combination at pH 7.0 can serve as a needle-free strategy to speed the onset and prolong the duration of buccal anesthesia. (C) 2015 Elsevier B.V. All rights reserved. (AU)

• FAPESP's process: 13/12174-3 - Study of resorbable polymers: the effect of degradation and erosion on dye release
• Grantee: Renê Oliveira Do Couto
• Support Opportunities: Scholarships abroad - Research Internship - Doctorate
• FAPESP's process: 12/05644-0 - Development of mucoadhesive semisolid systems for anesthetic release and iontophoresis application on the buccal cavity
• Grantee: Camila Cubayachi
• Support Opportunities: Scholarships in Brazil - Master