Full-Thickness Intraoral Mucosa Barrier Models for In Vitro Drug-Permeation Studies Using Microneedles

Author(s)

Serpe, Luciano ^[1] ; Muniz, Bruno Vilela ^[1] ; dos Santos, Cleiton Pita ^[1] ; da Silva, Camila Batista ^[1] ; Volpato, Maria Cristina ^[1] ; Groppo, Francisco Carlos ^[1] ; Vianna Lopez, Renata Fonseca ^[2] ; Franz-Montan, Michelle ^[1]

Affiliation

^[1] Univ Estadual Campinas, Piracicaba Dent Sch, Dept Physiol Sci, Piracicaba, SP - Brazil

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

• Document type: Journal article
• Source: Journal of Pharmaceutical Sciences; v. 108, n. 5, p. 1756-1764, MAY 2019.
• Web of Science Citations: 1

Abstract

The use of permeation enhancers such as microneedles (MNs) to increase drug penetration across intraoral mucosa has increased in recent years. Permeation studies, commonly performed using vertical diffusion cells, are a well-established way to preview formulations and enhance their performance during the development stage. However, to our knowledge, the existing intraoral mucosa barrier models do not permit permeation using MN-pretreated mucosa due to their insufficient thickness. Therefore, the objective of this study was to develop a barrier model using thick palate tissues to perform in vitro permeation studies, with physical enhancement of the permeability of intraoral mucosa by pretreatment with MNs. The adapted Franz-type cells used in the permeation experiments were validated (cell dimensions and volume, sealing effectiveness, stirring and dissolution efficiency, temperature control, and establishment of uniaxial flux). Commercially available MNs were used in the palatal mucosa. Optical images of the mucosa were acquired to analyze the microperforations created. In vitro permeation studies were conducted with the MN-pretreated mucosa. This work presents a new in vitro method for the evaluation of MNs as permeation enhancers, with the aim of improving the absorption of drug formulations topically applied within the oral cavity. (c) 2019 American Pharmacists Association (R). Published by Elsevier Inc. All rights reserved (AU)

• FAPESP's process: 12/06974-4 - Development, biocompatibility and permeation studies on gel formulations of poly-epsilon-caprolactone nanocapsules containing local anesthetics
• Grantee: Michelle Franz Montan Braga Leite
• Support Opportunities: Research Grants - Young Investigators Grants
• FAPESP's process: 12/02492-5 - In vitro study of the microneedles system appicability for topical anesthesia in swine oral tissues.
• Grantee: Luciano Serpe
• Support Opportunities: Scholarships in Brazil - Doctorate
• FAPESP's process: 11/18113-0 - Development of methods to perform permeation studies of topical formulations for dentistry applications
• Grantee: Francisco Carlos Groppo
• Support Opportunities: Regular Research Grants