Title:Ex vivo Skin Permeation Evaluation of An Innovative Transdermal Vehicle Using Nimesulide and Piroxicam as Model Drugs
Volume: 14
Issue: 4
Author(s): Rafaela de Oliveira Pereira, Taize Carla Costa Pelisson e Silva, Anderson de Oliveira Ferreira, Marcos Antonio Fernandes Brandao, Nadia Rezende Barbosa Raposo and Hudson Caetano Polonini*
Affiliation:
- Faculdade de Ciências Médicas e da Saúde de Juiz de Fora (SUPREMA), Juiz de Fora,Brazil
Keywords:
Nimesulide, NSAIDS, permeation studies, piroxicam, stratum corneum, transdermal vehicle, viable epidermis.
Abstract: Background: The transdermal dosage forms presented a limited usage for a long time, for it
was believed that the stratum corneum, the outermost layer of epidermis, made it impracticable the
permeation of medications through the skin. Studies exploring this area came up with strategies to
overcome this barrier; for example, creating a transdermal vehicle to facilitate the drug absorption.
Objective: This study aimed to evaluate a new transdermal vehicle through the comparison of its permeation
profile and the profile of commercial products, using nimesulide and piroxicam, non steroidal
anti-inflammatory drugs.
Methods: Four different products were evaluated: nimesulide and piroxicam compounded with the new
vehicle (emulsion) and commercial nimesulide and piroxicam gels. Ex vivo permeation experiments
using Franz-type diffusion cell equipment were conducted, using human skin as membrane. For
evaluation of permeated active pharmaceutical ingredients concentrations, we performed quantification
from the receptor solution, stratum corneum and viable epidermis + dermis, through high-performance
liquid chromatography analyses.
Results: The new vehicle promoted increased permeation of active pharmaceutical ingredients through
the viable epidermis and dermis, when compared to commercial products, but the stratum corrneum
continued to keep the highest retention.
Conclusion: The innovative vehicle was capable of enhancing the transdermal absorption of active
pharmaceutical ingredients from the compounded formulations, thus, demonstrating the capability
thereof to improve the permeability of active pharmaceutical ingredients by transdermal use.