Effect of Complexes and Microemulsions on the Permeability of Drugs: Determination Using a New Biomimetic Artificial Membrane

PONCE PONTE MICAELA

AAPS PHARMSCITECH

SPRINGER

Lugar: Berlin; Año: 2018 vol. 19 p. 2629 - 2629

1530-9932

he aim of this work was to predict the permeability of two model drugs,sulfamerazine (SMR) and indomethacin (INM), and to determine the effect on their apparent permeabilities by complexation with cyclodextrins and/or meglumine or incorporation in microemulsions. Permeation experiments were performed using two-chamberdiffusion cells with a new composition of bio-mimetic membrane composed of 80% of Lipoid® S100 and 20% of cholesterol in n-octanol 10% w/w solution, at 37 ± 0.5°C and 14,000 rpm. The predictive capacity of the permeability of passive diffusion absorbed compounds was evaluated using 20 drug standards and showed an exponential correlation between the apparent permeability coefficients (Papp) and the fraction absorbed percentages in humans (Fa%), with an R2 value of 0.67942 and a constant value of 4.1 ± 0.8. SMR and INM were classified as Class II and I, respectively, according to the BiopharmaceuticalClassification System. These drugs were complexed and incorporated in micr