Penetration of model hormones through the pericardium in simulated conditions in vivo

Abstract

The process of penetration of selected protein-peptide substances including insulin (INS), corticotropin (ACTH), prolactin (PRL) and albumin (reference protein) through the model membrane - pig pericardium was traced. These substances show a wide spectrum of therapeutic effects and diverse physicochemical properties (molecular weight, pI). The model substances penetrated the pericardium in simulated in vivo conditions from 1.0 mg / ml solutions. Based on the results obtained, pharmacokinetic parameters of the permeation process were determined - permeation rate (k), half-life (t_50%) and their pharmaceutical availability (AUC [0-24 h]). All tested model substances penetrate the pericardium to different degrees. Within 24 h, they penetrate from 16.8% of albumin to 98.9% of insulin. Corticotropin penetrates 43.8% and PRL 34.2%. The highest availability is achieved with insulin, followed by ACTH, PRL and the lowest content of albumin. The results obtained suggest that the higher molecular weight of model protein-peptide substances, the lower the pericardial penetration (R² = - 0.700) and availability (R² = - 0.600), and the longer the half-life (R² = 0.948).

Keywords: Hormones; Penetration; Pericardium.