ABSTRACT
Transdermal drug delivery is an administration route which can avoid the first-pass effect,maintain steady plasma concentrations and enhance bioavailability. Drug transporting through the skin by passage through the stratum corneum leads to the viable epidermis and the dermis.With the development of the computer technology,many mathematical models for predic-ting the absorption of drugs have been built according to physical and chemical properties of drugs and physiological characteristics of each skin layer.This article presented provides a summary of the progress of mathematical models for predicting percutaneous absorption of drugs.
ABSTRACT
[ ABSTRACT ] AIM: To investigate the effect of advanced oxidation protein product-human serum albumin ( AOPP-HSA) at different concentrations on the permeability of human umbilical vein endothelial cell ( HUVEC) monolayer and the protective effect of NADPH oxidase inhibitor diphenyleneiodonium ( DPI ) against AOPP-HSA exposure. METHODS: Cultured HUVECs were exposed to 200 mg/L HSA (control) or AOPP-HSA (50, 100 and 200 mg/L).The permeability of the endothelial monolayer was assessed by measuring CMFDA-labeled THP-1 cells across the endothelial cells.The cultured HUVECs were treated with HSA (200 mg/L), AOPP-HSA (200 mg/L), or AOPP-HSA (200 mg/L)+DPI (100 μmol/L), and the activation of NADPH oxidase, endothelial monolayer permeability and cytoskeleton rear-rangement were evaluated.RESULTS: AOPP-HSA increased the permeability of the endothelial cell monolayer, and AOPP-HSA at 200 mg/L significantly increased the phosphorylation level of NADPH oxidase in the cells.Treatment with 100 μmol/L DPI obviously attenuated AOPP-HSA-induced NADPH oxidase activation, the increase in the permeability of the cell monolayer and the cytoskeleton rearrangement.CONCLUSION: AOPP-HSA increases the hyperpermeability of HUVEC monolayer via the phosphorylation of NADPH oxidase, and the NADPH oxidase inhibitor DPI reverses such effects.