Delivery and stability of LHRH and Nafarelin in human skin: the effect of constant/pulsed iontophoresis.

Poor absorption and stability of peptides are the major obstacles concerning the development of therapeutically relevant iontophoretic devices for the transdermal delivery of peptides. The present study examined the impact of constant and pulsed (direct/alternating) current profiles on the transport and stability of two decapeptides LHRH and Nafarelin. The stability of these peptides was studied in a physiological buffer solution, with electrical current, and when the peptide solution was exposed to the stratum corneum or to the epidermal/dermal side of human skin.

Drug adsorption in human skin: a streaming potential study.

The objective of this study was to investigate the drug adsorption process in human skin using in vitro streaming potential measurements. Streaming potential is an electrokinetic phenomenon, which reflects both the charge density and the pore size of a membrane. Thus, the adsorption of charged solutes on the pore walls can be detected as a change of streaming potential, viz.

Effects of various absorption enhancers on transport of clodronate through Caco-2 cells.

The major disadvantage concerning clinical use of bishosphonate drugs, like clodronate, is their poor and variable absorption after oral administration. The objective of this study was to assess the effects of four different absorption enhancers-palmitoyl carnitine chloride (PCC), N-trimethyl chitosan chloride (TMC), sodium caprate (C10), and ethylene glycol-bis(beta-aminoethyl ether)-N,N,N',N'-tetraacetic acid (EGTA)-on the transport of clodronate using Caco-2 cell culture model. The transport experiments were performed in a normal (1.

Permeability profiles of M-alkoxysubstituted pyrrolidinoethylesters of phenylcarbamic acid across caco-2 monolayers and human skin.

Purpose: The purpose of the present research was to study 10 m-alkoxysubstituted pyrrolidinoethylesters of phenylcarbamic acid-potential local anesthetics. The relationships between the structure of the molecule, its physicochemical parameters (log D(oct), log k, R(M), solubility) were correlated to the permeability data obtained from permeation experiments in Caco-2 monolayers and excised human skin in vitro.

Methods: The extent and mechanism(s) of permeability of the series were studied through a Caco-2 monolayer in the apical-to-basolateral (a-b) and basolateral-to-apical (b-a) directions.