The mechanism of permeation of [‘4C]oleate into isolated rat adipocytes has been examined. The initial rates of uptake of the fatty acid were determined at 23 “C as a function of the concentration of unbound fatty acid in the medium. Under the conditions employed, the following observations were made. 1) The rates were maximal and linear for at least 15 s and were the same in the presence or ab...

We have found that an enzyme-modified cheese (EMC) inhibited the permeation of allergens such as ovalbumin (OVA), using Caco-2 cells as an in vitro intestinal epithelial model. In addition, NPWDQ (Asn-Pro-Trp-Asp-Gln, aa 107-111 of alphas(2)-casein) was isolated from EMC and identified as one of the responsible peptides for this inhibitory activity (Tanabe et al., J. Agric. Food Chem., (2007))....

preformulation studies on transdermal dosage forms involve liberal use of animal skin for assessing the permeation characteristics of drugs, influence of permeation enhancers, optimizing the formulation variables etc. the restricted availability of animal skin due to concerns regarding prevention of cruelty to animals has generated considerable interest in developing polymeric films for use as ...

Electrical measurements were carried out to investigate the contribution of chloroplast lipids to the passive proton permeability of both the thylakoid and inner-envelope membranes. Permeability coefficient and conductance to protons were measured for solvent-free bilayers made from monogalactosyldiglyceride:digalactosyldiglycerid: sulfoquinovosyldiglyceride:phosphatidylglycerol (2:1:0.5:0.5, w...

Ryanodine receptors (RyRs) are ion channels responsible for the fast release of Ca2+ from sarco/endoplasmic reticulum to cytosol and show a selectivity over monovalent cations. By utilizing recently developed multisite model in molecular dynamic simulations, we that multiple cations accumulate upper filter RyRs, small size high valence make it preferable K+ competition space this confined regio...

the purpose of this work was to study the effect of various permeation enhancers on the permeation of salbutamol sulphate (ss) buccal patches through buccal mucosa in order to improve the bioavailability by avoiding the first pass metabolism in the liver and possibly in the gut wall and also achieve a better therapeutic effect. the influence of various permeation enhancers, such as dimethyl sul...

Recent determination of the crystal structures of bacterial voltage-gated sodium (NaV) channels have raised hopes that modeling of the mammalian counterparts could soon be achieved. However, there are substantial differences between the pore domains of the bacterial and mammalian NaV channels, which necessitates careful validation of mammalian homology models constructed from the bacterial NaV ...

The aquaglyceroporin from Plasmodium falciparum (PfAQP) is a potential drug target for the treatment of malaria. It efficiently conducts water and other small solutes, and is proposed to intervene in several crucial physiological processes during the parasitic life cycle. Despite the wealth of experimental data available, a dynamical and energetic description at the single-molecule level of the...

Voltage-gated Cl- channels belonging to the ClC family exhibit unique properties of ion permeation and gating. We functionally probed the conduction pathway of a recombinant human skeletal muscle Cl- channel (hClC-1) expressed both in Xenopus oocytes and in a mammalian cell line by investigating block by extracellular or intracellular I- and related anions. Extracellular and intracellular I- ex...

Ethosomes can promote the penetration of lipophilic drugs into the skin, but the underlying mechanism is still unknown. The purpose of this study was to investigate the mechanism of transdermal permeation promotion of lipophilic drugs by ethosomes. The formulation of ethosomes was optimized using the Box-Behnken experimental design, in which Rhodamine B and 1-palmitoyl-2-{12-[(7-nitro-2-1,3-ben...