BACKGROUND The increase in C-reactive protein (CRP) during oral conjugated equine estrogen (CEE) may explain the initial excess of cardiovascular disease observed in clinical studies. Because the effect of transdermal estradiol (E2) on CRP is unclear, we compared CRP changes after 6 and 12 months of transdermal E2 and oral CEE in a randomized 2x2 retinoid-placebo trial. METHODS AND RESULTS A ...

To clarify pharmacological usefulness of transdermal oxybutynin in the therapy of overactive bladder, we have characterized muscarinic receptor binding in rat tissues with measurement of plasma concentrations of oxybutynin and its metabolite N-desethyl-oxybutynin (DEOB) and salivation after transdermal oxybutynin compared with oral route. At 1 and 3 h after oral administration of oxybutynin, th...

The present study was undertaken to develop a suitable transdermal matrix patch of ketorolac tromethamine with different proportions of polyvinyl pyrrolidone (PVP) and ethyl cellulose (EC) using a D-optimal mixture design. The prepared transdermal patches were subjected to different physicochemical evaluation. The surface topography of the patches was examined by scanning electron microscopy (S...

The use of Acetyl Salicylic Acid (ASA) in the secondary prevention of cardio vascular diseases is well known. Orally administered ASA is rapidly metabolized to its principal metabolite Salicylic Acid (SA) in the gastrointestinal fluids, during absorption in the intestine and liver. ASA, and not its hydrolysis product SA, which exhibits antithrombotic activity. Transdermal delivery of acetylsali...

It is clear that many drug transporters (both ABCs and SLCs) are present in the human skin. Different in vitro skin models can be used to investigate the role of drug transporters in the skin despite quantitative differences in expression profile across species. P-gp was shown to have an important influence on transdermal drug absorption in the skin and to function in “absorptive” transport, ca...

Purpose: To develop transdermal patches of meloxicam (MLX) using chitosan and hydroxypropyl methylcellulose (HPMC) and polyvinyl alcohol (PVA) as hydrophilic polymers, polyamido amine (PAMAM) dendrimer as a permeation enhancer, and dibutyl pthalate as a plasticizer Methods: The patches were prepared by solvent casting evaporation technique using 3-factor, 3-level Box-Behnken design. The patches...

Transdermal drug delivery of ibuprofen, a well known NSAID has sparked considerable research interest in the recent years. The hydrophobic nature of the drug as well as its water insolubility is a significant deterrent for its uptake through the skin and its bioavailability at the targeted site of pain/inflammation. This work addresses both concerns through a novel microemulsion formulation syn...

The body of scientific literature on transdermal alcohol testing dates back almost 70 years. The first viable method enabling this knowledge appeared in the 1980s in the form of an alcohol “sweat-patch”. Recently, transdermal alcohol monitoring bracelets have been used to measure transdermal vapor alcohol. Based on published research in this field, one can conclude that measuring alcohol transd...

Plasma fentanyl concentrations were measured during and after transdermal fentanyl delivery in groups of patients undergoing general surgery. At 8 and 12 h, concentrations did not differ from those observed in a matched group of patients receiving fentanyl by i.v. infusion. At 24 h, concentrations were significantly lower in one of the transdermal groups. Plasma fentanyl clearance did not diffe...