Efficient Transdermal Delivery of Benfotiamine in an Animal Model

Abstract

We designed a transdermal system to serve as a delivery platform for benfotiamine utilizing the attributes of passive penetration enhancing molecules to penetrate through the outer layers of skin combined with the advance of incorporating various peripherally-acting vasodilators to enhance drug uptake. Benfotiamine, incorporated into this transdermal formulation, was applied to skin in an animal model in order to determine the ability to deliver this thiamine pro-drug effectively to the sub-epithelial layers. In this proof of concept study in guinea pigs, we found that a single topical application of either a solubilized form of benfotiamine (15 mg) or a microcrystalline suspension form (25 mg) resulted in considerable increases of the dephosphorylated benfotiamine (S-benzoylthiamine) in the skin tissue as well as in significant increases in the thiamine and thiamine phosphate pools compared to control animals. The presence of a ~8000x increase in thiamine and increases in its phosphorylated derivatives in the epidermis

Development of a novel method for the bioanalysis of benfotiamine and sulbutiamine in cancer cells

“…3C and D). As shown in many studies, [9][10][11][12] these analogs easily diffuse across plasma membranes leading to increases in intracellular thiamine levels. Therefore, this result suggested that the thiamine analogs were converted into thiamine aer crossing the cell membrane.…”

“…Benfotiamine and sulbutiamine have excellent bioavailability [5][6][7][8]10,11 and are known to easily cross cell membranes and increase intracellular thiamine levels. [9][10][11][12] Benfotiamine, an S-acyl derivate of thiamine, was discovered to stimulate transketolase (TKT) activity involved in glucose metabolism and prevent diabetic nephropathy in a similar manner to high-dose thiamine. [13][14][15] Sulbutiamine, a dimer of two modied thiamine molecules, is widely used clinically as a treatment for brain function including memory disorders and asthenia.…”