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Pharmacokinetics of the transdermal delivery of benfotiamine

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Abstract

Aims

Accumulation of advanced glycation endpoints is a trigger to the development of diabetic peripheral neuropathy, which is a common complication of diabetes. Oral administration of benfotiamine (BFT) has shown some preclinical and clinical promise as a treatment for diabetic peripheral neuropathy. The purpose of this study was to evaluate the method of transdermal delivery of BFT as a possible, viable route of administration for the treatment of diabetic peripheral neuropathy.

Methods

A single application of 10 mg of BFT was given to guinea pigs topically. The levels of thiamine (T), thiamine monophosphate, thiamine diphosphate, S-benzoylthiamine and BFT were measured in the blood, skin and muscle at different time points within 24 h.

Results

At the 24-h time point, following the single BFT dose, the T level was increased 10× in the blood, more than 7× in the skin and almost 4× in the muscle compared to the untreated animals. The total T content (total) was increased 7× in the blood, 17× in the skin and 3× in the muscle compared to the untreated animals.

Conclusions

This strong increase in the tissue levels of T and the associated metabolic derivatives levels found in the blood and local tissues following a single dose indicate that topically applied BFT may be a viable and advantageous delivery method for the treatment of diabetic peripheral neuropathy.

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Acknowledgments

All funding for this research was provided by BioChemics, Inc.

Conflict of interest

The authors declare that they have no conflict of interest.

Ethical standard

All human and animal studies have been performed in accordance with the ethical standards of the responsible committee on animal experimentation (institutional and national) and with the Helsinki Declaration of 1975, as revised in 2008 (5).

Informed consent

Informed consent was obtained from all patients for being included in the study.

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Authors and Affiliations

  1. BioChemics Inc., 99 Rosewood Drive, Suite 270, Danvers, MA, 01923-4537, USA

    Zhen Zhu & Gyula Varadi

  2. Intrepid Life Sciences, Andover, MA, 01810, USA

    Stephen G. Carter

Authors
  1. Zhen Zhu
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  2. Gyula Varadi
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  3. Stephen G. Carter
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Correspondence to Zhen Zhu.

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Zhu, Z., Varadi, G. & Carter, S.G. Pharmacokinetics of the transdermal delivery of benfotiamine. Acta Diabetol 53, 317–322 (2016). https://doi.org/10.1007/s00592-015-0776-2

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  • DOI: https://doi.org/10.1007/s00592-015-0776-2

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