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Investigating Transdermal Delivery of Vitamin D3

Abstract

Transdermal delivery of therapeutic amounts of vitamin D3 is proposed to overcome its variable oral bioavailability, especially for people who suffer from fat malabsorption. The main challenge for this delivery route is to overcome the barrier properties of skin, especially for very lipophilic compounds such as vitamin D3. In this study, the effect of different penetration enhancers, such as oleic acid, dodecylamine, ethanol, oleic acid in propylene glycol, isopropyl myristate, octyldodecanol, and oleyl alcohol in propylene glycol were evaluated in vitro for their effectiveness in delivering vitamin D3 through polyamide filter, polydimethylsiloxane membrane, and porcine skin. A diffusion cell was used to study the transdermal permeability of vitamin D3. Ointment formulations of vitamin D3 were prepared containing the most widely used penetration enhancers, oleic acid, and dodecylamine. The ointment containing oleic acid as chemical penetration enhancer did not improve delivery compared to control. On the other hand, the formulation containing dodecylamine as a penetration enhancer did improve the transdermal delivery of vitamin D3. However, statistical significance and an amount high enough for nutritional supplementation purposes were reached only when the skin was pretreated with 50% ethanol. In these conditions, the ointment delivered an amount of 760-ng vitamin D3 per cm2 of skin. The research shows promise that transdermal delivery could be an effective administration route for vitamin D3 when ethanol and dodecylamine are used as penetration enhancers.

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Acknowledgments

The authors would like to acknowledge funding from the Albany College of Pharmacy and Health Sciences (Scholarship of Discovery for FMM). The authors’ work was independent of the funders.

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The authors have no conflict of interest to declare.

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Correspondence to Florin Marcel Musteata.

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Alsaqr, A., Rasoully, M. & Musteata, F.M. Investigating Transdermal Delivery of Vitamin D3 . AAPS PharmSciTech 16, 963–972 (2015). https://doi.org/10.1208/s12249-015-0291-3

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  • DOI: https://doi.org/10.1208/s12249-015-0291-3

KEY WORDS

  • dodecylamine
  • ethanol
  • penetration enhancer
  • transdermal delivery
  • vitamin D3