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Is Vitamin D3 Transdermal Formulation Feasible? An Ex Vivo Skin Retention and Permeation

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Abstract

Vitamin D3 supplementation is important to prevent and treat hypovitaminosis that is a worldwide public health issue. Most types of supplementation are by oral route or fortification foods. The alternative route must be investigated, as transdermal route, for people with fat malabsorption or other diseases that impair the absorption of vitamin D3. This study focused on verifying the feasibleness of vitamin D3 skin retention and permeation with the presence of chemical penetration enhancers (soybean lecithin, isopropyl palmitate, propylene glycol, ethoxydiglycol, and cereal alcohol) at different pharmaceutical forms (gel and cream) through a human skin. The integrity of skin was evaluated by transepidermal water loss (TEWL) during the skin retention and permeation test. The combination of chemical penetration enhancers presented in cream did not compromise the skin, different from the gel that association of cereal alcohol and propylene glycol compromised the skin in 24 h. Gel formulation showed vitamin D3 detection at stratum corneum in 4 h and at epidermis and dermis in 24 h. Vitamin D3 demonstrated an affinity with the vehicle in the cream formulation and was detected at the skin surface. No active was found at receptor fluid for both formulations. In conclusion, the vitamin D3 did not indicate feasibleness for transdermal use probably due to its physical-chemical characteristics such as high lipophilicity since it was not permeated through a human skin. Nevertheless, the transdermal route should be continuously investigated with less lipophilic derivates of vitamin D3 and with different combination of penetration enhancers.

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Acknowledgments

We would like to acknowledge the UNIFESP for the partnership and USP for all academic support. This study was supported by the Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq—no. 159265/2015-0 (GMDC)).

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Authors and Affiliations

  1. Department of Pharmacy, University of São Paulo (USP), Sao Paulo, Brazil

    Gabriela Maria D’Angelo Costa, Claudinéia Aparecida Sales de Oliveira Pinto, André Rolim Baby & Maria Valéria Robles Velasco

  2. Department of Exact and Earth Sciences, Universidade Federal de São Paulo (UNIFESP), Diadema, Brazil

    Vânia Rodrigues Leite-Silva

  3. Faculty of Pharmaceutical Sciences, University of São Paulo, 580, Prof. Lineu Prestes Avenue Bloco 13, Sao Paulo, SP, 05508-000, Brazil

    Maria Valéria Robles Velasco

Authors
  1. Gabriela Maria D’Angelo Costa
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  2. Claudinéia Aparecida Sales de Oliveira Pinto
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  3. Vânia Rodrigues Leite-Silva
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Correspondence to Maria Valéria Robles Velasco.

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D’Angelo Costa, G.M., Sales de Oliveira Pinto, C.A., Rodrigues Leite-Silva, V. et al. Is Vitamin D3 Transdermal Formulation Feasible? An Ex Vivo Skin Retention and Permeation. AAPS PharmSciTech 19, 2418–2425 (2018). https://doi.org/10.1208/s12249-018-1065-5

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  • DOI: https://doi.org/10.1208/s12249-018-1065-5

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