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AAPS PharmSciTech

, Volume 19, Issue 5, pp 2418–2425 | Cite as

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

  • Gabriela Maria D’Angelo Costa
  • Claudinéia Aparecida Sales de Oliveira Pinto
  • Vânia Rodrigues Leite-Silva
  • André Rolim Baby
  • Maria Valéria Robles Velasco
Research Article

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.

KEY WORDS

penetration enhancers transdermal delivery skin permeation skin retention vitamin D3 

Notes

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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Copyright information

© American Association of Pharmaceutical Scientists 2018

Authors and Affiliations

  • Gabriela Maria D’Angelo Costa
    • 1
  • Claudinéia Aparecida Sales de Oliveira Pinto
    • 1
  • Vânia Rodrigues Leite-Silva
    • 2
  • André Rolim Baby
    • 1
  • Maria Valéria Robles Velasco
    • 1
    • 3
  1. 1.Department of PharmacyUniversity of São Paulo (USP)Sao PauloBrazil
  2. 2.Department of Exact and Earth SciencesUniversidade Federal de São Paulo (UNIFESP)DiademaBrazil
  3. 3.Faculty of Pharmaceutical SciencesUniversity of São PauloSao PauloBrazil

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