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Nano-encapsulation of Vitamin D3 Active Metabolites for Application in Chemotherapy: Formulation Study and in Vitro Evaluation

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Abstract

Purpose

Calcitriol (1,25-dihydroxyvitamin D3), the active metabolite of vitamin D3, is a potential anticancer agent but with high risk of hypercalcemia which limits the achievement of effective serum concentrations. Thus, calcitriol targeting delivery by nanoparticles may present a good solution.

Methods

Vitamin D3 active metabolites were encapsulated into polymeric nanoparticles and different formulation parameters were tested. The growth inhibitory efficiency of these nanoparticles was carried out in vitro on human breast adenocarinoma cells (MCF-7).

Results

Using cholecalciferol (the inactive metabolite), different polymer and oil ratios were compared to select nanoparticles presenting high encapsulation efficiency and sustained release profile. Calcidiol/calcitriol loaded nanoparticles had good encapsulation efficiencies (around 90%) associated with sustained releases over 7 days and enhanced stability. Moreover, loaded nanoparticles showed similar growth inhibition to non-encapsulated metabolites of vitamin D3 on day 4 and higher activities on days 7 and 10 after treatment initiation.

Conclusion

The nano-encapsulation of vitamin D3 active metabolites may offer a new and potentially effective strategy for vitamin D3-based chemotherapy overcoming its actual limitations. The targeting delivery of vitamin D3 metabolites should be encouraged.

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Authors and Affiliations

  1. University Lyon, University Claude Bernard Lyon 1 Laboratoire d’Automatique et de Génie des Procédés, LAGEP UMR CNRS 5007, CPE-308 G, 43 bd. 11 Nov.1918, 69622, Villeurbanne, France

    Eyad Almouazen, Sandrine Bourgeois, Hatem Fessi & Stephanie Briançon

  2. Centre de Recherche en Cancérologie de Lyon, UMR INSERM U1052, CNRS 5286, 69000, Lyon, France

    Lars Petter Jordheim

  3. University Lyon 1, ISPB-School of Pharmacy, 69008, Lyon, France

    Sandrine Bourgeois, Lars Petter Jordheim, Hatem Fessi & Stephanie Briançon

Authors
  1. Eyad Almouazen
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  2. Sandrine Bourgeois
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  3. Lars Petter Jordheim
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  4. Hatem Fessi
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  5. Stephanie Briançon
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Correspondence to Sandrine Bourgeois.

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Almouazen, E., Bourgeois, S., Jordheim, L.P. et al. Nano-encapsulation of Vitamin D3 Active Metabolites for Application in Chemotherapy: Formulation Study and in Vitro Evaluation. Pharm Res 30, 1137–1146 (2013). https://doi.org/10.1007/s11095-012-0949-4

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  • DOI: https://doi.org/10.1007/s11095-012-0949-4

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