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Ethosomes and organogels for cutaneous administration of crocin

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Abstract

The present study describes the production and characterization of phosphatidylcholine based ethosomes and organogels, as percutaneous delivery systems for crocin. Crocin presence did not influence ethosome morphology, while the drug slightly increased ethosome mean diameter. Importantly, the poor chemical stability of crocin has been found to be long controlled by organogel. To investigate the performance of phosphatidylcholine lipid formulations as crocin delivery system, in vivo studies, based on tape stripping and skin reflectance spectrophotometry, were performed. Tape stripping results suggested a rapid initial penetration of crocin exerted by the organogel, probably due to a strong interaction between the peculiar supramolecular aggregation structure of phospholipids in the vehicle and the lipids present in the stratum corneum and a higher maintenance of crocin concentration in the case of ethosomes, possibly because of the formation of a crocin depot in the stratum corneum. Skin reflectance spectrophotometry data indicated that both vehicles promoted the penetration of crocin through the skin, with a more rapid anti-inflammatory effect exploited by ethosomes, attributed to an ethanol pronounced penetration enhancer effect and to the carrier system as a whole.

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Abbreviations

ETHO:

Ethosomes

ORG:

Organogels

CRO:

Crocin

X GUM:

Xanthan gum

PC:

Phosphatidylcholine

MED:

Minimal erythemal dose

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Acknowledgments

The authors are grateful to Sarah Villebrun from Institut Galien Paris-Sud, Châtenay-Malabry, France for rheological characterization.

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Authors and Affiliations

  1. Department of Life Sciences and Biotechnologies, University of Ferrara, I-44121, Ferrara, Italy

    Elisabetta Esposito, Gabriella Pavoni & Rita Cortesi

  2. Macromolecular Chemistry II, University of Bayreuth, Bayreuth, Germany

    Markus Drechsler

  3. Institut Galien Paris-Sud (CNRS UMR 8612), Faculté de Pharmacie, Université Paris-Sud, Orsay, France

    Nicolas Huang

  4. Department of Drug Science, University of Catania, I-95125, Catania, Italy

    Debora Santonocito & Carmelo Puglia

Authors
  1. Elisabetta Esposito
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  2. Markus Drechsler
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  4. Gabriella Pavoni
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  5. Rita Cortesi
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  7. Carmelo Puglia
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Correspondence to Elisabetta Esposito or Rita Cortesi.

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All procedures performed in studies involving human participants were in accordance with the 1964 Helsinki declaration and its later amendments or comparable ethical standards.

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A: Aspect of ethosome (ETHO); ethosome prepared in the presence of crocin (ETHO-CRO); ethosome prepared in the presence of crocin and added with x-gum 1 %, w/w ETHO-CRO-x-gum B: Aspect of organogels obtained with 1:1 and 2:1 molar water to PC ratios (1:1 [water]/[PC]; 2:1 [water]/[PC]) and ORG-CRO: organogel prepared with 3:1 molar water to PC ratio in the presence of crocin (ORG-CRO) (GIF 259 kb)

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Esposito, E., Drechsler, M., Huang, N. et al. Ethosomes and organogels for cutaneous administration of crocin. Biomed Microdevices 18, 108 (2016). https://doi.org/10.1007/s10544-016-0134-3

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  • DOI: https://doi.org/10.1007/s10544-016-0134-3

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