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Planta Med 2019; 85(03): 258-265
DOI: 10.1055/a-0732-5757
Formulation and Delivery Systems of Natural Products
Original Papers
Georg Thieme Verlag KG Stuttgart · New York

Nanotechnological Approach to Increase the Antioxidant and Cytotoxic Efficacy of Crocin and Crocetin

Carmelo Puglia
1   Department of Drug Sciences, University of Catania, Catania, Italy
,
Debora Santonocito
1   Department of Drug Sciences, University of Catania, Catania, Italy
,
Teresa Musumeci
1   Department of Drug Sciences, University of Catania, Catania, Italy
,
Venera Cardile
2   Department of Biomedical and Biotechnological Sciences, University of Catania, Catania, Italy
,
Adriana Carol Eleonora Graziano
2   Department of Biomedical and Biotechnological Sciences, University of Catania, Catania, Italy
,
Loredana Salerno
1   Department of Drug Sciences, University of Catania, Catania, Italy
,
Giuseppina Raciti
1   Department of Drug Sciences, University of Catania, Catania, Italy
,
Lucia Crascì
1   Department of Drug Sciences, University of Catania, Catania, Italy
,
Anna Maria Panico
1   Department of Drug Sciences, University of Catania, Catania, Italy
,
Giovanni Puglisi
1   Department of Drug Sciences, University of Catania, Catania, Italy
› Author Affiliations
Further Information

Publication History

received 03 July 2018
revised 20 August 2018

accepted 27 August 2018

Publication Date:
11 September 2018 (online)

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Abstract

Crocin and crocetin are two interesting constituents of saffron (Crocus sativus) that possess important biological activities. Their use as therapeutic agents is strongly compromised by a scarce stability, poor absorption, and low bioavailability. Therefore, to improve these unfavorable features, the aim of the present work has been to apply a nanotechnological approach based on the formulation of solid lipid nanoparticles containing crocin and crocetin. Solid lipid nanoparticles were formulated according to crocin and crocetin chemical properties, using a variation of the quasi-emulsion solvent diffusion method to formulate crocin-solid lipid nanoparticles, while crocetin-solid lipid nanoparticles were prepared following the solvent diffusion method. Morphology and dimensional distribution of solid lipid nanoparticles have been characterized by differential scanning calorimetry and photon correlation spectroscopy, respectively, while the effect of drug incorporation versus time has been studied by Turbiscan technology. In order to verify the role of the nanotechnological approach on the biological activities of crocin and crocetin, the antioxidant and antiproliferative effects of these carotenoids once incorporated in lipid nanoparticles have been evaluated. For this aim, the oxygen radical absorbance capacity assay and the MTT test were used, respectively.

The results pointed out the formulation of nanometric dispersions endowed with high homogeneity and stability, with an encapsulation efficiency ranging from 80 (crocetin-solid lipid nanoparticles) to 94% (crocin-crocetin). The oxygen radical absorbance capacity assay evidenced an interesting and prolonged antioxidant activity of crocin and crocetin once encapsulated in solid lipid nanoparticles, while the nanoencapsulation strategy showed a different mechanism in ameliorating the cytotoxic effect of these two substances.

Key words

Crocus sativus - Iridaceae - solid lipid nanoparticles - Turbiscan analysis - antioxidant - cytotoxic
 

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