title: Nanostructured lipid dispersions for topical administration of crocin, a potent antioxidant from saffron (Crocus sativus L.).
abstract: Crocin, a potent antioxidant obtained from saffron, shows anticancer activity in in vivo models. Unfortunately unfavorable physicochemical features compromise its use in topical therapy. The present study describes the preparation and characterization of nanostructured lipid dispersions as drug delivery systems for topical administration of crocin and the evaluation of antioxidant and antiproliferative effects of crocin once encapsulated into nanostructured lipid dispersions. Nanostructured lipid dispersions based on monoolein in mixture with sodium cholate and sodium caseinate have been characterized by cryo-TEM and PCS. Crocin permeation was evaluated in vitro by Franz cells, while the oxygen radical absorbance capacity assay was used to evaluate the antioxidant activity. Furthermore, the antiproliferative activity was tested in vitro by the MTT test using a human melanoma cell line. The emulsification of monoolein with sodium cholate and sodium caseinate led to dispersions of cubosomes, hexasomes, sponge systems and vesicles, depending on the employed emulsifiers. Permeation and shelf life studies demonstrated that nanostructured lipid dispersions enabled to control both rate of crocin diffusion through the skin and crocin degradation. The oxygen radical absorbance capacity assay pointed out an interesting and prolonged antioxidant activity of crocin while the MTT test showed an increase of crocin cytotoxic effect after incorporation in nanostructured lipid dispersions. This work has highlighted that nanostructured lipid dispersions can protect the labile molecule crocin from degradation, control its skin diffusion and prolong antioxidant activity, therefore suggesting the suitability of nanostructured lipid dispersions for crocin topical administration.
authors.affiliation: Department of Life Sciences and Biotechnology, University of Ferrara, I-44121 Ferrara, Italy. Electronic address: ese@unife.it.
authors.forename: Elisabetta
authors.initials: E
authors.lastname: Esposito
authors.affiliation: Macromolecular Chemistry II, University of Bayreuth, Germany.
authors.forename: Markus
authors.initials: M
authors.lastname: Drechsler
authors.affiliation: Department of Life and Environmental Sciences, Università Politecnica delle Marche, I-60131 Ancona, Italy.
authors.forename: Paolo
authors.initials: P
authors.lastname: Mariani
authors.affiliation: Department of Drug Sciences, University of Catania, I-95125 Catania, Italy.
authors.forename: Anna Maria
authors.initials: AM
authors.lastname: Panico
authors.affiliation: Department of Biomedical Sciences, University of Catania, I-95125 Catania, Italy.
authors.forename: Venera
authors.initials: V
authors.lastname: Cardile
authors.affiliation: Department of Drug Sciences, University of Catania, I-95125 Catania, Italy.
authors.forename: Lucia
authors.initials: L
authors.lastname: Crascì
authors.affiliation: Department of Life and Environmental Sciences, Università Politecnica delle Marche, I-60131 Ancona, Italy.
authors.forename: Federica
authors.initials: F
authors.lastname: Carducci
authors.affiliation: Department of Biomedical Sciences, University of Catania, I-95125 Catania, Italy.
authors.forename: Adriana Carol Eleonora
authors.initials: ACE
authors.lastname: Graziano
authors.affiliation: Department of Life Sciences and Biotechnology, University of Ferrara, I-44121 Ferrara, Italy. Electronic address: crt@unife.it.
authors.forename: Rita
authors.initials: R
authors.lastname: Cortesi
authors.affiliation: Department of Drug Sciences, University of Catania, I-95125 Catania, Italy.
authors.forename: Carmelo
authors.initials: C
authors.lastname: Puglia
mesh_terms: D000287:Administration, Topical; D000975:Antioxidants / Q000737:chemistry / Q000494:pharmacology; D002338:Carotenoids / Q000737:chemistry / Q000494:pharmacology; D002364:Caseins / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D027622:Crocus / Q000737:chemistry*; D016503:Drug Delivery Systems / Q000379:methods*; D004655:Emulsions; D005989:Glycerides / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D008545:Melanoma / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D020358:Sodium Cholate / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000975:Antioxidants; D002364:Caseins; D004655:Emulsions; D005989:Glycerides; D002338:Carotenoids; C029036:crocin; C005953:monoolein; D020358:Sodium Cholate
keywords: Antioxidant; Chemical stability; Formulation; Materials science; Nanotechnology