Unit:
Κατεύθυνση Φαρμακευτική ΤεχνολογίαLibrary of the School of Science
Supervisors info:
Γεωργία Βαλσαμή, Αναπληρώτρια καθηγήτρια, Τμήμα Φαρμακευτικής, Εθνικό και Καποδιστριακό Πανεπιστήμιο Αθηνών
Original Title:
In vitro ρινική διαπέραση της κροκίνης και σαφρανάλης ως συστατικά εκχυλισμάτων των στιγμάτων του φυτού Crocus sativus
Translated title:
In vitro transport of crocin and safranal from saffron extracts across rabbit nasal mucosa
Summary:
Introduction: Saffron, the dried stigma of Crocus sativus L., is a medicinal plant known for its antioxidant properties. It contains significant active components (crocin, safranal) with potential action against Alzheimer’s disease. For this purpose, it would be interesting the administration of a form of nasal powder, for possible direct into the brain delivery and specifically, a form of agglomerates.
Purpose: The formulation of dried saffron water extracts (SFE) in order to obtain a form of nasal powders and in addition, the in vitro evaluation of the nasal permeation of crocin and safranal using both artificial membranes and rabbit nasal mucosa as barrier and Franz- type diffusion cells.
Methods: Saffron stigmata macerated in HPLC grade water for three days at 40C. The obtained SFE was filtered, frozen, lyophilized (SFLE) or spray dried (SFSDE). Excipient microparticles of mannitol and lecithin (92:8 w/w) prepared by spray drying blended with the SFLE and SFSDE in a mass ratio of 90:10 and agglomerated using two sieves of 850 and 106 microns for 40 minutes. The content of SFLE, SFSDE and the agglomerates in crocin and safranal was quantified with HPLC-UV analysis. In addition, the nasal permeation of crocin and safranal was evaluated using Franz diffusion cells with either regenerated cellulose Membrane (MWCO 12 KDa) or rabbit nasal mucosa, using in the donor compartment SFE in solid formulations and also reconstituted in water.
Results and Conclusions: In the saffron water dried extracts crocin’s content was around 27% and safranal’s 0.32% w/w. The alcoholic extract was found to have very low content of safranal and crocin content around 8%. The agglomeration procedure was successful using the spray dried extract (SFSDE), as the extract particles might be more similar to the excipient microparticles in size. The permeability of safranal from either artificial membrane or rabbit mucosa was problematic. The in vitro transport rate of crocin of the solid formulations across rabbit nasal mucosa was much higher than that obtained with the reconstituted in water SFLE in the donor compartment. In addition, crocin exhibits comparable in vitro nasal permeability from both SFLE and SFSD and the corresponding agglomerates. There was no difference in permeation between the agglomerates made with the SFSD compared to those made with the SFLE. The highest permeation was observed for the SFSD and SFLE, mainly because they lead to higher crocin concentrations in contact with the mucosa. Finally, a small difference, although not significant, exists between the two extracts, with the SFSDE showing higher permeation, which may depend on different dissolution rates.
Main subject category:
Science
Other subject categories:
Pharmaceutical technology
Keywords:
crocin, safranal, in vitro transport, nasal delivery, Crocus sativus
Number of references:
122
File:
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ΚΡΟΚΟΣ ΚΟΖΑΝΗΣ- ΑΝΝΑ- draft-final.pdf
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File access is restricted only to the intranet of UoA.
