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Objectives To prepare a lyophilized saffron aqueous extract (SFE) and determine its chemical profile and serum and tissue pharmacokinetics after intravenous and oral administration to C57/Bl6J mice. Methods Lyophilized SFE was prepared, characterized using semi‐preparative HPLC and NMR analysis, and stability studies at room temperature, and was quantified for crocin content with an HPLC‐PDA method. After intravenous and oral administration of SFE (60 mg/kg, reconstituted with water for injection) to C57/Bl6J mice, crocetin (derived from in vivo crocin hydrolysis) serum and tissue levels (unconjugated and total) were measured with an HPLC‐PDA method and subjected to compartmental and non‐compartmental PK analysis. Key findings Saffron aqueous extract was rich in all‐trans‐crocin (27.8 ± 0.1% w/w) and stable for more than 15 months. One‐compartment PK model described crocetin's (unconjugated) kinetics after intravenous administration of SFE, while a first‐order kinetic parameter described the rate of crocetin biotransformation to crocetin metabolite (conjugated). Α οne‐compartment PK model with first‐order absorption described crocetin and crocetin's metabolite kinetics after SFE oral administration. Relative oral bioavailability was calculated at 1.17 for total crocetin. Tissue NCA PK analysis revealed extensive crocetin distribution to liver and kidneys. Conclusions SFE is a stable lyophilized extract rich in all‐trans‐crocin. The PK study allowed the estimation of basic PK parameters and the bioavailability of SFE’s main bioactive component, crocetin, after peros administration.

The essential oils isolated from the air-dried leaves of four Nigerian plants of Commiphora kerstingii Engl (Burseraceae), Mangifera indica L., (Anacardiaceae), Callitris glauca R. Br. ex R.T. Baker. et H.G. Smith (Cupressaceae) and Ficus mucosa Welw. ex Ficalho (Moraceae), were analyzed for their constituents by GC and GC/MS. The volatile oil of Com. kerstingii contained (Z)-a-bisabolene (34.9%), b-bisabolene (9.3%), linalool (8.7%) and trans-a-bergamotene (7.9%) as the major constituents. On the other hand, the leaf oil of M. indica possessed a considerable proportion of a-gurjunene (23.6%), b-selinene (20.6%), b-caryophyllene (11.2%) and a-humulene (10.8%), while C. glauca had an abundance of a-pinene (19.6%) and limonene (13.1%). In addition, b-caryophyllene (37.0%), ethyl octanoate (14.9%) and methyl octanoate (8.3%) were the compounds occurring in higher percentages in the leaf oil of F. mucosa.

The effect of the lipophilic extract of S. willeana and three terpenoids isolated therefrom, camphor, lupeol and oleanolic acid, on oxazolone-induced hypersensitivity was evaluated. The extract reduced the ear edema by 46% at 24 h after challenge. All three terpenoids inhibited the edema and suppressed cytokines release at different rates. Lupeol inhibited the swelling by over 50% and reduced the production of IL-1β by 62%. Camphor caused inhibition of the efferent phase (45% inhibition at 72 h) and the levels of IL-1β, IL-4 and TNF-α (around 80% inhibition). Oleanolic acid diminished moderately the reaction and the levels of IL-4 and TNF-α. We also demonstrated that the three terpenoids inhibited human T-lymphocytes proliferation in a concentration-dependent manner and induced their apoptosis. Thus, these terpenoids could be considered anti-inflammatory constituents of S. willeana.

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