ABSTRACT
Podophyllotoxin (PPT) is a precursor for the synthesis of drugs against cancer and other diseases. The present sources of PPT (Sinopodophyllum hexandrum and Podophyllum peltatum) are endangered species, with PPT production highly dependent on their growing conditions. In connection with the identification of new sources of PPT, the present study aimed to recover PPT from Juniperus virginiana leaves via atmospheric or high pressure extraction methods with a focus on using eco-friendly solvents. PPT quantification was determined by UHPLC/HRMS/MS. A thorough study of conventional extraction was carried out to reveal the optimal conditions (solvent ethyl acetate at room temperature and a duration of 1 h) for maximizing the PPT recovery (about 30 mg/g of dry extract and 3 mg/g of dry initial plant material). Peleg's equation was applied for process kinetics modeling. The best PPT content in the final dry extract (42-45 mg/g of dry extract) was obtained by high pressure methods under supercritical (scCO2 with ethanol or ethyl acetate, 30 MPa, 50 °C and 100 min) or accelerated solvent extraction conditions (solvent ethyl acetate, 10.35 MPa, 20 °C and 3 cycles for 15 min). Seasonal stability and storage stability of the raw material were also determined. The present results have potential applications in the pharmacy for the delivery of PPT from juniper leaves.
ABSTRACT
The solubility behavior of the pharmaceutical materials in a supercritical fluid is very important to produce the micro/nano-sized drug particulates. In the current study, solubility of montelukast as a potential treatment of COVID-19, in supercritical carbon dioxide (SC-CO2) was considered under different sets of temperature (308–338 K) and pressure (12–30 MPa). The obtained solubilities were in the range of 0.4 × 10-6 to 6.12 × 10-5 at (338 K, 12 MPa) and (338 K, 30 MPa), respectively. Two approaches i) empirical equations (i.e., Sodeifian et al., Bartle et al., Chrastil and Bian et al., Mendez-Santiago and Teja (MST) and Jouyban et al. and ii) equations of state (i.e., Peng-Robinson (PR)) combined with van der Waals (vdW2) mixing rules, SAFT-VR Mie were applied to correlate the experimental solubility data. According to the results, it could be concluded that Chrastil and Bartle et al. models produced the best correlations with the average absolute relative deviation % of 10.28 and 10.81, respectively. In addition, PR and SAFT-VR Mie EoS could provide satisfactory results for SC-CO2 solubility of montelukast at 308 to 338 K. Eventually, the results were devised to estimate the vaporization (ΔHvap), solvation (ΔHsol) and total enthalpies (ΔHtotal) of the solution. © 2021 Elsevier B.V.
ABSTRACT
Nigella sativa (N. sativa) is an annual flowering plant that has been used as a traditional remedy for many centuries. The seed possesses a large variety of compounds with thymoquinone (TQ) considered its major but not sole bioactive constituent. Supercritical fluid extraction, geographical location, and oxidative status of N. sativa produces the highest yield of essential oil content including TQ. Thymoquinone is lipophilic, heat and light sensitive with low oral bioavailability and rapid elimination that have significantly inhibited its pharmacological development. Novel developments in nanoparticulate-based oral administration, nasal spray and transdermal delivery may allow the clinical development of N. sativa and TQ as therapeutic agents. Animal and human studies indicate a potential role of N. sativa seed oil and TQ for a diverse range of disease processes including hypertension, dyslipidaemia, type 2 diabetes mellitus, arthritis, asthma, bacterial and viral infections, neurological and dermatological disorders, as it belongs to the group of pan-assay interference compounds. This review outlines the pharmacological properties of N. sativa and TQ and their potential wide application for a large variety of human diseases. The paper will focus on recent studies of the anti-inflammatory and antiviral properties that make N. sativa and TQ promising therapeutic agents targeting contemporary inflammatory and infectious diseases including Covid 19.