Kamoun Jannet, Krichen Fatma, Koubaa Imed, Zouari Nacim, Bougatef Ali, Abousalham Abdelkarim, Aloulou Ahmed
University of Sfax, National Engineering School of Sfax, Laboratory of Biochemistry and Enzymatic Engineering of Lipases, Sfax 3038, Tunisia.
Univ Lyon, Université Lyon 1, Institut de Chimie et de Biochimie Moléculaires et Supramoléculaires (ICBMS), UMR 5246 CNRS, Génie Enzymatique, Membranes Biomimétiques et Assemblages Supramoléculaires (GEMBAS), Bât Raulin, 43 Bd du 11 Novembre 1918, F-69622 Villeurbanne Cedex, France.
Heliyon. 2021 Apr 7;7(4):e06717. doi: 10.1016/j.heliyon.2021.e06717. eCollection 2021 Apr.
Lipid-based drug delivery systems are widely used for enhancing the bioavailability of poorly water-soluble drugs. However, following oral intake, lipid excipients often undergo gastrointestinal lipolysis, which drastically affects drugs solubility and bioavailability. That's why developing new lipid excipients which are resistant to digestion would be of great interest. We studied here the potential role of the unconventional Chinese star anise whole seedpod oil (CSAO) as an alternative multifunctional lipid excipient. Pancreatic lipase-mediated digestion of the extracted crude oil emulsion was assessed . Pancreatic lipase, being a strict -1,3-regioselective lipase, showed a high (16-fold) olive oil to CSAO activity ratio, which could be attributed to fatty acids composition and triglycerides intramolecular structure. For the sake of comparison, the non-regioselective lipase Novozyme® 435 exhibited higher activity than pancreatic lipase on CSAO emulsion, perhaps due to its ability to release fatty acids from the internal -2 position of TAGs. Apart counteracting lipolysis, CSAO oil also showed additional biopharmaceutical benefits including moderate antioxidant and antihypertensive activities. Altogether, these findings highlight for the first time the potential use of star anise unconventional whole seedpod oil as a multifunctional lipid excipient for the development of new lipid formulations.
基于脂质的药物递送系统被广泛用于提高难溶性药物的生物利用度。然而，口服摄入后，脂质辅料常常会经历胃肠道脂解作用，这会极大地影响药物的溶解度和生物利用度。这就是为什么开发抗消化的新型脂质辅料会备受关注。我们在此研究了非常规的中国八角全籽荚油（CSAO）作为一种替代性多功能脂质辅料的潜在作用。评估了胰脂肪酶介导的提取原油乳液的消化情况。胰脂肪酶作为一种严格的1,3-区域选择性脂肪酶，显示出较高的（16倍）橄榄油与CSAO的活性比，这可归因于脂肪酸组成和甘油三酯的分子内结构。为作比较，非区域选择性脂肪酶诺维信®435在CSAO乳液上表现出比胰脂肪酶更高的活性，这可能是由于其能够从TAGs的内部-2位释放脂肪酸。除了抵消脂解作用外，CSAO油还显示出其他生物制药益处，包括适度的抗氧化和降压活性。总之，这些发现首次突出了八角非常规全籽荚油作为开发新型脂质制剂的多功能脂质辅料的潜在用途。
