Molecular Bio-computation and Drug Design Laboratory, School of Health Sciences, University of KwaZulu-Natal, Westville Campus, Durban, 4001, South Africa.
Cell Biochem Biophys. 2020 Sep;78(3):267-289. doi: 10.1007/s12013-020-00922-5. Epub 2020 Jun 5.
The pharmacological propensities of curcumin have been reported in a plethora of pre-clinical and clinical studies. However, innate attributes account for extremely low oral bioavailability which impedes its development as a therapeutic agent. Regardless, these drawbacks have not deterred researchers from optimizing its potentials. This review discussed the pharmacokinetic properties of curcumin relative to its outlook as a lead compound in drug discovery. Also, we highlighted therapeutic strategies that have expedited improvements in curcumin oral bioavailability and delivery to target sites over the years. Recent implementations of these strategies were also covered. More research efforts should be directed towards investigating the pharmacokinetic impacts of these novel curcumin formulations in human clinical studies since inter-species disparities could limit the accuracies of animal studies. We envisaged that integrative-clinical research would help determine 'actual' improvements in curcumin pharmacokinetics coupled with suitable administrative routes, optimal dosing, and drug-enzyme or drug-drug interactions. In addition, this could help determine formulations for achieving higher systemic exposure of parent curcumin thereby providing a strong impetus towards the development of curcumin as a drug candidate in disease treatment.
姜黄素的药理学特性在大量的临床前和临床研究中都有报道。然而，由于其内在属性导致口服生物利用度极低，这阻碍了它作为治疗剂的发展。尽管如此，这些缺点并没有阻止研究人员优化其潜力。本文讨论了姜黄素的药代动力学特性及其作为药物发现的先导化合物的前景。此外，我们还强调了多年来加速提高姜黄素口服生物利用度和递送至靶部位的治疗策略。最近还介绍了这些策略的实施情况。由于种间差异可能限制动物研究的准确性，因此应将更多的研究工作用于研究这些新型姜黄素制剂在人体临床研究中的药代动力学影响。我们设想，综合临床研究将有助于确定姜黄素药代动力学的“实际”改善，以及合适的管理途径、最佳剂量、药物-酶或药物-药物相互作用。此外，这有助于确定实现母体姜黄素更高系统暴露的配方，从而为姜黄素作为疾病治疗候选药物的开发提供强大动力。
