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.

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姜黄素药理学用途的最新进展：它是否在药物发现管道中失败了？

大量的临床前和临床研究已经报道了姜黄素的药理特性。然而，先天属性导致极低的口服生物利用度，这阻碍了其作为治疗剂的发展。无论如何，这些缺点并没有阻止研究人员优化其潜力。这篇综述讨论了姜黄素的药代动力学特性及其作为药物发现先导化合物的前景。此外，我们强调了多年来加快改善姜黄素口服生物利用度和递送至靶位点的治疗策略。这些策略最近的实施也包括在内。更多的研究工作应该针对研究这些新型姜黄素制剂在人类临床研究中的药代动力学影响，因为种间差异可能会限制动物研究的准确性。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，以及合适的给药途径、最佳剂量和药物-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全身暴露的配方，从而为姜黄素作为疾病治疗候选药物的开发提供强大的推动力。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，以及合适的给药途径、最佳剂量和药物-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全身暴露的配方，从而为姜黄素作为疾病治疗候选药物的开发提供强大的推动力。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，以及合适的给药途径、最佳剂量和药物-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全身暴露的配方，从而为姜黄素作为疾病治疗候选药物的开发提供强大的推动力。