Levodopa is the most effective drug for the treatment of Parkinson’s disease, but its use as an oral medication is complicated by its erratic absorption, extensive metabolism and short plasma half-life. On long-term use and with disease progression, there is a high incidence of motor and non-motor complications, which remain a major clinical and research challenge. It is widely accepted that levodopa needs to be administered using formulations that result in good and consistent bioavailability and the physiologically relevant and continuous formation of dopamine in the brain to maximise its efficacy while avoiding and reversing ‘wearing off’ and dyskinesia. However, the physicochemical properties of levodopa along with its pharmacokinetic and pharmacodynamic profile make it difficult to deliver the drug in a manner that fulfils these criteria. In this review, we examine the problems associated with the administration of levodopa in Parkinson’s disease and how the use of novel technologies and delivery devices is leading to a more consistent and sustained levodopa delivery with the aim of controlling motor function as well as non-motor symptoms.

左旋多巴是治疗帕金森病最有效的药物，但由于其吸收不稳定、代谢广泛和血浆半衰期短，其作为口服药物的使用变得复杂。长期使用并随着疾病进展，运动和非运动并发症的发生率很高，这仍然是临床和研究的主要挑战。人们普遍认为，左旋多巴需要使用具有良好和一致的生物利用度以及生理相关和持续形成的多巴胺在大脑中的制剂给药，以最大限度地提高其功效，同时避免和逆转“磨损”和运动障碍。然而，左旋多巴的理化特性及其药代动力学和药效学特性使得难以以符合这些标准的方式输送药物。