恶性肿瘤是全球主要死因，对人类健康构成严重威胁。数十年来，天然产物一直被证明是新型抗癌药物研发的重要来源。紫草素 (SHK) 是从紫草根中分离的自然分子，显示出在抗癌治疗中的巨大潜力。然而，由于生物利用度低、不良反应和非选择性毒性，它的进一步临床应用显著受限。随着纳米技术的发展，纳米药物输送系统已成为提高药物生物利用度并增强治疗效果的有希望的策略。为克服SHK的缺点，开发了各种纳米药物输送系统，如脂质体、聚合物胶束、纳米粒子、纳米凝胶和纳米乳液，以实现高效的输送，以提高抗肿瘤效果。本文总结了SHK的抗癌药理学活性和药代动力学。此外，还概述了SHK纳米药物在癌症治疗中的最新进展，重点关注长循环、肿瘤靶向能力、肿瘤微环境响应性药物释放和纳米系统介导的联合治疗。最后，重点介绍了SHK纳米药物未来临床应用的挑战和前景。© 2023 Yan et al.

Malignant tumor, the leading cause of death worldwide, poses a serious threat to human health. For decades, natural product has been proven to be an essential source for novel anticancer drug discovery. Shikonin (SHK), a natural molecule separated from the root of Lithospermum erythrorhizon, shows great potential in anticancer therapy. However, its further clinical application is significantly restricted by poor bioavailability, adverse effects, and non-selective toxicity. With the development of nanotechnology, nano drug delivery systems have emerged as promising strategies to improve bioavailability and enhance the therapeutic efficacy of drugs. To overcome the shortcoming of SHK, various nano drug delivery systems such as liposomes, polymeric micelles, nanoparticles, nanogels, and nanoemulsions, were developed to achieve efficient delivery for enhanced antitumor effects. Herein, this review summarizes the anticancer pharmacological activities and pharmacokinetics of SHK. Additionally, the latest progress of SHK nanomedicines in cancer therapy is outlined, focusing on long circulation, tumor targeting ability, tumor microenvironment responsive drug release, and nanosystem-mediated combination therapy. Finally, the challenges and prospects of SHK nanomedicines in the future clinical application are spotlighted.© 2023 Yan et al.