长春碱（VCR）是一种化疗药物，来源于自然生物碱植物长春花。VCR在肺癌、淋巴细胞型白血病、胶质母细胞瘤和急性髓细胞性白血病的治疗中具有显著的作用。VCR通过与微管蛋白纤维结合，阻止丝状体聚合，从而永久抑制肿瘤细胞的有丝分裂。临床上，为了减少不良药物反应和由单药治疗导致的骨髓抑制的潜在阻塞，VCR常与多药联合使用。然而，VCR对癌细胞组织的亲和性较低，较高剂量时常导致不可逆的神经毒性。常规的VCR注射剂在临床上取得了成功应用，但缺乏控制释放、非特异性生物分布和随之而来的靶外副作用仍然是主要挑战。目前，纳米技术药物递送系统正在研究用于改善VCR的药代动力学特征和肿瘤特异性靶向。各种纳米医药制剂，如脂质体、脂质纳米颗粒和聚合物纳米载体的VCR，已在不同的体外和体内模型中进行了研究。在本综述中，我们总结了VCR的化疗作用，评估了其作用机制、药代动力学和VCR递送相关的挑战。此外，还讨论了VCR在纳米医药中的应用以及对临床前和临床环境中抗癌效果的影响。© 2023. 作者。

Vincristine (VCR) is a chemotherapeutic agent obtained from natural alkaloid plant source Catharanthus roseus. VCR has been significantly useful in treatments of lung cancer, lymphocyte-based leukaemia, glioblastomas and acute myeloid leukaemia. VCR attaches to tubulin fibrils and prevents filament polymerization that permanently led to mitosis inhibition in cancer cells. Clinically, VCR is administered to patients in multidrug combination to reduce adverse drug effects and potential blockage of bone marrow inhibition due to prescribed monotherapy. However, VCR possesses low cancer tissue affinity and at higher dose often led to irreversible neurotoxicity. Conventional VCR injectables are successfully used in clinics, but lack of controlled release, non-specific biodistribution and consequent off-target side effects are still major challenges. Currently, nanotechnological drug delivery systems are being explored for improvement of VCR pharmacokinetic profile and tumour-specific targeting. Various nanomedicine formulations such as liposomes, lipid nanoparticles, and polymeric nanocarriers of VCR have been studied under various in vitro and in vivo models. In this review, we have summarised the chemotherapeutic role of VCR, evaluated the mechanism of action, pharmacokinetics and challenges associated with VCR delivery. Moreover, application of VCR in nanomedicine and effect on anticancer efficacy in preclinical and clinical setting are also being discussed.© 2023. The Author(s).