Classical platinum(II) anticancer agents are widely-used chemotherapeutic drugs in the clinic against a range of cancers. However, severe systemic toxicity and drug resistance have become the main obstacles which limit their application and effectiveness. Because divalent cisplatin analogues are easily destroyed in vivo, their bioavailability is low and no selective to tumor tissues. The platinum(IV) prodrugs are attractive compounds for cancer treatment because they have great advantages, e.g., higher stability in biological media, aqueous solubility and no cross-resistance with cisplatin, which may become the next generation of platinum anticancer drugs. In addition, platinum(IV) drugs could be taken orally, which could be more acceptable to cancer patients, breaking the current situation that platinum(II) drugs can only be given by injection. The coupling of platinum(IV) complexes with tumor targeting groups avoids the disadvantages such as instability in blood, irreversible binding to plasma proteins, rapid renal clearance, and non-specific distribution in normal tissues. Because of the above advantages, the combination of platinum complexes and tumor targeting groups has become the hottest field in the research and development of new platinum drugs. These approaches can be roughly categorized into two groups: active and passive targeted strategies. This review concentrates on various targeting and delivery strategies for platinum(IV) complexes to improve the efficacy and reduce the side effects of platinum-based anticancer drugs. We have made a summary of the related articles on platinum(IV) targeted delivery in recent years. We believe the results of the studies described in this review will provide new ideas and strategies for the development of platinum drugs.

经典的铂（II）抗癌剂是临床上针对多种癌症的广泛使用的化疗药物。但是，严重的全身毒性和耐药性已成为限制其应用和有效性的主要障碍。由于二价顺铂类似物在体内容易被破坏，因此它们的生物利用度低，对肿瘤组织没有选择性。铂（IV）前药是有吸引力的癌症治疗化合物，因为它们具有很大的优势，例如在生物介质中具有更高的稳定性，水溶性以及与顺铂无交叉耐药性，这可能成为下一代铂类抗癌药。此外，可以口服铂（IV）药物，这对于癌症患者来说更容易接受，这打破了目前只能注射铂（II）药物的现状。铂（IV）配合物与肿瘤靶向基团的偶联避免了诸如血液不稳定，与血浆蛋白不可逆结合，肾脏快速清除以及正常组织中非特异性分布等缺点。由于上述优点，铂复合物和肿瘤靶向基团的组合已成为新铂药物研究和开发中的最热门领域。这些方法可以大致分为两类：主动和被动目标策略。这篇综述集中于铂（IV）配合物的各种靶向和递送策略，以提高功效并减少铂基抗癌药的副作用。我们对近年来针对铂（IV）交付的相关文章进行了总结。