Cancer is the second highest cause of death globally, with about 70% of deaths occurring in low- or middle-income countries, thus calling for efficient cures. Nanotechnology research has evidenced numerous therapeutic innovations that target the tumor tissues either passively or actively. Camptothecin is a potent anticancer drug which has shown appreciable antitumor activity against a broad spectrum of cancers such as breast, ovarian, colon, lung and stomach. Nonetheless, applications of camptothecin are limited by water insolubility, rapid conversion of its bioactive lactone form to inactive carboxylate under physiological conditions, drug resistance and off-target side effects. Here, we review the delivery of camptothecin by active and passive targeting for anticancer activity. We discuss the mechanism of action and the novel targeted drug delivery platforms that have been explored for the delivery of camptothecin for the treatment of solid tumors.

癌症是全球第二大死亡原因，大约70％的死亡发生在低收入或中等收入国家，因此需要有效的治疗方法。纳米技术研究已经证明了无数或被动地靶向肿瘤组织的治疗创新。喜树碱是一种有效的抗癌药物，对多种癌症（例如乳腺癌，卵巢癌，结肠癌，肺癌和胃癌）显示出明显的抗肿瘤活性。然而，喜树碱的应用受到水不溶性，其生物活性内酯形式在生理条件下快速转化为非活性羧酸盐，耐药性和脱靶副作用的限制。在这里，我们回顾了喜树碱通过主动和被动靶向抗癌活性的传递。