癌症一直被认为是基因突变的复杂恶性后果，控制细胞增殖、分化和稳态平衡，使肿瘤治疗极具挑战性。到目前为止，各种载体分子，包括核酸药物（pDNA、miRNA和siRNA）、治疗药物（阿霉素、紫杉醇、多柔比星和吉非替尼）和成像剂（放射性同位素、荧光染料和磁共振对比剂）被视为潜在的临床应用药物。然而，由于肿瘤异质性和多重药物耐受性，单一治疗药物可能无法产生满意的临床效果，基于纳米技术的联合治疗正成为增强抗癌效果的先进重要模式。本综述汇集了目前先进的发展方向，旨在利用基于纳米医学的联合递送小分子药物和核酸进行抗癌治疗。此外，具体介绍了其优势和克服临床挑战的障碍。最后，展示了以其合理方向的未来展望，结合药物和核酸进行综合治疗的肿瘤。 ©作者。

Cancer has been considered as complex malignant consequence of genetic mutations that control the cellular proliferation, differentiation and homeostasis, thus making tumor treatment extremely challenging. To date, a variety of cargo molecules, including nucleic acids drugs (pDNA, miRNA and siRNA), therapeutic drugs (doxorubicin, paclitaxel, daunomycin and gefitinib) and imaging agents (radioisotopes, fluorescence dyes, and MRI contrast agents) have been regarded as the potential medicines in clinical application. However, non-single therapeutic drug could induce the satisfied clinical results because of tumor heterogeneity and multiple drug resistance and the nanotechnology-based combined therapy is becoming an advanced important mode for enhanced anticancer effects. The review gathers the current advanced development to co-deliver small-molecular drugs and nucleic acids for the anticancer therapy with nanomedicine-based combination. Furthermore, the superiority is definitely presented and the barriers are detail discussed to surmount the clinical challenges. In final, future perspectives in rational direction for combined tumor therapy of drugs and nucleic acids are exhibited.© The author(s).