This review aimed to determine the potential of the combination of chitosan and alginate as a targeted drug carrier in cancer therapy. This article is based on the results of previous research journals collected from Google Scholar, Scopus, PubMed and Science Direct sites using the keywords chitosan, alginate, targeted drug delivery for cancer, nanoparticle chitosan alginate. With the inclusion criteria, only English-language journals, journals published in the last 10 y, related to chitosan and alginate-based formulations. Meanwhile, the exclusion criteria were journals on pharmacological properties and bioactivity, food and cosmetics. The combination of cationic chitosan and anionic alginate forming strong cross-links showed good mucoadhesive properties, higher resistance to low pH and high-efficiency encapsulation without showing any obvious cytotoxicity. Ch/Alg can overcome the shortcomings of the active substance, such as its rapid release process and the required active ingredient is lower than that required to enter the cancer target cells so as to minimize side effects of the drug by providing drug-induced release. in response to various stimuli that are well suited to the intended purpose, such as pH stimuli, redox gradients, light, temperature, and magnetism. It is shown that the combination of chitosan and alginate base has great potential in targeting cancer therapy by increasing its therapeutic effectiveness and selectivity.