This review discusses the use of folate receptor (FR)-mediated transporters in cancer therapy and diagnosis. Targeted drug delivery is a promising approach to enhance treatment efficacy while minimizing side effects. Folate receptor-mediated transporters use cell membrane receptors like the folate receptor to guide drug transporters precisely to malignant cells. These transporters have been developed with various (bio)chemistries and mechanical properties, offering advantages and challenges. Modern folic acid-conjugated stimuli-responsive drug transporters enable systemic drug delivery and controlled release, reducing dosages, circumventing drug resistance, and minimizing adverse effects. The review focuses on brain and breast cancer, highlighting recent advances from 2017 to 2023 in conjugated drug transporters. It discusses the chemical and biochemical pathways involved in targeted drug delivery, emphasizing the importance of FR-targeted strategies in precision cancer therapy and diagnosis. The review also explores the structural design, loading, and release chemistry of drug transporters, including the use of linkers, spacers, and stimuli-responsive release mechanisms. The review highlights the potential of FR-targeted strategies in overcoming the limitations of passive targeting and improving drug delivery to cancer cells. The review also discusses the role of FRs as distinct cellular markers and their potential as prognostic biomarkers for selective internalization of FA-conjugated drug transporters. The review covers various types of nanocarriers, including polymeric nanocarriers, dextran-based nanocarriers, cyclodextrins, and poloxamers, and their applications in breast cancer treatment. The review emphasizes the importance of optimizing the chemical, physical, and biological properties of nanocarriers to enhance their efficacy in targeted drug delivery. The review concludes that FR-targeted strategies offer a promising approach for improving cancer therapy and diagnosis through targeted drug delivery.This review discusses the use of folate receptor (FR)-mediated transporters in cancer therapy and diagnosis. Targeted drug delivery is a promising approach to enhance treatment efficacy while minimizing side effects. Folate receptor-mediated transporters use cell membrane receptors like the folate receptor to guide drug transporters precisely to malignant cells. These transporters have been developed with various (bio)chemistries and mechanical properties, offering advantages and challenges. Modern folic acid-conjugated stimuli-responsive drug transporters enable systemic drug delivery and controlled release, reducing dosages, circumventing drug resistance, and minimizing adverse effects. The review focuses on brain and breast cancer, highlighting recent advances from 2017 to 2023 in conjugated drug transporters. It discusses the chemical and biochemical pathways involved in targeted drug delivery, emphasizing the importance of FR-targeted strategies in precision cancer therapy and diagnosis. The review also explores the structural design, loading, and release chemistry of drug transporters, including the use of linkers, spacers, and stimuli-responsive release mechanisms. The review highlights the potential of FR-targeted strategies in overcoming the limitations of passive targeting and improving drug delivery to cancer cells. The review also discusses the role of FRs as distinct cellular markers and their potential as prognostic biomarkers for selective internalization of FA-conjugated drug transporters. The review covers various types of nanocarriers, including polymeric nanocarriers, dextran-based nanocarriers, cyclodextrins, and poloxamers, and their applications in breast cancer treatment. The review emphasizes the importance of optimizing the chemical, physical, and biological properties of nanocarriers to enhance their efficacy in targeted drug delivery. The review concludes that FR-targeted strategies offer a promising approach for improving cancer therapy and diagnosis through targeted drug delivery.