Functional ligands for improving anticancer drug therapy: current status and applications to drug delivery systems

• Published in: Drug delivery Vol. 29; no. 1; pp. 1959 - 1970
• Main Authors: Bajracharya, Rajiv, Song, Jae Geun, Patil, Basavaraj Rudragouda, Lee, Sang Hoon, Noh, Hye-Mi, Kim, Da-Hyun, Kim, Gyu-Lin, Seo, Soo-Hwa, Park, Ji-Won, Jeong, Seong Hoon, Lee, Chang Hoon, Han, Hyo-Kyung
• Format: Journal Article
• Language: English
• Published: Philadelphia Taylor & Francis 31.12.2022; Taylor & Francis Ltd; Taylor & Francis Group
• Subjects: anticancer; Cancer; cell penetrating peptides; cell surface receptors; Chemotherapy; Drug delivery; Drug delivery systems; Ligands; Peptides; target selectivity; tight junction opening
• ISSN: 1071-7544; 1521-0464; 1521-0464
• DOI: 10.1080/10717544.2022.2089296

Conventional chemotherapy lacking target selectivity often leads to severe side effects, limiting the effectiveness of chemotherapy. Therefore, drug delivery systems ensuring both selective drug release and efficient intracellular uptake at the target sites are highly demanded in chemotherapy to improve the quality of life of patients with low toxicity. One of the effective approaches for tumor-selective drug delivery is the adoption of functional ligands that can interact with specific receptors overexpressed in malignant cancer cells. Various functional ligands including folic acid, hyaluronic acid, transferrin, peptides, and antibodies, have been extensively explored to develop tumor-selective drug delivery systems. Furthermore, cell-penetrating peptides or ligands for tight junction opening are also actively pursued to improve the intracellular trafficking of anticancer drugs. Sometimes, multiple ligands with different roles are used in combination to enhance the cellular uptake as well as target selectivity of anticancer drugs. In this review, the current status of various functional ligands applicable to improve the effectiveness of cancer chemotherapy is overviewed with a focus on their roles, characteristics, and preclinical/clinical applications.