Chapter 4.3 - Pharmacologic advantages of anthracyclines encapsulated in poly-ethylene-glycol coated stealth liposomes: Potential for tumor targeting

Abstract

This chapter explores the pharmacologic advantages of anthracyclines encapsulated in poly-ethylene-glycol coated stealth liposomes. Chemotherapy is a powerful tool in cancer treatment, not only as the main treatment modality against metastatic cancer, but also as a useful adjuvant to surgery and radiotherapy in localized cancer. The design of drug delivery systems for cancer therapy is faced with serious obstacles, either in the form of occult micrometastases or clinically detectable macrometastases. One of the most encouraging areas in the liposome-anticancer drug field is the work with anthracyclines. Doxorubicin (DOX), a major anti-neoplastic anthracycline and one of the most widely used drugs in cancer chemotherapy, has a broad spectrum of anti-tumor activity against solid tumors and leukemias. The slow release effect of the liposomal delivery of anthracyclines may reduce the peak plasma concentration of free drug—a factor which is directly correlated with cardiotoxicity. Long circulating polyethylene-glycol(PEG)-coated liposomes, as carriers of anthracyclines, show superior therapeutic efficacy as compared to free DOX and conventional liposomes. The broad versatility of liposome formulations has a strong impact on the pharmacokinetics and pharmacodynamics of liposome encapsulated drugs. The delivery of anthracyclines remains a leading project in the field.