Preparation of Anthracyclines Liposomes for Tumor-Targeting Drug Delivery

Living reference work entry
Part of the Biomaterial Engineering book series (BIOENG)


Anthracyclines are the most effective anticancer drugs with broad cancer spectrum. They demonstrate strong anticancer efficacy in vitro but are less effective in vivo during treatment of brain cancer due to the hindrance of the blood-brain barrier (BBB). In this regard, this protocol focuses on the fabrication of dual-ligand modified anthracycline liposomes for treatment of brain cancer through transferring drug across the BBB and then for targeting brain cancer. Here, the preparation and characterization techniques of dual-targeting daunorubicin liposomes are described. In this construct, daunorubicin is used as a model drug, while all anthracyclines could be loaded into the liposomes with the same procedures. The present results demonstrate that the dual-targeting daunorubicin liposomes exhibit a high drug encapsulation efficiency (>90%), an increased transport of the drug liposomes across the BBB, and then a targeted effect in killing brain glioma cells, thereby improving the therapeutic efficacy of brain glioma in vitro and in animals.


Anthracyclines Dual -targeting Liposomes Blood-brain barrier Brain glioma-bearing rats Survival 


  1. Bouma J, Beijnen JH, Bult A, Underberg WJ (1986) Anthracycline antitumour agents. A review of physicochemical, analytical and stability properties. Pharm Weekbl Sci 8(2):109–133CrossRefGoogle Scholar
  2. Cortés-Funes H, Coronado C (2007) Role of anthracyclines in the era of targeted therapy. Cardiovasc Toxicol 7(2):56–60CrossRefGoogle Scholar
  3. Coune A (1988) Liposomes as drug delivery system in treatment of infectious diseases. Potential applications and clinical experience. Infection 16(3):141–147CrossRefGoogle Scholar
  4. Du J, Lu WL, Ying X, Liu Y, Du P, Tian W et al (2009) Dual-targeting topotecan liposomes modified with tamoxifen and wheat germ agglutinin significantly improve drug transport across the blood-brain barrier and survival of brain tumor-bearing animals. Mol Pharm 6(3):905–917CrossRefGoogle Scholar
  5. Forssen EA, Tökes ZA (1979) In vitro and in vivo studies with adriamycin liposomes. Biochem Biophys Res Commun 91(4):1295–1301CrossRefGoogle Scholar
  6. Huwyler J, Drewe J, Krähenbuhl S (2008) Tumor targeting using liposomal antineoplastic drugs. Int J Nanomedicine 3(1):21–29CrossRefGoogle Scholar
  7. Lotfi K, Zackrisson AL, Peterson C (2002) Comparison of idarubicin and daunorubicin regarding intracellular uptake, induction of apoptosis, and resistance. Cancer Lett 178(2):141–149CrossRefGoogle Scholar
  8. Lyman GH, Kuderer NM, Crawford J, Wolff DA, Culakova E, Poniewierski MS, Dale DC (2011) Predicting individual risk of neutropenic complications in patients receiving cancer chemotherapy. Cancer 117(9):1917–1927CrossRefGoogle Scholar
  9. McGowan JV, Chung R, Maulik A, Piotrowska I, Walker JM, Yellon DM (2017) Anthracycline chemotherapy and cardiotoxicity. Cardiovasc Drugs Ther 31(1):63–75CrossRefGoogle Scholar
  10. Minotti G, Menna P, Salvatorelli E, Cairo G, Gianni L (2004) Anthracyclines: molecular advances and pharmacologic developments in antitumor activity and cardiotoxicity. Pharmacol Rev 56(2):185–229CrossRefGoogle Scholar
  11. Moghimi SM, Patel HM (1992) Opsonophagocytosis of liposomes by peritoneal macrophages and bone marrow reticuloendothelial cells. Biochim Biophys Acta 1135(3):269–274CrossRefGoogle Scholar
  12. Peng X, Chen B, Lim CC, Sawyer DB (2005) The cardiotoxicology of anthracycline chemotherapeutics: translating molecular mechanism into preventative medicine. Mol Interv 5(3):163–171CrossRefGoogle Scholar
  13. Simeonova M, Ivanova G, Enchev V, Markova N, Kamburov M, Petkov C, Devery A, O'Connor R, Brougham D (2009) Physicochemical characterization and in vitro behavior of daunorubicin-loaded poly(butylcyanoacrylate) nanoparticles. Acta Biomater 5(6):2109–2121CrossRefGoogle Scholar
  14. Simone EA, Dziubla TD, Muzykantov VR (2008) Polymeric carriers: role of geometry in drug delivery. Expert Opin Drug Deliv 5(12):1283–1300CrossRefGoogle Scholar
  15. Tila D, Ghasemi S, Yazdani-Arazi SN, Ghanbarzadeh S (2015) Functional liposomes in the cancer-targeted drug delivery. J Biomater Appl 30(1):3–16CrossRefGoogle Scholar
  16. Weiss RB (1992) The anthracyclines: will we ever find a better doxorubicin? Semin Oncol 19(6):670–686Google Scholar
  17. Ying X, Wen H, Lu WL, Du J, Guo J, Tian W, Men Y, Zhang Y, Li RJ, Yang TY, Shang DW, Lou JN, Zhang LR, Zhang Q (2010) Dual-targeting daunorubicin liposomes improve the therapeutic efficacy of brain glioma in animals. J Control Release 141(2):183–192CrossRefGoogle Scholar
  18. Ying X, Wen H, Yao HJ, Zhang Y, Tian W, Zhang L, Ju RJ, Wang XX, Yu Y, Lu WL (2011) Pharmacokinetics and tissue distribution of dual-targeting daunorubicin liposomes in mice. Pharmacology 87(1–2):105–114CrossRefGoogle Scholar

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© Springer-Verlag GmbH Germany 2018

Authors and Affiliations

  1. 1.School of Pharmaceutical Sciences/Key Laboratory of Xinjiang Phytomedicine Resources UtilizationShihezi UniversityXinjiangRepublic of China

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