The Effectiveness of Raloxifene-Loaded Liposomes and Cochleates in Breast Cancer Therapy

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MUTLU AĞARDAN N. B. , Degim Z., Yilmaz S., Altintas L., Topal T.

AAPS PHARMSCITECH, vol.17, no.4, pp.968-977, 2016 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 17 Issue: 4
  • Publication Date: 2016
  • Doi Number: 10.1208/s12249-015-0429-3
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.968-977
  • Keywords: cochleates, dimethyl-beta-cyclodextrin, liposomes, MCF-7, MMP-2, raloxifene, sodium taurocholate, DRUG-DELIVERY, CACO-2 CELLS, IN-VITRO, N-NITROSOMETHYLUREA, MAMMARY-TUMORS, AMPHOTERICIN-B, ABSORPTION, NANOPARTICLES, TRANSPORT, RAT
  • Gazi University Affiliated: Yes


Liposome (spherical vesicles) and cochleate (multilayer crystalline, spiral structure) formulations containing raloxifene have been developed having dimethyl-beta-cyclodextrin (DM-beta-CD) or sodium taurocholate (NaTC). Raloxifene was approved initially for the treatment of osteoporosis but it is also effective on breast tissue and endometrial cells. Raloxifene inhibits matrix metalloproteinase-2 (MMP-2) enzyme, which is known to be responsible for tumor invasion and the initiation of angiogenesis during the tumor growth. Therefore, raloxifene was selected as a model drug. A series of raloxifene-loaded liposome and cochleate formulations were prepared. In vitro release studies and in vivo tests were performed. Breast cancer cell lines (MCF-7) were also used to find the most effective formulation. Highest antitumor activity was observed, and MMP-2 enzyme was also found to be inhibited with raloxifene-loaded cochleates containing DM-beta-CD. These developed formulations can be helpful for further treatment alternatives and new strategies for cancer therapy.