title: The Effectiveness of Raloxifene-Loaded Liposomes and Cochleates in Breast Cancer Therapy.
abstract: Liposome (spherical vesicles) and cochleate (multilayer crystalline, spiral structure) formulations containing raloxifene have been developed having dimethyl-β-cyclodextrin (DM-β-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-β-CD. These developed formulations can be helpful for further treatment alternatives and new strategies for cancer therapy.
authors.affiliation: Department of Pharmaceutical Technology, Gazi University Faculty of Pharmacy, 06330, Ankara, Turkey.
authors.forename: N Başaran Mutlu
authors.initials: NB
authors.lastname: Ağardan
authors.affiliation: Department of Pharmaceutical Technology, Gazi University Faculty of Pharmacy, 06330, Ankara, Turkey. zdegim@gazi.edu.tr.
authors.forename: Zelihagül
authors.initials: Z
authors.lastname: Değim
authors.affiliation: Food and Mouth Diseases Institute, 06520, Ankara, Turkey.
authors.forename: Şükran
authors.initials: Ş
authors.lastname: Yılmaz
authors.affiliation: Department of Pharmacology and Toxicology, Ankara University Faculty of Veterinary Medicine, 06110, Ankara, Turkey.
authors.forename: Levent
authors.initials: L
authors.lastname: Altıntaş
authors.affiliation: Department of Physiology, Gülhane Military Medical Academy, 06010, Ankara, Turkey.
authors.forename: Turgut
authors.initials: T
authors.lastname: Topal
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D018938:Caco-2 Cells; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical / Q000379:methods; D005260:Female; D006801:Humans; D008081:Liposomes / Q000494:pharmacology*; D061986:MCF-7 Cells; D020778:Matrix Metalloproteinase 2 / Q000378:metabolism; D020849:Raloxifene Hydrochloride / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013656:Taurocholic Acid / Q000494:pharmacology*; D047392:beta-Cyclodextrins / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D008081:Liposomes; D047392:beta-Cyclodextrins; D020849:Raloxifene Hydrochloride; C038119:heptakis(2,6-O-dimethyl)beta-cyclodextrin; D013656:Taurocholic Acid; D020778:Matrix Metalloproteinase 2
keywords: MCF-7; MMP-2; cochleates; dimethyl-β-cyclodextrin; liposomes; raloxifene; sodium taurocholate