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

被引:44
作者
Agardan, N. Basaran Mutlu [1 ]
Degim, Zelihagul [1 ]
Yilmaz, Sukran [2 ]
Altintas, Levent [3 ]
Topal, Turgut [4 ]
机构
[1] Gazi Univ, Dept Pharmaceut Technol, Fac Pharm, TR-06330 Ankara, Turkey
[2] Food & Mouth Dis Inst, TR-06520 Ankara, Turkey
[3] Ankara Univ, Dept Pharmacol & Toxicol, Fac Vet Med, TR-06110 Ankara, Turkey
[4] Gulhane Mil Med Acad, Dept Physiol, TR-06010 Ankara, Turkey
关键词
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;
D O I
10.1208/s12249-015-0429-3
中图分类号
R9 [药学];
学科分类号
100702 [药剂学];
摘要
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.
引用
收藏
页码:968 / 977
页数:10
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