Antitumoral and MMP-2 inhibition activity of raloxifene or tamoxifen loaded nanoparticles containing dimethyl-beta-cyclodextrin

A new nanoparticle formulation has been developed by using dimethyl-beta-cyclodextrin (DM-beta-CD) with raloxifene HCl or tamoxifene citrate. Both drugs are insoluble in water and represent as low bioavailibilities when given orally. Tamoxifen has an FDA approval for breast cancer prevention and the treatment. Raloxifene is approved for osteoprosis treatment. Both drugs were selected as a model drug antitumoural activity and MMP-2 inhibition studies were evaluated on breast cancer cell lines MCF-7 and MDA-MB 231. MMP-2 is known to be responsible for tumour invasion and initation the of angiogenesis. DM-beta-CD and sodium taurocholate (NaTC) have been used as absorption enhancers to increase penetration effect of raloxifene/tamoxifen on the tumour cells and aimed to provide high antitumoral activity and MMP-2 inhibition results by developed nanoparticle formulations. The effects of two absorption enhancers were compared. The highest antitumoral activity was observed for DM-beta-CD-raloxifene HCl nanoparticle formulation and also MMP-2 enzyme inhibit effectively.