Complexation behavior of antiestrogen drug tamoxifen citrate with natural and modified β-cyclodextrins |
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| Authors: | Erem Bilensoy Lale Doğan Murat Şen Atilla Hıncal |
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| Affiliation: | (1) Faculty of Pharmacy, Department of Pharmaceutical Technology, Hacettepe University, 06100 Ankara, Turkey;(2) Faculty of Medicine Oncology Institute, Department of Basic Oncology, Hacettepe University, 06100 Ankara, Turkey;(3) Department of Chemistry, Polymer Chemistry Division, Hacettepe University, Beytepe, 06532 Ankara, Turkey |
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| Abstract: | Inclusion complexes of the poorly-soluble antiestrogen drug tamoxifen citrate (TMX) were prepared with β-cyclodextrin (β-CD) and 2,3-di-O-hexanoyl-β-cyclodextrin (β-CDC6) being natural and amphiphilic cyclodextrins, respectively using the co-lyophilization technique. Complexation occurred in aqueous medium for natural cyclodextrin β-CD and a medium of water:ethanol mixture for the amphiphilic cyclodextrin β-CDC6. The complexes were characterized using analytical techniques including Differential Scanning Calorimetry (DSC), Fourier Transform Infrared spectroscopy (FTIR) and proton Nuclear Magnetic Resonance Spectrometry (1H NMR). Anticancer efficacies of the complexes were determined against MCF-7 human breast carcinoma cell line with MTT assay. It was found that tamoxifen citrate can be incorporated in the cavity for β-CD and both in the cavity and the aliphatic chains for β-CDC6. The latter having two hydrophobic sites for inclusion of water-insoluble drug exhibited significantly higher anticancer efficacy accordingly. |
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| Keywords: | Amphiphilic cyclodextrin β -CDC6 β -Cyclodextrin Tamoxifen citrate Inclusion complex Characterization DSC FTIR NMR Anticancer efficacy MTT assay |
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