Evaluation of host-guest system to enhance the tamoxifen efficiency

Abstract

Hydrophobic drugs can absorb as guest molecules inside the cavity of cyclodextrins as host sites. So, forming the drug-cyclodextrin complex can exert a profound effect on the physicochemical and biological properties of the drugs. According to these advantages, in this study, we synthesized the tamoxifen (TMX) loaded cyclodextrin (CD)-conjugated MNPs to evaluate simultaneously the cytotoxicity and sustained release as well as hepatoprotective effect of this nanomedicine. The average size of Fe3O4-DPA-PEG-CD-TMX NPs was approximately 31 nm. By energy-dispersive X-ray spectroscopy (EDS), it was revealed that Fe3O4 constitutes 14.34% of the composition of modified MNPs. In the other words, nearly 85% of Fe3O4-DPA-PEG-CD NPs are made of dopamine (DPA), polyethylene glycol (PEG) and ?-cyclodextrin (?-CD). The TMX loaded MNPs (with entrapment efficiency of 33 mg TMX per unit CD (mg) and loading efficiency of 87.5%) showed sustained liberation of TMX molecules (with 91% release in 120 h). Cytotoxicity assay and apoptosis assay by TUNEL analysis revealed that the engineered Fe3O4-DPA-PEG-CD-TMX NPs were able to significantly inhibit the MCF-7 breast cancer cells. According to effect of CD on TMX sustained release, it was found that CD can decrease the hepatotoxicity induced by TMX nearly 30%. Based upon these findings, we suggest the Fe3O4-DPA-PEG-CD-TMX NPs as an effective multifunctional nanomedicine with simultaneous therapeutic and hepatoprotective effects. é 2016 Informa UK Limited, trading as Taylor & Francis Group.