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Concept Design,Development and Preliminary Physical and Chemical Characterization of Tamoxifen-Guided-Mesoporous Silica Nanoparticles
Authors:Candace M. Day  Martin J. Sweetman  Shane M. Hickey  Yunmei Song  Yongjun Liu  Na Zhang  Sally E. Plush  Sanjay Garg
Affiliation:1.Clinical and Health Sciences, University of South Australia, North Terrace, Adelaide, SA 5000, Australia; (C.M.D.); (M.J.S.); (S.M.H.); (Y.S.);2.Future Industry Institute, University of South Australia, Mawson Lakes, SA 5095, Australia;3.School of Pharmaceutical Science, Shandong University, Ji’nan 250012, China; (Y.L.); (N.Z.)
Abstract:Conventional chemotherapies used for breast cancer (BC) treatment are non-selective, attacking both healthy and cancerous cells. Therefore, new technologies that enhance drug efficacy and ameliorate the off-target toxic effects exhibited by currently used anticancer drugs are urgently needed. Here we report the design and synthesis of novel mesoporous silica nanoparticles (MSNs) equipped with the hormonal drug tamoxifen (TAM) to facilitate guidance towards estrogen receptors (ERs) which are upregulated in breast tumours. TAM is linked to the MSNs using a poly-ʟ-histidine (PLH) polymer as a pH-sensitive gatekeeper, to ensure efficient delivery of encapsulated materials within the pores. XRD, HR-TEM, DLS, SEM, FT-IR and BET techniques were used to confirm the successful fabrication of MSNs. The MSNs have a high surface area (>1000 m2/g); and a mean particle size of 150 nm, which is an appropriate size to allow the penetration of premature blood vessels surrounding breast tumours. Successful surface functionalization was supported by FT-IR, XPS and TGA techniques, with a grafting ratio of approximately 29%. The outcomes of this preliminary work could be used as practical building blocks towards future formulations.
Keywords:breast cancer, tamoxifen, targeting vector, poly-ʟ  -histidine, mesoporous silica nanoparticles, functionalized nanostructures, surface reactivity
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