10.6084/m9.figshare.7624637.v1
Khaled Greish
Khaled
Greish
Hayley Nehoff
Hayley
Nehoff
Fatemah Bahman
Fatemah
Bahman
Tara Pritchard
Tara
Pritchard
Sebastien Taurin
Sebastien
Taurin
Raloxifene nano-micelles effect on triple-negative breast cancer is mediated through estrogen receptor-β and epidermal growth factor receptor
Taylor & Francis Group
2019
Triple-negative breast cancer
raloxifene
nanomedicine
micelle
oestrogen receptor-β
SERM
EGFR
2019-01-24 16:36:13
Journal contribution
https://tandf.figshare.com/articles/journal_contribution/Raloxifene_nano-micelles_effect_on_triple-negative_breast_cancer_is_mediated_through_estrogen_receptor-_and_epidermal_growth_factor_receptor/7624637
<p>Triple-negative breast cancer (TNBC) is an aggressive subtype of breast cancer that differs in progression, recurrence, and prognosis from other forms of breast cancer. The heterogeneity of TNBC has remained a challenge as no targeted therapy is currently available. Previously, we and others have demonstrated that raloxifene, a selective oestrogen receptor modulator, was also acting independently of the oestrogen receptor-α. However, raloxifene is characterised by a low bioavailability <i>in vivo</i>. Thus, we encapsulated raloxifene into a styrene-maleic acid (SMA) micelle to improve its pharmacokinetics. The micellar raloxifene had higher cytotoxicity when compared to the free formulation, promoted a higher cellular uptake and affected critical signalling pathways. Furthermore, SMA-raloxifene reduced TNBC tumour growth more efficiently than free raloxifene. Finally, we showed that this effect was partially mediated through oestrogen receptor-β. In conclusion, we have provided new insight into the role of raloxifene nanoformulation in improving the management of TNBC.</p>