Estrogen Anchored Micelles For Co-Delivery of Paclitaxel and BH3- Mimetic Enhance Therapeutic Efficacy in Breast Cancer: A Proteomics-Guided Nano-therapeutics Discovery
Improve Targeting EfficacyBH3 mimic has anti-neoplastic activitiesInduces Cell DeathEffectively deliver PaclitaxelCounters Paclitaxel drug resistance
Breast cancer, drugs
The invention entails construction of a novel targeting moiety ╬▓-cyclodextrin conjugated estrone (CDE1) that has been synthesized and integrated in a polymeric nanoparticle. The integration of CDE1 increases uptake by the tumor and decreases the side effects of the encapsulated cytotoxic drugs. The enhanced anti-tumor activities with improved targeting efficacy have been achieved in vitro and in vivo. The systemic toxicity associated with the solvent of the cytotoxic drugs isminimal due to the hydrophilic nano-formulation. Moreover, the molecular mechanism for the cell death induced by the nanoparticle has been explored thoroughly by a systematic proteomics study. The results suggest thatenhanced G2/M cell cycle arrest and PI3K/Akt/mTOR mediated autophagy, account for the exceedingly potent anti-tumor activity of this convergent nanoparticle.
美国
