Nano-Targeted Delivery of Toremifene, an Estrogen Receptor-α Blocker in Prostate Cancer

Pharmaceutical Research
Waseem HaririShaker A Mousa

Abstract

Estrogen Receptor-α (ERα) expression is increased in prostate cancer and acts as an oncogene. We propose that blocking of estrogen hormone binding to ERα using the ERα blocker toremifene will reduce the tumorigenicity of prostate cancer, and nano-targeted delivery of toremifene will improve anticancer efficacy. We report the synthesis and use in an orthotopic mouse model of PLGA-PEG nanoparticles encapsulating toremifene and nanoparticles encapsulating toremifene that are also conjugated to anti-PSMA for targeted prostate tumor delivery. Human prostate cancer cell line PC3M and a nude mouse model were used to test efficacy of nano-targeted and nano-encapsulated toremifene versus free toremifene on the growth and differentiation of tumor cells. Treatment with free toremifene resulted in a significant reduction in growth of prostate tumor and proliferation, and its nano-targeting resulted in greater reduction of prostate tumor growth, greater toremifene tumor uptake, and enhanced tumor necrosis. Tumors from animals treated with nano-encapsulated toremifene conjugated with anti-PSMA showed about a 15-fold increase of toremifene compared to free toremifene. Our data provide evidence that blocking ERα by toremifene and targeting pro...Continue Reading

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Citations

May 20, 2016·Endocrine-related Cancer·Habibur P RahmanPaul A Foster
Aug 28, 2016·Nanomedicine : Nanotechnology, Biology, and Medicine·Dhruba J BharaliShaker A Mousa
Feb 12, 2020·International Journal of Molecular Sciences·Paola OstanoGiovanna Chiorino
Jun 7, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Kavitha GoduguShaker A Mousa
Sep 17, 2020·Biomedicines·Lavinia SalamaShaker A Mousa
Jun 6, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Noureldien H E DarwishShaker A Mousa
Jun 8, 2017·Journal of Applied Toxicology : JAT·Hong SuMin Ding
Jul 23, 2020·Current Pharmaceutical Design·Hooman YariVibhudutta Awasthi

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