{"id":179,"date":"2025-05-27T19:09:38","date_gmt":"2025-05-27T19:09:38","guid":{"rendered":"https:\/\/wwwtest.pharmacy.wisc.edu\/faculty\/kwon-research-group\/?p=179"},"modified":"2025-05-27T19:09:38","modified_gmt":"2025-05-27T19:09:38","slug":"oligolactic-acid8-docetaxel-prodrug-loaded-peg-b-pla-micelles-for-prostate-cancer","status":"publish","type":"post","link":"https:\/\/wwwtest.pharmacy.wisc.edu\/faculty\/kwon-research-group\/2025\/05\/27\/oligolactic-acid8-docetaxel-prodrug-loaded-peg-b-pla-micelles-for-prostate-cancer\/","title":{"rendered":"Oligo(Lactic Acid)8-Docetaxel Prodrug-Loaded PEG-b-PLA Micelles for Prostate Cancer"},"content":{"rendered":"
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October 17, 2021<\/div>\r\nCite this<\/a><\/div>\r\n
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Abstract\"cover<\/h2>\r\nDocetaxel (DTX) is among the most frequently prescribed chemotherapy drugs and has recently been shown to extend survival in advanced prostate cancer patients. However, the poor water solubility of DTX prevents full exploitation of this potent anticancer drug. The current marketed formulation, Taxotere\u00ae<\/sup>, contains a toxic co-solvent that induces adverse reactions following intravenous injection. Nano-sized polymeric micelles have been proposed to create safer, water-soluble carriers for DTX, but many have failed to reach the clinic due to poor carrier stability in vivo. In this study, we aimed to improve micelle stability by synthesizing an ester prodrug of DTX, oligo(lactic acid)8<\/sub>-docetaxel (o(LA)8<\/sub>-DTX), for augmented compatibility with the core of poly(ethylene glycol)-b<\/span>-poly(lactic acid) (PEG-b<\/span>-PLA) micelles. Due to the enhancement of drug-carrier compatibility, we were able to load 50% (w<\/span>\/w<\/span>) prodrug within the micelle, solubilize 20 mg\/mL o(LA)8<\/sub>-DTX (~12 mg\/mL DTX-equivalent) in aqueous media, and delay payload release. While the micelle core prohibited premature degradation, o(LA)8<\/sub>-DTX was rapidly converted to parent drug DTX through intramolecular backbiting (t1\/2<\/sub>\u00a0= 6.3 h) or esterase-mediated degradation (t1\/2<\/sub>\u00a0= 2.5 h) following release. Most importantly, o(LA)8<\/sub>-DTX micelles proved to be as efficacious but less toxic than Taxotere\u00ae<\/sup>\u00a0in a preclinical mouse model of prostate cancer.\r\n\r\n<\/div>\r\n<\/div>\r\n<\/section><\/section><\/div>\r\n
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Cited by<\/h2>\r\n<\/div>\r\n<\/div>\r\n
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\r\n\r\nThis article is cited by 4 publications\r\n
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  1. \r\n
    Repp, L., Skoczen, S. L., Rasoulianboroujeni, M., Stern, S. T., & Kwon, G. S. (2023). Plasma Stability and Plasma Metabolite Concentration-Time Profiles of Oligo(Lactic Acid)8-Paclitaxel Prodrug Loaded Polymeric Micelles.\u00a0The AAPS journal<\/i>,\u00a025<\/i>(3), 39.\u00a0https:\/\/doi.org\/10.1208\/s12248-023-00807-4<\/a><\/div><\/li>\r\n \t
  2. \r\n
    Wu, Y., Wang, M., Li, Y., Xia, H., Cheng, Y., Liu, C., Xia, Y., Wang, Y., Yue, Y., Cheng, X., & Xie, Z. (2022). The Fabrication of Docetaxel-Containing Emulsion for Drug Release Kinetics and Lipid Peroxidation.\u00a0Pharmaceutics<\/i>,\u00a014<\/i>(10), 1993.\u00a0https:\/\/doi.org\/10.3390\/pharmaceutics14101993<\/a><\/div><\/li>\r\n \t
  3. \r\n
    Fatfat, Z., Fatfat, M., & Gali-Muhtasib, H. (2022). Micelles as potential drug delivery systems for colorectal cancer treatment.\u00a0World journal of gastroenterology<\/i>,\u00a028<\/i>(25), 2867\u20132880.\u00a0https:\/\/doi.org\/10.3748\/wjg.v28.i25.2867<\/a><\/div><\/li>\r\n \t
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    Cammas-Marion S. (2022). Development of Multifunctional Nanoparticles for Therapy and\/or Diagnosis.\u00a0Nanomaterials (Basel, Switzerland)<\/i>,\u00a012<\/i>(14), 2321.\u00a0https:\/\/doi.org\/10.3390\/nano12142321<\/a><\/div><\/li>\r\n<\/ol>\r\n<\/div>\r\n<\/div>","protected":false},"excerpt":{"rendered":"October 17, 2021 Cite this Abstract Docetaxel (DTX) is among the most frequently prescribed chemotherapy drugs and has recently been shown to extend survival in advanced prostate cancer patients. However, the poor water solubility of …","protected":false},"author":7,"featured_media":0,"comment_status":"closed","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":{"_acf_changed":false,"footnotes":""},"categories":[1],"tags":[],"class_list":["post-179","post","type-post","status-publish","format-standard","hentry","category-uncategorized"],"acf":[],"_links":{"self":[{"href":"https:\/\/wwwtest.pharmacy.wisc.edu\/faculty\/kwon-research-group\/wp-json\/wp\/v2\/posts\/179","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/wwwtest.pharmacy.wisc.edu\/faculty\/kwon-research-group\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/wwwtest.pharmacy.wisc.edu\/faculty\/kwon-research-group\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/wwwtest.pharmacy.wisc.edu\/faculty\/kwon-research-group\/wp-json\/wp\/v2\/users\/7"}],"replies":[{"embeddable":true,"href":"https:\/\/wwwtest.pharmacy.wisc.edu\/faculty\/kwon-research-group\/wp-json\/wp\/v2\/comments?post=179"}],"version-history":[{"count":1,"href":"https:\/\/wwwtest.pharmacy.wisc.edu\/faculty\/kwon-research-group\/wp-json\/wp\/v2\/posts\/179\/revisions"}],"predecessor-version":[{"id":182,"href":"https:\/\/wwwtest.pharmacy.wisc.edu\/faculty\/kwon-research-group\/wp-json\/wp\/v2\/posts\/179\/revisions\/182"}],"wp:attachment":[{"href":"https:\/\/wwwtest.pharmacy.wisc.edu\/faculty\/kwon-research-group\/wp-json\/wp\/v2\/media?parent=179"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/wwwtest.pharmacy.wisc.edu\/faculty\/kwon-research-group\/wp-json\/wp\/v2\/categories?post=179"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/wwwtest.pharmacy.wisc.edu\/faculty\/kwon-research-group\/wp-json\/wp\/v2\/tags?post=179"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}