Please use this identifier to cite or link to this item: http://hdl.handle.net/123456789/1285
Title: Bile Acid Tethered Docetaxel-Based Nanomicelles Mitigate Tumor Progression through Epigenetic Changes
Authors: Mukhopadhyay, Arnab
Sengupta, Sagar
Dasgupta, Ujjaini
Bajaj, Avinash
Sreekanth, Vedagopuram
Kar, Animesh
Kumar, Sandeep
Pal, Sanjay
Yadav, Poonam
Sharma, Yamini
Komalla, Varsha
Sharma, Harsh
Shyam, Radhey
Sharma, Ravi Datta
Keywords: Cancer therapy; docetaxel; epigenetic changes; nanomicelles; toxicity
Issue Date: Mar-2021
Publisher: Wiley-VCH GmbH
Abstract: In this study, we describe the engineering of sub-100 nm nanomicelles (DTX-PC NMs) derived from phosphocholine derivative of docetaxel (DTX)-conjugated lithocholic acid (DTX-PC) and poly(ethylene glycol)-tethered lithocholic acid. Administration of DTX-PC NMs decelerate tumor progression and increase the mice survivability compared to Taxotere (DTX-TS), the FDA-approved formulation of DTX. Unlike DTX-TS, DTX-PC NMs do not cause any systemic toxicity and slow the decay rate of plasma DTX concentration in rodents and non-rodent species including non-human primates. We further demonstrate that DTX-PC NMs target demethylation of CpG islands of Sparcl1 (a tumor suppressor gene) by suppressing DNA methyltransferase activity and increase the expression of Sparcl1 that leads to tumor regression. Therefore, this unique system has the potential to improve the quality of life in cancer patients and can be translated as a next-generation chemotherapeutic.
URI: http://hdl.handle.net/123456789/1285
Appears in Collections:Molecular Aging, Publications

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