Sreekanth, Vedagopuram and Kar, Animesh and Kumar, Sandeep and Pal, Sanjay and Yadav, Poonam and Sharma, Yamini and Komalla, Varsha and Sharma, Harsh and Shyam, Radhey and Sharma, Ravi D and Mukhopadhyay, Arnab and Sengupta, Sagar and Dasgupta, Ujjaini and Bajaj, Avinash (2020) Bile Acid Tethered Docetaxel‐based Nanomicelles Mitigate Tumor Progression through Epigenetic Changes. Angewandte Chemie International Edition. ISSN 1433-7851

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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.

Item Type:	Article
Subjects:	Biomedical Science Bioengineering & Devices
Depositing User:	RCB Library
Date Deposited:	04 Jan 2021 09:06
Last Modified:	04 Jan 2021 09:06
URI:	http://rcb.sciencecentral.in/id/eprint/552

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