Antitumor efficacy of ceranib-2 with nano-formulation of PEG and rosin esters

Ben Taleb, Ali and Karakuş, Selcan and Tan, Ezgi and Ilgar, Merve and Kutlu, Özlem and Gözüaçık, Devrim and Kutlu, Hatice Mehtap and Kilislioğlu, Ayben (2021) Antitumor efficacy of ceranib-2 with nano-formulation of PEG and rosin esters. In: Mavromoustakos, Thomas and Tzakos, Andreas G. and Durdagi, Serdar, (eds.) Supramolecules in Drug Discovery and Drug Delivery: Methods and Protocols. Methods in Molecular Biology; 2207. Humana Press, New York, NY, pp. 199-220. ISBN 978-1-0716-0919-4 (Print) 978-1-0716-0920-0 (Online)

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Ceranib-2 is a recently discovered, poorly water-soluble potent ceramidase inhibitor, with the ability to suppress cancer cell proliferation and delay tumor growth. However, its poor water solubility and weak cellular bioavailability hinder its use as a therapeutic agent for cancer. PEGylated rosin esters are an excellent platform as a natural polymer for drug delivery applications, especially for controlling drug release due to their degradability, biocompatibility, capability to improve solubility, and pharmacokinetics of potent drugs. In this study, stable aqueous amphiphilic submicron-sized PEG400-rosin ester-ceranib-2 (PREC-2) particles, ranging between 100 and 350 nm in a 1:1 mixture, were successfully synthesized by solvent evaporation mediated by sonication. Conclusion: Stable aqueous PEGylated rosin ester nanocarriers might present a significant solution to improve solubility, pharmacokinetic, and bioavailability of ceranib-2, and hold promises for use as an anticancer adjacent drug after further investigations.
Item Type: Book Section / Chapter
Uncontrolled Keywords: Anticancer; Ceranib-2; Nanoencapsulation; PEGylation; Rosin ester
Divisions: Sabancı University Nanotechnology Research and Application Center
Depositing User: Özlem Kutlu
Date Deposited: 02 Sep 2022 12:39
Last Modified: 02 Sep 2022 12:39

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