Antitumor Efficacy of Ceranib-2 with Nano-Formulation of PEG and Rosin Esters.

Abstract

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.

• Authors: Ali Ben Taleb, Selcan Karakuş, Ezgi Tan, Merve Ilgar, Özlem Kutlu, Devrim Gözüaçık, Hatice Mehtap Kutlu, Ayben Kilislioğlu
• Journal: Methods in molecular biology (Clifton, N.J.) (Methods Mol Biol) Vol. 2207 Pg. 199-220 ( 2021) ISSN: 1940-6029 [Electronic] United States
• PMID: 33113138 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• 3-(3-(4-methoxyphenyl)acryloyl)-4-phenyl-1H-quinolin-2-one
• Antineoplastic Agents
• Drug Carriers
• Quinolones
• Resins, Plant
• Polyethylene Glycols
• rosin
• polyethylene glycol 400

Topics

• Antineoplastic Agents (chemistry, pharmacokinetics, pharmacology)
• Drug Carriers (chemistry, pharmacokinetics, pharmacology)
• HeLa Cells
• Humans
• Neoplasms (drug therapy, metabolism, pathology)
• Polyethylene Glycols (chemistry)
• Quinolones (chemistry, pharmacokinetics, pharmacology)
• Resins, Plant (chemistry)