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


Ben Taleb A., KARAKUŞ S., TAN E., İLGAR M., KUTLU Ö., Gozuacik D., ...More

SUPRAMOLECULES IN DRUG DISCOVERY AND DRUG DELIVERY, vol.2207, pp.199-220, 2021 (Journal Indexed in SCI) identifier identifier

  • Publication Type: Article / Article
  • Volume: 2207
  • Publication Date: 2021
  • Doi Number: 10.1007/978-1-0716-0920-0_16
  • Title of Journal : SUPRAMOLECULES IN DRUG DISCOVERY AND DRUG DELIVERY
  • Page Numbers: pp.199-220
  • Keywords: Ceranib-2, Rosin ester, PEGylation, Nanoencapsulation, Anticancer, SMART DRUG-DELIVERY, SPHINGOLIPID METABOLISM, BIODEGRADABLE POLYMERS, CELL-SURVIVAL, GLOBAL BURDEN, CANCER, CERAMIDE, PEGYLATION, STRESS, SPHINGOSINE-1-PHOSPHATE

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.