Skip to main content
padlock icon - secure page this page is secure

Chemical Derivatization of the Anticancer Agent Cabazitaxel Using a Polyunsaturated Fatty Acid for Safe Drug Delivery In Vivo

Buy Article:

$106.34 + tax (Refund Policy)

The utilization of nonionic surfactants is a practical way to formulate hydrophobic chemotherapeutics, facilitating the clinical translation of drug candidates during the development process. However, since the drug toxicity in patients is primarily determined by the cytotoxic drugs themselves, such a formulation approach is unable to improve the drug tolerability. Therefore, additional strategies for enhancing drug safety profiles are necessary when considering the use of surfactants as formulation excipients. Using cabazitaxel as a target agent, we show that the miscibility of α-linolenic acid (LNA)tethered cabazitaxel conjugate 1 with polysorbate 80 (Tween 80) was enhanced. Upon further blending with aqueous solutions, conjugate 1 formed stable colloidal nanoemulsions with Tween 80. Thus, the nanoemulsions are systemically injectable and suitable for preclinical studies. Compared with parent cabazitaxel, conjugate 1 displayed a substantial improvement in its safety profile in animals. Therapeutic studies in a mouse xenograft model of human cancer further demonstrated the effectiveness of conjugate 1 in suppressing tumor growth. These results suggest that attaching flexible lipid chains to the highly toxic cabazitaxel generates a new drug entity that is more compatible with Tween 80-based formulations than its free drug form. This new entity retains its antitumor activity while improving its tolerability in vivo.
No Reference information available - sign in for access.
No Citation information available - sign in for access.
No Supplementary Data.
No Article Media
No Metrics


Document Type: Research Article

Publication date: November 1, 2018

More about this publication?
  • Journal of Biomedical Nanotechnology (JBN) is a peer-reviewed multidisciplinary journal providing broad coverage in all research areas focused on the applications of nanotechnology in medicine, drug delivery systems, infectious disease, biomedical sciences, biotechnology, and all other related fields of life sciences.
  • Editorial Board
  • Information for Authors
  • Subscribe to this Title
  • Terms & Conditions
  • Ingenta Connect is not responsible for the content or availability of external websites
  • Access Key
  • Free content
  • Partial Free content
  • New content
  • Open access content
  • Partial Open access content
  • Subscribed content
  • Partial Subscribed content
  • Free trial content
Cookie Policy
Cookie Policy
Ingenta Connect website makes use of cookies so as to keep track of data that you have filled in. I am Happy with this Find out more