Tethered polymer nanoassemblies for sustained carfilzomib release and prolonged suppression of proteasome activity

Derek Reichel, Min Jae Lee, Wooin Lee, Kyung Bo Kim, Younsoo Bae

Research output: Contribution to journalArticlepeer-review

10 Scopus citations

Abstract

Aim: Proteasome inhibitors, such as carfilzomib (CFZ), have shown potential to treat various types of cancers in preclinical models, but clinical applications are limited likely due to formulation and delivery issues. Results & methodology: Tethered polymer nanoassemblies (TNAs) were synthesized by tethering hydrophilic polymers and hydrophobic groups to charged polymer scaffolds, and then end-capping remaining amines on scaffold. Drug entrapment and drug release half-lives increased as charge was removed from scaffold. TNAs with sustained CFZ release maintained drug efficacy after preincubation and increased duration of proteasome inhibition in cancer cells compared with free CFZ. Conclusion: TNAs fine-tuned CFZ release as charge was removed from polymer scaffold, which allowed for sustained proteasome inhibition in cancer cells and potentially enhanced anticancer efficacy.

Original languageEnglish
Pages (from-to)665-681
Number of pages17
JournalTherapeutic Delivery
Volume7
Issue number10
DOIs
StatePublished - Oct 2016

Bibliographical note

Publisher Copyright:
© 2016 Future Science Ltd.

Keywords

  • cancer chemotherapy
  • controlled release
  • nanoparticles
  • proteasome inhibitors
  • solid cancers

ASJC Scopus subject areas

  • Pharmaceutical Science

Fingerprint

Dive into the research topics of 'Tethered polymer nanoassemblies for sustained carfilzomib release and prolonged suppression of proteasome activity'. Together they form a unique fingerprint.

Cite this