Nanomedicine from amphiphilizedprodrugs: Concept and clinical translation

Adv Drug Deliv Rev. 2021 Dec:179:114027. doi: 10.1016/j.addr.2021.114027. Epub 2021 Oct 31.

Abstract

Nanomedicines generally consisting of carrier materials with small fractions of active pharmaceutical ingredients (API) have long been used to improve the pharmacokinetics and biodistributions, augment the therapeutic efficacies and mitigate the side effects. Amphiphilizing hydrophobic/hydrophilic drugs to prodrugs capable of self-assembly into well-defined nanostructures has emerged as a facile approach to fabricating nanomedicines because this amphiphilized prodrug (APD) strategy presents many advantages, including minimized use of inert carrier materials, well-characterized prodrug structures, fixed and high drug loading contents, 100% loading efficiency, and burst-free but controlled drug release. This review comprehensively summarizes recent advances in APDs and their nanomedicines, from the rationale and the stimuli-responsive linker chemistry for on-demand drug release to their progress to the clinics, clinical performance of APDs, as well as the challenges and perspective on future development.

Keywords: Amphiphilized prodrug; Clinical translation; Drug delivery; Nanomedicine; Stimuli-responsive.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Delayed-Action Preparations
  • Drug Development
  • Drug Evaluation, Preclinical
  • Drug Liberation
  • Enzymes / metabolism
  • Humans
  • Hydrogen-Ion Concentration
  • Hydrophobic and Hydrophilic Interactions*
  • Nanoparticle Drug Delivery System / chemistry*
  • Nanoparticle Drug Delivery System / pharmacokinetics*
  • Oxidation-Reduction
  • Peptides / chemistry
  • Polymers / chemistry
  • Surface-Active Agents / chemistry
  • Ultraviolet Rays

Substances

  • Delayed-Action Preparations
  • Enzymes
  • Nanoparticle Drug Delivery System
  • Peptides
  • Polymers
  • Surface-Active Agents