Gemcitabine-loaded innovative nanocarriers vs GEMZAR: biodistribution, pharmacokinetic features and in vivo antitumor activity

Expert Opin Drug Deliv. 2011 Dec;8(12):1609-29. doi: 10.1517/17425247.2011.632630. Epub 2011 Nov 5.

Abstract

Introduction: Gemcitabine, an anticancer drug, is a nucleoside analog deoxycytidine antimetabolite, which acts against a wide range of solid tumors. The limitation of gemcitabine is its rapid inactivation by the deoxycytidine deaminase enzyme following its in vivo administration.

Areas covered: One of the most promising new approaches for improving the biopharmaceutical properties of gemcitabine is the use of innovative drug delivery devices. This review explains the current status of gemcitabine drug delivery, which has been under development over the past 5 years, with particular emphasis on liposomal delivery. In addition, the use of novel supramolecular vesicular aggregates (SVAs), polymeric nanoparticles and squalenoylation were treated as interesting innovative approaches for the administration of the nucleoside analog.

Expert opinion: Different colloidal systems containing gemcitabine have been realized, with the aim of providing important potential advancements through traditional ways of therapy. A possible future commercialization of modified gemcitabine is desirable, as was true in the case of liposomal doxorubicin (Doxil(®), Caely(®)).

Publication types

  • Review

MeSH terms

  • Animals
  • Antimetabolites, Antineoplastic / administration & dosage*
  • Antimetabolites, Antineoplastic / pharmacokinetics
  • Deoxycytidine / administration & dosage
  • Deoxycytidine / analogs & derivatives*
  • Deoxycytidine / pharmacokinetics
  • Drug Carriers / administration & dosage*
  • Drug Carriers / pharmacokinetics
  • Gemcitabine
  • Humans
  • Liposomes / administration & dosage
  • Liposomes / pharmacokinetics
  • Nanoparticles / administration & dosage
  • Neoplasms / drug therapy
  • Neoplasms / metabolism
  • Polymers / administration & dosage
  • Squalene / chemistry
  • Tissue Distribution

Substances

  • Antimetabolites, Antineoplastic
  • Drug Carriers
  • Liposomes
  • Polymers
  • Deoxycytidine
  • Squalene
  • Gemcitabine