Jump to main content
Jump to site search

Issue 65, 2016
Previous Article Next Article

Synthesis and characterization of TPGS–gemcitabine prodrug micelles for pancreatic cancer therapy

Author affiliations

Abstract

The therapeutic potential of a nucleoside analog, gemcitabine, is severely compromised due to its rapid clearance from systemic circulation by enzymatic degradation into an inactive metabolite. In the present investigation, micelles based on polymer–drug conjugate were developed for gemcitabine and investigated for their potential to improve cancer chemotherapy. The tocopherol poly(ethylene glycol) succinate 1000 (TPGS)–gemcitabine prodrug was synthesized via an amide linkage and characterised by analytical methods, including FT-IR, 1H NMR, and MALDI-TOF. The micellar formulation of TPGS–gemcitabine prodrug was developed by a self-assembly technique and evaluated for various physicochemical parameters including particle size, polydispersity, morphology, critical micelle concentration and release profile. It was observed that gemcitabine present in TPGS–gemcitabine micelles was resistant to deamination by crude cytidine deaminase. The improved cytotoxicity of the micellar formulation was observed using TPGS–gemcitabine micelles against pancreatic cancer cells. Further, it was found that, unlike native gemcitabine, nucleoside transporters were not required for TPGS–Gem micelles to demonstrate their anticancer potential. These findings revealed that TPGS–gemcitabine micelles may serve as a promising platform for gemcitabine in order to improve its anticancer efficacy.

Graphical abstract: Synthesis and characterization of TPGS–gemcitabine prodrug micelles for pancreatic cancer therapy

Back to tab navigation

Supplementary files

Article information


Submitted
11 Apr 2016
Accepted
14 Jun 2016
First published
15 Jun 2016

This article is Open Access

RSC Adv., 2016,6, 60126-60137
Article type
Paper
Author version available

Synthesis and characterization of TPGS–gemcitabine prodrug micelles for pancreatic cancer therapy

V. Khare, W. Al. Sakarchi, P. N. Gupta, A. D. M. Curtis and C. Hoskins, RSC Adv., 2016, 6, 60126
DOI: 10.1039/C6RA09347G

This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence. Material from this article can be used in other publications provided that the correct acknowledgement is given with the reproduced material and it is not used for commercial purposes.

Reproduced material should be attributed as follows:

  • For reproduction of material from NJC:
    [Original citation] - Published by The Royal Society of Chemistry (RSC) on behalf of the Centre National de la Recherche Scientifique (CNRS) and the RSC.
  • For reproduction of material from PCCP:
    [Original citation] - Published by the PCCP Owner Societies.
  • For reproduction of material from PPS:
    [Original citation] - Published by The Royal Society of Chemistry (RSC) on behalf of the European Society for Photobiology, the European Photochemistry Association, and RSC.
  • For reproduction of material from all other RSC journals:
    [Original citation] - Published by The Royal Society of Chemistry.

Information about reproducing material from RSC articles with different licences is available on our Permission Requests page.


Social activity

Search articles by author

Spotlight

Advertisements