The therapeutic potential of a nucleoside analog, gemcitabine, is severely compromised due to its rapid clearance from systemic circulation by enzymatic degradation into 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 amide linkage and characterised by analytical methods, including FT-IR, 1 H-NMR, and MALDI-TOF.The micellar formulation of TPGS-Gemcitabine prodrug was developed by self-assembly technique and evaluated for various physicochemical parameters including particle size, polydispersity, morphology, critical micelle concentration and release profile. It was shown observed that gemcitabine present in TPGS-Gemcitabine micelles were resistant to deamination from crude cytidine deaminase. The improved cytotoxicity of the micellar formulation was observed by TPGS-Gemcitabine micelles against pancreatic cancer cells. Further, it was investigated that unlike native gemcitabine, the nucleoside transporters were not required for TPGS-Gem micelles to demonstrate its anticancer potential. These finding revealed that TPGS-Gemcitabine micelles may serve as a promising platform for gemcitabine in order to improve its anticancer efficacy.
Correction for ‘Synthesis and characterization of TPGS–gemcitabine prodrug micelles for pancreatic cancer therapy’ by Vaibhav Khare et al., RSC Adv., 2016, 6, 60126–60137.
Further correction for ‘Synthesis and characterization of TPGS–gemcitabine prodrug micelles for pancreatic cancer therapy’ by Vaibhav Khare et al., RSC Adv., 2016, 6, 60126–60137.
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