Long circulating polymeric nanoparticles of gemcitabine HCl using PLGA-PEG-PPG-PEG block co-polymer

Abstract

In this study, Gemcitabine (GEM) HCl is loaded in long-circulating polymeric nanoparticles (NPs) using PLGA- PEG-PPG-PEG in combination with succinic anhydride (SA) to overcome issues of rapid metabolism. The optimized batch had size of 230.9 nm, zeta potential of −15.4 mV, and a high entrapment efficiency (EE) of 69.69%. The in vitro drug release was sustained up to 72 h. The IC50 values for the MDA-MB-231 cancer cells for free GEM, GP NPs, and GS NPs were 110.47, 91.23, and 78.25 µM. The pharmacokinetic study of the formulated NPs on Sprague Dawley rats confirmed long circulation up to 72 h.

Graphical Abstract

In-vivo fate of Gem conventional injectable formulation Vs Presently developed GEM loaded SA-PLGA-PEG-PPG-PEG Nanoparticles (GS NPs)

Keywords:

• Gemcitabine
• long circulating
• polymeric nanoparticles
• PLGA
• PEG-PPG-PEG

Acknowledgments

The authors thank Shilpa Medicare Limited (Hyderabad, India) for providing gift sample of GEM HCl for conducting our research.

Disclosure statement

No potential conflict of interest was reported by the author(s).