Development of docetaxel-loaded PEG–PLA nanoparticles using surfactant-free method for controlled release studies

ABSTRACT

Docetaxel (DTX)-loaded poly(ethylene glycol)–poly(D,L-lactide) is prepared by nanoprecipitation method in the absence of any surfactants. The average particle size of the copolymer was found to be 101 nm. The drug entrapment efficiency (%) and drug loading (%) of polymer were found to be 9.471 ± 0.047 and 94.71 ± 0.466, respectively. The in vitro drug release characteristics show the controlled release of 98% of docetaxel in 72 h. The 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and apoptosis measured in terms of cleaved Poly(ADP-ribose) Polymerase (PARP) and cleaved caspase-3 protein expression shows that the copolymer has better cytotoxicity effect and apoptosis in comparison to free DTX in HeLa cells.

GRAPHICAL ABSTRACT

KEYWORDS:

• Drug delivery systems
• micelles
• nanoparticles
• PEG–PLA

Acknowledgments

The authors wish to acknowledge the grant-in-aid received from Department of Science and Technology (DST), New Delhi, for Project No. SR/S1/PC-24/2009. Kind help of Dr. Rajakishore Mishra, Centre for Life Sciences (CLS), and Prof. A. N. Misra, Head, CLS, Central University of Jharkhand, for providing necessary laboratory facilities to perform the biological studies, is also gratefully acknowledged. University fellowship to Prajna Mishra for pursuing her PhD is thankfully acknowledged.

Additional information

Funding

This work was supported by the Department of Science and Technology, New Delhi [Grant Number SR/S1/PC-24/2009].