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AAPS PharmSciTech

, Volume 16, Issue 4, pp 855–864 | Cite as

Development of Novel Docetaxel Phospholipid Nanoparticles for Intravenous Administration: Quality by Design Approach

  • Dharmendra K. Yadav
  • Harish Pawar
  • Shrikant Wankhade
  • Sarasija Suresh
Research Article

Abstract

The objective of this study was to develop novel docetaxel phospholipid nanoparticles (NDPNs) for intravenous administration. Modified solvent diffusion-evaporation method was adopted in the NDPN preparation. Central composite design (CCD) was employed in the optimization of the critical formulation factor (drug content) and process variable (stirring rate) to obtain NDPNs with 215.53 ± 1.9-nm particle size, 0.329 ± 0.02 polydispersity index (PDI), and 75.41 ± 4.81% entrapment efficiency. The morphological examination by transmission electron microscopy revealed spherical structure composed of a drug core stabilized within the phospholipid shell. Enhanced cell uptake of coumarin-6-loaded phospholipid nanoparticles by MCF-7 cell line indicated NDPN-efficient cell uptake. In vitro hemolysis test confirmed the safety of the phospholipid nanoparticles. NDPNs exhibited increased area under the curve (AUC) and mean residence time (MRT) by 3.0- and 3.3-fold, respectively, in comparison with the existing docetaxel parenteral formulation (Taxotere®), indicating a potential for sustained action. Thus, the novel NDPNs exhibit an ability to be an intravenous docetaxel formulation with enhanced uptake, decreased toxicity, and prolonged activity.

KEY WORDS

cancer delivery vehicle docetaxel phospholipid nanoparticles nanoparticles pharmacokinetics 

Notes

Acknowledgments

The authors wish to express their gratitude to the Mr. Ashok K. Datusalia, Piyush Dave, Prashant Gupta (Department of Pharmacology and Toxicology), and Charan Singh (Department of Pharmaceutical Technology) for their valuable support in conducting the animal studies. We thank Lipoid (GmbH, Germany) for providing gift samples of phospholipids.

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Copyright information

© American Association of Pharmaceutical Scientists 2015

Authors and Affiliations

  • Dharmendra K. Yadav
    • 1
  • Harish Pawar
    • 1
  • Shrikant Wankhade
    • 1
  • Sarasija Suresh
    • 1
  1. 1.Department of Pharmaceutical Technology (Formulation)National Institute of Pharmaceutical Education and Research (NIPER)SAS Nagar (Mohali)India

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