Abstract
Objective: The present study discusses paclitaxel (PTX)-loaded mannosylated-DSPE (Distearoyl-phosphatidyl-ethanolamine) solid lipid nanoparticles (M-SLNs) using mannose as a lectin receptor ligand conjugate for lung cancer targeting and to increase the anticancer activity of PTX against A549 lung’s epithelial cancer cells.
Materials and methods: The PTX-SLNs were prepared by solvent injection method and mannose was conjugated to the free amine group of stearylamine. The M-SLNs obtained were characterized for their particle size, polydispersity index, zeta potential and morphology by transmission electron microscope.
Results: The M-SLNs were spherical in shape with 254 ± 2.3 nm average size, positive zeta potential (3.27 mV), 79.4 ± 1.6 drug entrapment efficiency and showed the lower extent of drug release 40% over 48 h in vitro. Cytotoxicity study on A549 cell lines and biodistrubtion study of drug revealed that M-SLNs deliver a higher concentration of PTX as compared to PTX-SLNs in an alveolar cell site.
Discussion and conclusion: These results suggested that mannosylated M-SLNs are safe and potential vector for lung cancer targeting.
Acknowledgements
We express our sincere thanks to All India Institute of Medical Science (AIIMS), New Delhi, India for providing us the necessary facilities for conducting Transmission Electron Microscopy study of our developed formulation, NIPER Chandigarh for Particle size and zeta potential analysis, IR from Department of Chemistry, Dr H. S. Gour Central University, Sagar (M.P.). We would like to thank the Tata Memorial Advance Cancer Research Institute, Bombay, to provide lung cancer cell line (A549) for in vitro cytotoxic study.
Declaration of interest
The authors report no conflicts of interest. The authors alone are responsible for the content and writing of this article.