Paclitaxel and Erlotinib-co-loaded Solid Lipid Core Nanocapsules: Assessment of Physicochemical Characteristics and Cytotoxicity in Non-small Cell Lung Cancer



Lung cancer is the leading cause of cancer-related deaths. The aim of this study was to design solid lipid core nanocapsules (SLCN) comprising a solid lipid core and a PEGylated polymeric corona for paclitaxel (PTX) and erlotinib (ERL) co-delivery to non-small cell lung cancer (NSCLC), and evaluate their physicochemical characteristics and in vitro activity in NCI-H23 cells.


PTX/ERL-SLCN were prepared by nanoprecipitation and sonication and physicochemically characterized by dynamic light scattering, transmission electron microscopy, differential scanning calorimetry, X-ray diffraction, and Fourier-transform infrared spectroscopy. In vitro release profiles at pH 7.4 and pH 5.0 were studied and analyzed. In vitro cytotoxicity and cellular uptake and apoptosis assays were performed in NCI-H23 cells.


PTX/ERL-SLCN exhibited appropriately-sized spherical particles with a high payload. Both PTX and ERL showed pH-dependent and sustained release in vitro profiles. PTX/ERL-SLCN demonstrated concentration- and time-dependent uptake by NCI-H23 cells and caused dose-dependent cytotoxicity in the cells, which was remarkably greater than that of not only the free individual drugs but also the free drug cocktail. Moreover, well-defined early and late apoptosis were observed with clearly visible signs of apoptotic nuclei.


PTX/ERL-SLCN could be employed as an optimal approach for combination chemotherapy of NSCLC.

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Acetate buffer solution


Didodecyldimethylammonium bromide


Dynamic light scattering


Dulbecco’s Modified Eagle’s medium


Dimethyl sulfoxide


Differential scanning calorimetry


Epidermal growth factor receptor




Fluorescence-activated cell sorting


Fetal bovine serum


Fourier-transform infrared spectroscopy


Glyceryl monostearate


High-performance liquid chromatography


Loading capacity


Loading efficiency


3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide


Molecular weight cut-off


Non-small cell lung cancer


Phosphate-buffered saline


Polydispersity index


Poly(ethylene glycol)




Small cell lung cancer


Soya lecithin


Solid lipid core nanocapsules


Transmission electron microscopy


Tyrosine kinase inhibitor


X-ray diffraction


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Acknowledgments and Disclosures

This research was supported by the National Research Foundation of Korea (NRF) grant funded by the Korea government (MSIP) (No. 2015R1A2A2A01004118, 2015R1A2A2A04004806, and by the Medical Research Center Program (2015R1A5A2009124) through the NRF funded by MSIP).

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Correspondence to Chul Soon Yong or Jong Oh Kim.

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Gupta, B., Poudel, B.K., Regmi, S. et al. Paclitaxel and Erlotinib-co-loaded Solid Lipid Core Nanocapsules: Assessment of Physicochemical Characteristics and Cytotoxicity in Non-small Cell Lung Cancer. Pharm Res 35, 96 (2018).

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Key Words

  • Erlotinib
  • paclitaxel
  • solid lipid core nanocapsules
  • non-small cell lung cancer