Journal
PHARMACEUTICAL RESEARCH
Volume 35, Issue 5, Pages -Publisher
SPRINGER/PLENUM PUBLISHERS
DOI: 10.1007/s11095-017-2337-6
Keywords
Erlotinib; paclitaxel; solid lipid core nanocapsules; non-small cell lung cancer
Funding
- National Research Foundation of Korea (NRF) grant - Korea government (MSIP) [2015R1A2A2A01004118, 2015R1A2A2A04004806]
- National Research Foundation of Korea (NRF) grant - Korea government (MSIP) (Medical Research Center Program through the NRF - MSIP) [2015R1A5A2009124]
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Purpose 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. Methods 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 pH7.4 and pH5.0 were studied and analyzed. In vitro cytotoxicity and cellular uptake and apoptosis assays were performed in NCI-H23 cells. Results 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 timedependent uptake by NCI-H23 cells and caused dosedependent 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. Conclusion PTX/ERL-SLCN could be employed as an optimal approach for combination chemotherapy of NSCLC.
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