Abstract
Zaltoprofen is a nonsteroidal anti-inflammatory drug with poor oral bioavailability. S(+)-zaltoprofen (SZPF)-loaded nanostructured lipid carriers (NLCs) were prepared to enhance oral bioavailability. SZPF-loaded NLCs (NLC-SZPF) were prepared using the hot-melting homogenization method and optimized using the Box-Behnken design. The characterization of optimized NLC-SZPF, in vitro release, cytotoxicity, cellular uptake, ex vivo permeability, and pharmacokinetic parameters were evaluated to confirm the advantages of NLC formulation. NLC-SZPF with a diameter of 105.5 ± 1.2 nm had a high encapsulation efficiency of 99.84 ± 0.01%. NLC-SZPF showed a sustained-release profile, high biocompatibility, and high permeability across the intestinal tract. The relative bioavailability of NLC-SZPF was 431.3% compared with that of SZPF after oral administration to experimental rats. NLC-SZPF was successfully optimized using experimental designs to enhance the oral bioavailability of SZPF. Hence, NLC-SZPF could be a promising approach to overcome the poor oral bioavailability of SZPF.
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Acknowledgements
This work was supported by the Basic Science Research Program (2019R1A2C1086102) through the National Research Foundation of Korea (NRF). We would like to acknowledge the financial support from the Korea Institute of Toxicology (KIT, Korea) grant funded by the National Research Council of Science & Technology (NST) Grant by the Korea government (MSIT) (Grant No. CRC21021-600).
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Pham, T.M.A., Lee, D.H., Na, YG. et al. Enhancement of S(+)-zaltoprofen oral bioavailability using nanostructured lipid carrier system. Arch. Pharm. Res. 45, 822–835 (2022). https://doi.org/10.1007/s12272-022-01413-2
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DOI: https://doi.org/10.1007/s12272-022-01413-2