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KMID : 0043320220450110822
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Archives of Pharmacal Research
2022 Volume.45 No. 11 p.822 ~ p.835
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Enhancement of S(+)-zaltoprofen oral bioavailability using nanostructured lipid carrier system
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Pham Thi Mai Anh
Lee Dong-Hoon
Na Young-Guk
Jin Min-Ki
Jung Min-Woo
Kim Ha-Eun
Yoo Hye-Lim
Won Jong-Hee
Lee Jae-Young
Baek Jong-Suep
Han Su-Cheol
Lee Hong-Ki
Cho Cheong-Weon
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Abstract
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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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KEYWORD
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Bioavailability, Box?Behnken design, Nanostructured lipid carrier, Optimization, S(+)-zaltoprofen.
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