Development and Characterization of 5-Fluorouracil Solid Lipid Nanoparticles for Treatment of Colorectal Cancer

Journal of Pharmaceutical Innovation(2022)

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摘要
Purpose In this study, the oral nanotherapeutic approach of 5-fluorouracil solid lipid nanoparticles (5-FU SLNs) for the synergistic treatment of colorectal cancer in preclinical DMH rat model is studied. Method 5-Fluorouracil solid lipid nanoparticles with solvent evaporation emulsification method by using different ratios of polymer and surfactant. Result 5-FU SLNs with chitosan and poloxamer 407 ratio of 2.4:0.1 has shown better particle size (147.9 ± 1.48 nm) with entrapment efficiency 90.60 ± 0.01% and loading content 3.40 ± 0.03%. In vitro, drug release studies were done by using simulated fluids at various pHs (1.2, 4.5, 7.5, and 7.0) to mimic the GIT tract and achieve 85.16 ± 0.26% at 24 h in a sustained manner. In the current investigation, treatment with 5-FU SLNs increased levels of SOD, CAT, and GSH in the colonic tissue which were considerably DMH-treated rats having lower level. It should be highlighted that the 5-FU SLNs anticancer activity on colorectal was superior over the course of the study, utilizing an in vivo model. Colonic tumour incidence, speed, size, and multiplicity, as well as the number of ACFs, have all decreased. Conclusion Collectively, based on the chitosan-TPP platform, these results suggest that both 5-fluorouracil solid lipid nanoparticles confirmed in vitro and in vivo has shown to provide a promising oral delivery for colorectal cancer. Graphic Abstract
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关键词
5-Fluorouracil, Solid lipid nanoparticles, Colorectal cancer
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