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

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Abstract

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.

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Data Availability

Data included in article/supplementary material/referenced in article.

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Acknowledgements

The authors express their deep sense of gratitude towards Bharati Vidyapeeth College of Pharmacy (Kolhapur Maharashtra) and Government College of Pharmacy (Karad, Maharashtra) for provision of obligatory facilities to carry out present research work. Authors are profusely thankful to Dr. Riyaz Ali M. Osmani Department of Biosciences and Bioengineering, Indian Institute of Technology Bombay (IITB), Mumbai, for his valuable inputs and constructive suggestions.

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Authors and Affiliations

  1. Department of Pharmaceutical Chemistry, Ashokrao Mane College of Pharmacy, Peth Vadgaon, Maharashtra, India

    Poournima Patil

  2. Department of Pharmaceutical Chemistry, Bharati Vidyapeeth College of Pharmacy, Kolhapur, Maharashtra, India

    Poournima Patil & Harinath More

  3. Department of Pharmacognosy, Shree Sant Gajanan Maharaj College of Pharmacy, Mahagaon, Maharashtra, India

    Suresh Killedar

  4. Department of Pharmaceutical Chemistry, Rajarambapu College of Pharmacy, Kasegaon, Maharashtra, India

    Ganesh Vambhurkar

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  1. Poournima Patil
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Contributions

P. S. Patil: conceived and designed the experiments; contributed reagents, materials, analysis tools, or data; performed the experiments; and analyzed and wrote the paper. H. N. More: analyzed and wrote the paper. S. G. Killedar: conceived and designed the experiments; analyzed and interpreted the data; and wrote the paper. G. Wabhujkar: analyzed and interpreted the data and wrote the paper.

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Correspondence to Poournima Patil.

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Patil, P., Killedar, S., More, H. et al. Development and Characterization of 5-Fluorouracil Solid Lipid Nanoparticles for Treatment of Colorectal Cancer. J Pharm Innov 17, 1268–1281 (2022). https://doi.org/10.1007/s12247-021-09605-x

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