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Abstract

Introduction

Colorectal cancer is an important cause of cancer-related mortality, necessitating innovative therapies to improve efficacy and reduce side effects. This study explores the potential of Cisplatin and Rutin-loaded nanoliposomes (Cis-NLs and Rut-NLs) for anti-colorectal cancer activity.

Methods

Cis-NLs and Rut-NLs were prepared using thin-film hydration, achieving encapsulation efficiencies of 95.5% and 62.5%, respectively. Drug release studies revealed controlled profiles, with Cis-NLs showing a complete release (100%) and Rut-NLs reaching 23.48% over 48 hours. Stability assessments demonstrated minimal changes in size, polydispersity index (PDI), and zeta potential over three months. Encapsulation efficiency decreased slightly for Cis-NLs (92.87%) and significantly for Rut-NLs (26.55%). Several tests were performed to evaluate the biological activity of this combination on colorectal cancer cells and HDF cells to check its selectivity.

Results

cytotoxicity studies on HT29 colorectal cancer cells revealed IC values of 1.72 µg/mL for free Cisplatin, 2.35 µg/mL for Cis-NLs, >100 µg/mL for free Rutin, and 63.33 µg/mL for Rut-NLs. A combination of Cis-NLs and Rut-NLs reduced the IC to 2.2 µg/mL. Selective toxicity evaluation using human dermal fibroblasts showed an IC of 79.24 µM for cisplatin, reduced to 63.3 µM in Cis-NLs, with Rut-NLs demonstrating negligible toxicity.

Discussion

Wound healing assays confirmed significant inhibition of cell migration, with wound closure reduced from 62.41% in controls to 34.35% in treated groups. Utilizing nanotechnology, liposomal formulations were synthesized to enhance drug delivery and therapeutic synergy.

Conclusion

These results highlight the potential of Cisplatin and Rutin-loaded nanoliposomes as a combination therapy for colorectal cancer.

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2025-07-16
2025-09-27

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References

  1. Diori Karidio I. Sanlier S.H. Reviewing cancer’s biology: An eclectic approach. J. Egypt. Natl. Canc. Inst. 2021 33 1 32 10.1186/s43046‑021‑00088‑y 34719756
    [Google Scholar]
  2. Laconi E. Marongiu F. DeGregori J. Cancer as a disease of old age: Changing mutational and microenvironmental landscapes. Br. J. Cancer 2020 122 7 943 952 10.1038/s41416‑019‑0721‑1 32042067
    [Google Scholar]
  3. Bray F. Laversanne M. Sung H. Ferlay J. Siegel R.L. Soerjomataram I. Jemal A. Global cancer statistics 2022: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries. CA Cancer J. Clin. 2024 74 3 229 263 10.3322/caac.21834 38572751
    [Google Scholar]
  4. Ferlay J. Colombet M. Soerjomataram I. Parkin D.M. Piñeros M. Znaor A. Bray F. Cancer statistics for the year 2020: An overview. Int. J. Cancer 2021 149 4 778 789 10.1002/ijc.33588 33818764
    [Google Scholar]
  5. Anand P. Kunnumakara A.B. Sundaram C. Harikumar K.B. Tharakan S.T. Lai O.S. Sung B. Aggarwal B.B. Cancer is a preventable disease that requires major lifestyle changes. Pharm. Res. 2008 25 9 2097 2116 10.1007/s11095‑008‑9661‑9 18626751
    [Google Scholar]
  6. Darmadi D. Mohammadian-Hafshejani A. Kheiri S. Global disparities in colorectal cancer: Unveiling the present landscape of incidence and mortality rates, analyzing geographical variances, and assessing the human development index. J. Prev. Med. Hyg. 2025 65 4 E499 E514 10.15167/2421‑4248/jpmh2024.65.4.3071 40026425
    [Google Scholar]
  7. Kumar R. Harilal S. Carradori S. Mathew B. A comprehensive overview of colon cancer- a grim reaper of the 21st century. Curr. Med. Chem. 2021 28 14 2657 2696 10.2174/0929867327666201026143757 33106132
    [Google Scholar]
  8. Mármol I. Sánchez-de-Diego C. Pradilla Dieste A. Cerrada E. Rodriguez Yoldi M. Colorectal carcinoma: A general overview and future perspectives in colorectal cancer. Int. J. Mol. Sci. 2017 18 1 197 10.3390/ijms18010197 28106826
    [Google Scholar]
  9. Ditonno I. Novielli D. Celiberto F. Rizzi S. Rendina M. Ierardi E. Di Leo A. Losurdo G. Molecular pathways of carcinogenesis in familial adenomatous polyposis. Int. J. Mol. Sci. 2023 24 6 5687 10.3390/ijms24065687 36982759
    [Google Scholar]
  10. Gorzo A. Galos D. Volovat S.R. Lungulescu C.V. Burz C. Sur D. Landscape of immunotherapy options for colorectal cancer: Current knowledge and future perspectives beyond immune checkpoint blockade. Life 2022 12 2 229 10.3390/life12020229 35207516
    [Google Scholar]
  11. Neugut A.I. Lin A. Raab G.T. Hillyer G.C. Keller D. O’Neil D.S. Accordino M.K. Kiran R.P. Wright J. Hershman D.L. FOLFOX and FOLFIRI use in stage IV colon cancer: Analysis of SEER-medicare data. Clin. Colorectal Cancer 2019 18 2 133 140 10.1016/j.clcc.2019.01.005 30878317
    [Google Scholar]
  12. Vanneman M. Dranoff G. Combining immunotherapy and targeted therapies in cancer treatment. Nat. Rev. Cancer 2012 12 4 237 251 10.1038/nrc3237 22437869
    [Google Scholar]
  13. Han Y. Wen P. Li J. Kataoka K. Targeted nanomedicine in cisplatin-based cancer therapeutics. J. Control. Release 2022 345 709 720 10.1016/j.jconrel.2022.03.049 35367476
    [Google Scholar]
  14. Reedijk J. Lohman P.H.M. Cisplatin: Synthesis, antitumour activity and mechanism of action. Pharm. Weekbl. Sci. 1985 7 5 173 180 10.1007/BF02307573 3906559
    [Google Scholar]
  15. Ganeshpurkar A. Saluja A.K. The pharmacological potential of rutin. Saudi Pharm. J. 2017 25 2 149 164 10.1016/j.jsps.2016.04.025 28344465
    [Google Scholar]
  16. Gatasheh M.K. Identifying key genes against rutin on human colorectal cancer cells via ROS pathway by integrated bioinformatic analysis and experimental validation. Comput. Biol. Chem. 2024 112 108178 10.1016/j.compbiolchem.2024.108178 39191167
    [Google Scholar]
  17. Asnaashari S. Amjad E. Sokouti B. Synergistic effects of flavonoids and paclitaxel in cancer treatment: A systematic review. Cancer Cell Int. 2023 23 1 211 10.1186/s12935‑023‑03052‑z 37743502
    [Google Scholar]
  18. Bukhari I.A. Mohamed O.Y. Alhowikan A.M. Lateef R. Hagar H. Assiri R.A. Alqahtani W.M.A. Protective effect of rutin trihydrate against dose-dependent, cisplatin-induced cardiac toxicity in isolated perfused rat’s heart. Cureus 2022 14 1 e21572 10.7759/cureus.21572 35228931
    [Google Scholar]
  19. Al-Ekaid N.M. Al-Samydai A. Al-deeb I. Nsairat H. Khleifat K. Alshaer W. Preparation, characterization, and anticancer activity of PEGylated nano liposomal loaded with rutin against human carcinoma cells (HT29). Chem. Biodivers. 2023 20 11 e202301167 10.1002/cbdv.202301167 37781742
    [Google Scholar]
  20. Ismail A. El-Biyally E. Sakran W. An innovative approach for formulation of rutin tablets targeted for colon cancer treatment. AAPS PharmSciTech 2023 24 2 68 10.1208/s12249‑023‑02518‑7 36792766
    [Google Scholar]
  21. Al-Nasrawi H. Shalan N. Abualsoud B.M. Nsairat H. Preparation, characterization and in vitro evaluation of 5-fluorouracil loaded into chitosan–acacia gum nanoparticles. Ther. Deliv. 2024 15 5 339 353 10.4155/tde‑2023‑0136 38469691
    [Google Scholar]
  22. Tamma M.A. Nsairat H. El-Tanani M. Madi R. In vitro evaluation of lipidic nanocarriers for mebendazole delivery to improve anticancer activity. Drug Dev. Ind. Pharm. 2024 50 11 917 926 10.1080/03639045.2024.2428405 39527027
    [Google Scholar]
  23. Peleg-Shulman T. Gibson D. Cohen R. Abra R. Barenholz Y. Characterization of sterically stabilized cisplatin liposomes by nuclear magnetic resonance. Biochim. Biophys. Acta Biomembr. 2001 1510 1-2 278 291 10.1016/S0005‑2736(00)00359‑X 11342165
    [Google Scholar]
  24. Abdelnabi H. Alshaer W. Azzam H. Alqudah D. Al-Samydai A. Aburjai T. Loading of capsaicin-in-cyclodextrin inclusion complexes into PEGylated liposomes and the inhibitory effect on IL-8 production by MDA-MB-231 and A549 cancer cell lines. Z. Naturforsch. C J. Biosci. 2021 76 11-12 503 514 10.1515/znc‑2021‑0018 34036759
    [Google Scholar]
  25. Ballacchino G. Weaver E. Mathew E. Dorati R. Genta I. Conti B. Lamprou D.A. Manufacturing of 3D-printed microfluidic devices for the synthesis of drug-loaded liposomal formulations. Int. J. Mol. Sci. 2021 22 15 8064 10.3390/ijms22158064 34360832
    [Google Scholar]
  26. Slotte J.P. The importance of hydrogen bonding in sphingomyelin’s membrane interactions with co-lipids. Biochim. Biophys. Acta Biomembr. 2016 1858 2 304 310 10.1016/j.bbamem.2015.12.008 26656158
    [Google Scholar]
  27. Al-Samydai A. Al Qaraleh M. Al-Halaseh L.K. Abu Hajleh M.N. Carradori S. Abdulmaged M. Kareem R. Alzaidi H. Mousa A.K. M.; Al-Hiari, Y.; Nsairat, H.; Alshaer, W. Optimized rutin-incorporating PEGylated nanoliposomes as a model wit remarkable selectivity against PANK1 and MCF7 cell lines. Anticancer. Agents Med. Chem. 2025 ••• 25 10.2174/0118715206231749241209073759 39844565
    [Google Scholar]
  28. Martinho N. Santos T.C.B. Florindo H.F. Silva L.C. Cisplatin-membrane interactions and their influence on platinum complexes activity and toxicity. Front. Physiol. 2019 9 1898 10.3389/fphys.2018.01898 30687116
    [Google Scholar]
  29. Kodel H.A.C. Alizadeh P. Ebrahimi S.N. Machado T.O.X. Oliveira M.B.P.P. Fathi F. Souto E.B. Liposomes and niosomes: New trends and applications in the delivery of bioactive agents for cancer therapy. Int. J. Pharm. 2025 668 124994 10.1016/j.ijpharm.2024.124994 39586512
    [Google Scholar]
  30. ben Sghaier, M.; Pagano, A.; Mousslim, M.; Ammari, Y.; Kovacic, H.; Luis, J. Rutin inhibits proliferation, attenuates superoxide production and decreases adhesion and migration of human cancerous cells. Biomed. Pharmacother. 2016 84 1972 1978 10.1016/j.biopha.2016.11.001 27829548
    [Google Scholar]
  31. de Bono J.S. Tolcher A.W. Rowinsky E.K. The future of cytotoxic therapy: Selective cytotoxicity based on biology is the key. Breast Cancer Res. 2003 5 3 154 159 10.1186/bcr597 12793897
    [Google Scholar]
  32. Kessler M. Ubeaud G. Jung L. Anti- and pro-oxidant activity of rutin and quercetin derivatives. J. Pharm. Pharmacol. 2003 55 1 131 142 10.1211/002235702559 12625877
    [Google Scholar]
  33. Arfin S. Jha N.K. Jha S.K. Kesari K.K. Ruokolainen J. Roychoudhury S. Rathi B. Kumar D. Oxidative stress in cancer cell metabolism. Antioxidants 2021 10 5 642 10.3390/antiox10050642 33922139
    [Google Scholar]
  34. Deng X. Yang Z. Han M. Ismail N. Esa N.M. Razis A.F.A. Bakar M.Z.A. Chan K.W. Comprehensive insights into the combinatorial uses of selected phytochemicals in colorectal cancer prevention and treatment: Isothiocyanates, quinones, carotenoids, and alkaloids. Phytother. Res. 2025 39 1 413 452 10.1002/ptr.8378 39557422
    [Google Scholar]
  35. Bozzuto G. Calcabrini A. Colone M. Condello M. Dupuis M.L. Pellegrini E. Stringaro A. Phytocompounds and nanoformulations for anticancer therapy: A review. Molecules 2024 29 16 3784 10.3390/molecules29163784 39202863
    [Google Scholar]
/content/journals/acamc/10.2174/0118715206388843250709121645
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Investigating the Therapeutic Potential of Cisplatin- and Rutin-Loaded Nanoliposomes against Colorectal Cancer Cells
Bentham Science Publishers ; https://doi.org/10.2174/0118715206388843250709121645
/content/journals/acamc/10.2174/0118715206388843250709121645
/content/journals/acamc/10.2174/0118715206388843250709121645
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  • Article Type:     Research Article
Keywords: rutin ; cancer ; Liposomes ; cisplatin ; colorectal cancer ; stability

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