Design, Development, and In Vitro AGS Cell Survival of Rebamipide-Loaded Solid Lipid Nanoparticles for Gastric Cytoprotection in Peptic Ulcer Management

Authors

  • Rohit
  • Anuj Mittal

Keywords:

Rebamipide, Solid lipid nanoparticles, AGS cell line, Peptic ulcer, Gastroprotection, Nanomedicine, Sustained release, Neonatal mucosal injury

Abstract

Peptic ulcer disease (PUD), characterized by mucosal erosion in the stomach or duodenum, remains a significant global health concern. Rebamipide, a gastroprotective drug with anti-inflammatory and cytoprotective effects, suffers from poor water solubility and limited bioavailability, hindering its therapeutic efficacy. This study aimed to design and develop Rebamipide-loaded solid lipid nanoparticles (SLNs) to enhance gastric cytoprotection and investigate their performance using AGS human gastric epithelial cells in vitro. SLNs were prepared using the high-speed homogenization and ultrasonication method, with stearic acid as lipid and poloxamer 188 as a surfactant. The optimized formulation (F3) was characterized by particle size (~112 nm), polydispersity index (PDI = 0.204), zeta potential (−23.4 mV), and entrapment efficiency (~87.3%). Transmission electron microscopy confirmed spherical morphology and uniform distribution.

In vitro drug release studies demonstrated a sustained release of Rebamipide over 24 hours, with initial burst release followed by controlled diffusion. Stability studies at 25°C and 40°C for three months revealed minimal change in physicochemical properties. Cytotoxicity and cell survival studies using AGS cells showed enhanced viability and proliferation in cells treated with Rebamipide-SLNs compared to the drug suspension. The nanoformulated Rebamipide significantly promoted mucosal healing and provided a protective effect against ethanol-induced damage in vitro. The study highlights the potential of SLNs as a delivery system for poorly soluble drugs like Rebamipide and opens avenues for their application in pediatric and neonatal gastroprotection, especially in critical care scenarios. Further in vivo and clinical studies are warranted to confirm translational benefits.

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References

Tanigawa, T., Pai, R., Arakawa, T., & Tarnawski, A. S. (2007). Rebamipide inhibits gastric cancer cell growth. Digestive Diseases and Sciences, 52, 240–247. https://doi.org/10.1007/s10620-006-9226-x sciencedirect.com+15link.springer.com+15link.springer.com+15

Nagamatsu, K., et al. (2010). Rebamipide-induced downregulation of phospholipase D inhibits... Experimental & Molecular Medicine, 42, 8 56. https://doi.org/10.3858/emm.2010.42.8.056 nature.com

Arjun Narala, Swathi Guda, & Kishan Veerabrahma. (2019). Lipid nanoemulsions of Rebamipide: formulation, characterization, and in vivo evaluation. AAPS PharmSciTech, 20, 26. https://doi.org/10.1208/s12249-018-1225-7 link.springer.com+1academia.edu+1

Thapa, P., et al. (2022). Solid lipid nanoparticles of Rebamipide: formulation, characterization and in vivo pharmacokinetic evaluation. International Journal of Applied Pharmaceutics, 14(2), 143–150. https://doi.org/10.22159/ijap.2022v14i2.42945 sciencedirect.com+15academia.edu+15researchgate.net+15

Kak, M. (2025). Rebamipide in gastric mucosal protection and healing: An Asian perspective. World Journal of Gastrointestinal Pharmacology and Therapeutics, 16(1), 101753. https://doi.org/10.4292/wjgpt.v16.i1.101753 link.springer.com+2wjgnet.com+2en.wikipedia.org+2

Lee, J., et al. (2025). Rebamipide attenuates lupus nephritis by enhancing antioxidative... International Journal of Molecular Sciences, 26(12), 5809. https://doi.org/10.3390/ijms26125809

Tung, N. T., Park, C. W., Oh, T. O., Kim, J. Y., Ha, J. M., Rhee, Y. S., & Park, E. S. (2011). Formulation of solid dispersion of rebamipide evaluated in a rat model for improved bioavailability and efficacy. Journal of Pharmacy and Pharmacology, 63(12), 1539–1547. https://doi.org/10.1111/j.2042-7158.2011.01360.x mdpi.com+3journals.innovareacademics.in+3pubmed.ncbi.nlm.nih.gov+3

Noriaki Nagai, R. Sakamoto, S. Yamamoto, S. Deguchi, H. Otake, & T. Tanino. (2019). Solid nanocrystals of rebamipide promote recovery from indomethacin induced gastrointestinal bleeding. International Journal of Molecular Sciences, 20(20), 4990. https://doi.org/10.3390/ijms20204990 pmc.ncbi.nlm.nih.gov

Arjun Narala, S. Guda, & K. Veerabrahma. (2019). Lipid nanoemulsions of rebamipide: Formulation, characterization, and in vivo pharmacokinetic evaluation. AAPS PharmSciTech, 20(1), 26. https://doi.org/10.1208/s12249-018-1225-7 ouci.dntb.gov.ua+1journals.innovareacademics.in+1

Dudhipala, N., & Veerabrahma, K. (2022). Solid lipid nanoparticles of rebamipide: Formulation, characterization and in vivo pharmacokinetic evaluation. International Journal of Applied Pharmaceutics, 14(2), 143–150. https://doi.org/10.22159/ijap.2022v14i2.42945 pubmed.ncbi.nlm.nih.gov+5journals.innovareacademics.in+5ouci.dntb.gov.ua+5

Genta, R. M. (2003). Review article: The role of rebamipide in the management of inflammatory disease of the gastrointestinal tract. Alimentary Pharmacology & Therapeutics, 18 (Supplement 1), 8–13. https://doi.org/10.1046/j.1365-2036.18.s1.5.x journals.innovareacademics.in+1pubmed.ncbi.nlm.nih.gov+1

Park, C. W., Tung, N. T., Rhee, Y. S., Kim, J. Y., Oh, T. O., Ha, J. M., Chi, S. C., & Park, E. S. (2013). Physicochemical, pharmacokinetic and pharmacodynamic evaluations of novel ternary solid dispersion of rebamipide with poloxamer 407. Drug Development and Industrial Pharmacy, 39(6), 836–844. https://doi.org/10.3109/03639045.2012.674138 pubmed.ncbi.nlm.nih.gov+1journals.innovareacademics.in+1

Tanigawa, T., Pai, R., Arakawa, T., & Tarnawski, A. S. (2007). Rebamipide inhibits gastric cancer cell growth. Digestive Diseases and Sciences, 52, 240–247. https://doi.org/10.1007/s10620-006-9226-x ouci.dntb.gov.ua+4journals.innovareacademics.in+4pmc.ncbi.nlm.nih.gov+4

Hu, F. Q., Yuan, H., Zhang, H. H., & Fang, M. (2002). Preparation of solid lipid nanoparticles with clobetasol propionate by a novel solvent diffusion method in aqueous system. International Journal of Pharmaceutics, 239(1–2), 121–128. https://doi.org/10.1016/S0378-5173(02)00081-9 link.springer.com+1journals.innovareacademics.in+1

Kim, K. T., Lee, J. Y., Park, J. H., Cho, H. J., Yoon, I. S., & Kim, D. D. (2017). Capmul MCM/Solutol HS15-based microemulsion for enhanced oral bioavailability of rebamipide. Journal of Nanoscience and Nanotechnology, 17(4), 2340–2344. https://doi.org/10.1166/jnn.2017.13314 journals.innovareacademics.in

Nair, R., Kumar, A. C., Priya, V. K., et al. (2012). Formulation and evaluation of chitosan solid lipid nanoparticles of carbamazepine. Lipids in Health and Disease, 11, 72. https://doi.org/10.1186/1476-511X-11-72

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Published

2025-06-30

How to Cite

1.
Rohit R, Mittal A. Design, Development, and In Vitro AGS Cell Survival of Rebamipide-Loaded Solid Lipid Nanoparticles for Gastric Cytoprotection in Peptic Ulcer Management. J Neonatal Surg [Internet]. 2025Jun.30 [cited 2025Jul.11];14(32S):2842-5. Available from: https://jneonatalsurg.com/index.php/jns/article/view/7834

Issue

Vol. 14 No. 32S (2025): Journal of Neonatal Surgery

Section

Original Article

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