Fexofenadine-loaded chitosan coated solid lipid nanoparticles (SLNs): A potential oral therapy for ulcerative colitis
The targeting and mucoadhesive features of chitosan (CS)-linked solid lipid nanoparticles (SLNs) were exploited to efficiently deliver fexofenadine (FEX) into the colon, forming a novel and potential oral therapeutic option for ulcerative colitis (UC) treatment. Different FEX-CS-SLNs with varied molecular weights of CS were prepared and optimized. Optimized FEX-CS-SLNs exhibited 229 ± 6.08 nm nanometric size, 36.3 ± 3.18 mV zeta potential, 64.9 % EE, and a controlled release profile. FTIR, DSC, and TEM confirmed good drug entrapment and spherical particles. Mucoadhesive properties of FEX-CS-SLNs were investigated through mucin incubation and exhibited considerable mucoadhesion. The protective effect of FEX-pure, FEX-market, and FEX-CS-SLNs against acetic acid-induced ulcerative colitis in rats was examined.
Oral administration of FEX-CS-SLNs for 14 days before ulcerative colitis induction reversed UC symptoms and almost restored the intestinal mucosa to normal integrity and inhibited Phosphatidylinositol-3 kinase (73.6 %), protein kinase B (73.28 %), and elevated nuclear factor erythroid 2-related factor 2 (185.9 %) in colonic tissue. Additionally, FEX-CS-SLNs inhibited tumor necrosis factor α (TNF-α) and interleukin 6 (IL-6) to (70.79 % & 72.99 %) in colonic tissue. The ameliorative potential of FEX-CS-SLNs outperformed that of FEX-pure and FEX-market. The exceptional protective effect of FEX-CS-SLNs makes it a potentially effective oral system for managing ulcerative colitis.
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Materials
FEX (purity > 99 %) was gifted from Amoun Pharmaceuticals and Chemical Industries (Cairo, Egypt). Cetyl palmitate (purity > 98 %) was procured from Sigma Aldrich Chemical Co. (St. Louis, MO, USA). Chitosan (LMW, MMW, and HMW) was purchased from Sigma Aldrich Chemical Co. (St. Louis, MO, USA). Tween® 20 was gifted from Sigma Pharmaceuticals (Quesna, Egypt). Mucin, type II, was purchased from Alpha Chemika Co.(Mumbai, Maharashtra, India). Ethanol, sodium hydroxide, hydrochloric acid, and sodium.
Walaa A. El-Dakroury, Moataz B. Zewail, Gihan F. Asaad, Heba M.I. Abdallah, Marwa E. Shabana, Abdelrahman R. Said, Ahmed S. Doghish, Hadeer A. Azab, Dalia H. Amer, Ahmed E. Hassan, Alaa S. Sayed, Ghada M. Samra, Al-Aliaa M. Sallam, Fexofenadine-loaded chitosan coated solid lipid nanoparticles (SLNs): A potential oral therapy for ulcerative colitis, European Journal of Pharmaceutics and Biopharmaceutics, Volume 196, 2024, 114205, ISSN 0939-6411, https://doi.org/10.1016/j.ejpb.2024.114205.