Unraveling the Nano-Challenge: Plackett-Burman Formulation of Etodolac-Loaded, Folic Acid-Conjugated Nanoliposomes for Colon Delivery
نویسندگان
1 Department of pharmaceutics and Industrial pharmacy ,university of Kufa,Iraq
2 Department of pharmaceutics and Industrial pharmacy ,university of Kufa,Iraq
doi
10.22052/JNS.2026.01.018چکیده
This study aimed to formulate targeted nanoliposomes for cancer cell delivery. Liposomes were prepared using the thin-film hydration method, with optimization achieved through a Plackett-Burman design of experiments. Folic acid (FA) was employed as a ligand for targeted delivery. The independent variables included DSP weight, cholesterol weight, solvent volume, solubilization temperature, evaporation speed, rehydration temperature, rehydration rotation speed, extrusion number, and freeze-thaw cycles. The dependent variables (responses) were particle size, polydispersity index (PDI), entrapment efficiency (EE), and loading capacity (LC). The particle sizes of all formulations ranged from 99.1 to 250 nm, and the entrapment efficiencies ranged from 56.1% to 88.7%. The optimized formulations were characterized using FESEM, which revealed spherical liposomes without aggregation. DSC and FTIR analyses indicated the drug’s transformation to an amorphous state. MTT assays on SW480 cell lines confirmed the formulations’ safety. Cytotoxicity assays on SW480 cells demonstrated time- and concentration-dependent cytotoxicity. The IC50 values were: pure etodolac (713.72 ± 4.85 µg/mL at 24 hours, 536.98 ± 6.23 µg/mL at 48 hours), non-targeted liposomes (F1: 602.03 ± 2.8 µg/mL at 24 hours, 419.33 ± 3.55 µg/mL at 48 hours), and targeted liposomes (F2: 554.6 ± 9.12 µg/mL at 24 hours, 128.88 ± 5.26 µg/mL at 48 hours). Cellular etodolac uptake was measured as 12.54 ± 0.078 µg per 10^4 cells for pure etodolac, 20.48 ± 0.19 µg per 10^4 cells for F1, and 26.31 ± 0.11 µg per 10^4 cells for F2. The optimized formulations exhibited good stability over two months.