Formulation, Box-Behnken Optimization, and Characterization of Iguratimod-Loaded Nanostructured Lipid Carriers for Enhanced Rheumatoid Arthritis Therapy (Research Article)

Author(s): Amit Kumar Pandey* and Amit Kumar

Abstract: Background: Iguratimod (IGU), a novel disease-modifying antirheumatic drug (DMARD), exhibits poor aqueous solubility and low oral bioavailability, limiting its therapeutic efficacy in rheumatoid arthritis (RA). Nanostructured lipid carriers (NLCs) offer a promising strategy to overcome these limitations. Methods: Iguratimod-loaded NLCs were prepared by the ultra-sonication method using glyceryl monostearate (solid lipid), oleic acid (liquid lipid, 7:3 ratio), and Tween 20 (surfactant). A Box-Behnken design (13 runs) was employed to optimize three independent variables: total lipid concentration (X1: 1–3% w/v), surfactant concentration (X2: 0.5–1.5% w/v), and sonication time (X3: 10–20 seconds), evaluating particle size (R1), polydispersity index (R2), and percentage drug entrapment (R3). Results: The optimized formulation showed a particle size of 143.7 nm, PDI of 0.211, and entrapment efficiency of 73.24 ± 1.23%. Zeta potential was −19.1 ± 0.3 mV. FTIR and DSC studies confirmed no drug-excipient incompatibility. TEM revealed spherical particles with smooth surfaces. In vitro drug release demonstrated sustained release of 83.18 ± 1.36% over 30 hours. Stability studies over 3 months showed optimal stability at refrigerated (2–8°C) and room temperature conditions. Conclusion: The optimized Iguratimod-loaded NLCs exhibited excellent physicochemical characteristics, sustained release profile, and stability, representing a promising oral delivery system for RA treatment.

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