Thiolated Poloxamer F127–assisted self–nanoemulsifying drug delivery system for mefenamic acid: An in vitro physicochemical proof–of–concept study

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Background: Mefenamic acid is an effective non–steroidal anti–inflammatory drug (NSAID) used for dysmenorrhea and musculoskeletal pain, but its clinical use is limited by poor aqueous solubility, short half–life, and dose–related gastrointestinal adverse effects. Formulation strategies that enhance dissolution and modulate drug release may improve formulation performance and drug delivery characteristics. Objective: This study aimed to develop and physicochemically characterise a thiolated Poloxamer F127–assisted self–nanoemulsifying drug delivery system (Th–Polo–F127 SNEDDS) for mefenamic acid with improved encapsulation, stability, mucoadhesion, and in vitro release behaviour. Methods: SNEDDS were prepared using oleic acid as the oil phase, Tween 80 as the surfactant, and PEG 400 as the co–surfactant. Poloxamer F127 was thiolated using EDC ⁄ NHS chemistry and incorporated into the optimised formulation. The nanoformulation was evaluated for droplet size, polydispersity index (PDI), zeta potential, thermodynamic stability, entrapment efficiency, in vitro drug release, and mucoadhesion. Structural modification was confirmed using FTIR and DSC analyses. Results: The thiolated SNEDDS exhibited a mean droplet size of 215.6 ± 115.7 nm with a PDI of 0.23 and a zeta potential of −19.4 ± 7.16 mV. Entrapment efficiency increased to 82%, while cumulative drug release reached 97% over 72 h at pH 6.8. Mucoadhesion studies demonstrated enhanced interaction with mucin dispersion, consistent with thiol–mediated interfacial interactions. Conclusion: These findings demonstrate improved in vitro physicochemical performance of the Th–Polo–F127 SNEDDS, including enhanced drug entrapment, mucoadhesive interaction, colloidal stability, and sustained release. Further pharmacokinetic, analgesic efficacy, and gastrointestinal safety studies are required to determine whether these formulation–level advantages translate into therapeutic benefit.

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