Development and Evaluation of Exenatide Loaded PLGA Nanoparticles for Intranasal Delivery in the Treatment of Obesity

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Background: Obesity, considered a complex condition, is the fastest-growing public health concern worldwide. Its treatment is limited due to the side effects of pharmacological options available, outweighing their benefits. Aim: The present study aims to formulate a novel biodegradable formulation of exenatide for direct brain delivery through the nasal route. Methods: To formulate exenatide loaded poly (lactide-co-glycolide) (PLGA) nanoparticles, a dou-ble emulsion (w/o/w) solvent evaporation method was employed. A full factorial (33) design of the experiment was used to optimize the formulation. Results: The entrapment efficiency and particle size of the optimized formulation were found to be 68% and 110 nm, respectively. The in-vitro drug release study indicated the sustained release of 48% drug in 5 days. The safety of drug-loaded PLGA nanoparticles for intranasal delivery was in-dicated by the sheep nasal toxicity study. The efficacy of the developed nanoparticles was demon-strated by an in-vivo pharmacodynamics study on Albino Wistar rats, showing a 6.2% weight reduc-tion after 30 days of treatment. Conclusion: Thus, exenatide is a novel peptide having significant weight loss benefits and no se-vere side effects. Long-term studies in at least two or more animal models followed by extensive clinical evaluation can safely result in a product for clinical use.