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Formulation, Optimisation, and In Vitro Evaluation of Polymeric Nanoparticles for Enhanced Oral Delivery of Semaglutide

Year: 2026
Type: article
Abstract: Oral delivery of peptide therapeutics is limited by enzymatic degradation in the gastrointestinal tract and poor intestinal permeability. Semaglutide, a glucagon-like peptide-1 (GLP-1) receptor agonist used for the treatment of type 2 diabetes and obesity, is primarily administered via injection, which may reduce patient compliance. In this study, semaglutide-loaded polymeric nanoparticles were prepared using the solvent evaporation method and optimized using a Box–Behnken design. The effects of polymer concentration, surfactant concentration, and homogenization speed were evaluated on particle size, polydispersity index (PDI), and encapsulation efficiency. The optimized formulation was further characterized for physicochemical properties, drug loading, and in vitro drug release behaviour. The optimized nanoparticles exhibited a particle size of 145 ± 8 nm, PDI of 0.18 ± 0.02, and zeta potential of −22.5 ± 1.6 mV. Encapsulation efficiency and drug loading were found to be 78.4 ± 2.3% and 9.6 ± 0.8%, respectively. In vitro release studies showed an initial release of 28.3% within 6 hours, followed by sustained release reaching 85.6% over 48 hours. Stability studies demonstrated minimal changes in physicochemical properties over 30 days. Overall, the developed polymeric nanoparticle system shows promise as an effective strategy for enhancing the oral delivery of semaglutide. Further in vivo studies are required to confirm its bioavailability and therapeutic potential.
Language: English
Open Access status: bronze
OpenAlex ID: W7155506751
FWCI:
Cites: 32
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Related to: 10