Development and Characterization of Modified Release Dosage Form Utilizing Semaglutide

An agonist of the glucagon-like peptide-1 (GLP-1) receptor, semaglutide, when administered as a pure medication solution, has a significant degree of variability in bioavailability due to its low solubility and low permeability. This variability is reflected in the wide range of plasma concentration values (5.85–38.14), affecting its therapeutic effectiveness. The present study aimed to develop and characterize a modified-release dosage form (FPR-8) to enhance the pharmacokinetic profile of Semaglutide by ensuring controlled and sustained drug release over 24 hours, thereby reducing fluctuations in plasma concentration and improving bioavailability. The optimized formulation FPR-8 was developed and evaluated for its drug release profile, pharmacokinetic parameters, and in vivo performance in animal models. The improved formulation's plasma concentration values were contrasted with those of a pure drug solution. Administration of FPR-8 resulted in significantly reduced variability in plasma concentration values (4.12–19.46) compared to the pure drug suspension. The controlled-release formulation facilitated slow and gradual absorption, ensuring prolonged systemic circulation of Semaglutide over 24 hours. This sustained-release effect contributed to enhanced bioavailability and reduced fluctuations, addressing the limitations associated with the pure drug's pharmacokinetic profile. The development of a modified-release dosage form (FPR-8) successfully optimized the pharmacokinetic behavior of Semaglutide, ensuring consistent absorption, prolonged circulation, and reduced intersubject variability. This approach holds promise for improving therapeutic efficacy and patient compliance in the clinical use of Semaglutide.