World Journal of
Pharmaceutical and Life Sciences

FORMULATION AND EVALUATION OF GASTRORETENTIVE MICROBALLOONS OF SAXAGLIPTIN

Rajeev Ranjan*, V. P. Gupta, Bhupendra Tiwari

ABSTRACT

Saxagliptin is an oral dipeptidyl peptidase-4 (DPP-4) inhibitor widely used in the management of type 2 diabetes mellitus. However, its relatively short biological half-life necessitates repeated dosing, which may reduce patient compliance. The present study was undertaken to formulate and evaluate gastroretentive floating microballoons of saxagliptin with the objective of prolonging gastric residence time and achieving sustained drug release. Gastroretentive microballoons were prepared using the solvent evaporation technique with suitable polymers such as ethyl cellulose and cellulose acetate in different ratios. The prepared formulations were optimized by varying the polymer concentration and drug-to-polymer ratio to obtain spherical, hollow microballoons with excellent floating ability and controlled drug release characteristics. The prepared formulations were evaluated for percentage yield, particle size, bulk density, tapped density, angle of repose, Carr's index, Hausner ratio, drug entrapment efficiency, buoyancy, swelling behavior, surface morphology, zeta potential, polydispersity index (PDI), in vitro drug release, and stability studies. Fourier Transform Infrared (FTIR) spectroscopy confirmed the absence of significant drug–polymer interactions, indicating the compatibility of saxagliptin with the selected excipients. Scanning Electron Microscopy (SEM) revealed spherical microballoons with smooth surfaces and hollow internal cavities, confirming successful formulation. Among all the formulations, F8 demonstrated the most desirable characteristics, exhibiting high production yield, excellent entrapment efficiency, prolonged floating behavior with buoyancy exceeding 90%, favorable particle size distribution, zeta potential of approximately –34.8 mV, PDI of 0.186, and sustained drug release extending up to 12 hours. Stability studies conducted according to ICH guidelines showed no significant changes in the physicochemical properties or drug release profile over the storage period. The study concludes that gastroretentive floating microballoons of saxagliptin represent a promising sustained-release drug delivery system capable of enhancing gastric retention, maintaining prolonged drug release, reducing dosing frequency, and improving patient compliance in the treatment of type 2 diabetes mellitus. The optimized formulation (F8) demonstrated superior pharmaceutical performance and may serve as an effective gastroretentive delivery platform for saxagliptin.

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