BILE ACID-BASED NANOPARTICLES FOR AUGMENTING ORAL BIOAVAILABILITY OF GLICLAZIDE: IN VITRO AND IN VIVO CHARACTERIZATION
DOI:
https://doi.org/10.22159/ajpcr.2026v19i6.58421Keywords:
Oral bioavailability, Gliclazide,, Solubility,, Bile acid,, NanoparticlesAbstract
Objectives: To investigate the ability of bile acid-based nanoparticles to improve the oral bioavailability of gliclazide (GCZ), which suffers from poor solubility, first-pass metabolism, and inter-subject variability.
Methods: A hot emulsification followed by ultrasonication technique was employed to prepare gliclazide nanoparticles (GLNs) using lipids and bile acid. The prepared GLNs were characterized, including solubility, dissolution rate, and permeability. The bioavailability of the GLNs was tested in rats in comparison with a marketed formulation.
Results: The prepared GLNs exhibited a particle size of 197.4 nm with a polydispersity index of 0.239, 1.33 mg/mL solubility, 4.37×10−5 cm/s permeability, and in vitro dissolution was improved to 67.1% from 9.8% of pure GCZ. The developed bioanalytical method exhibited linearity over 0.1–10 μg/mL. In vivo studies revealed that at a 10 mg/kg dose, the GLNs exhibited an improvement of 42.5% in Cmax and 47.7% in area under the curve when compared to the marketed formulation.
Conclusion: The experimental findings confirmed that the GLNs were a promising approach in overcoming the multiple limitations of GCZ to have high oral bioavailability.
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