Gliclazide loaded spanlastic nanovesicles: empowering bioavailability and antidiabetic efficacy.

Abstract

Objective: This work aimed to prepare spanlastics nanovesicles (SNVs) loaded with gliclazide (GCZ) to increase the drug's oral bioavailability and anti-diabetic effects.

Methods: Two types of edge activators (tween 80 and/or brij35) and two types of spans (span 60 and span 80) were used to prepare SNVs using the ethanol injection method,2³ factorial design was used to investigate the effects of various span types, edge activator types, and the ratio of span to edge activator.

Results: The optimum formulation (F6) was selected and its in-vitro drug release, in-vivo pharmacokinetics, and pharmacodynamics were evaluated. A transition electron microscope (TEM) showed spherical particles with smooth surfaces, (F6) drug release was (Q₁₂ 97.05 ± 4.85) while GCZ powder was (97.89 ± 4.56 after 4 h) also showed better entrapment efficiency (EE% 95.1 ± 3.8). In- vivo pharmacokinetic study showed an increase in C_max and t_max (12.93 ± 1.34, 3.2 ± 0.83) compared to unprocessed GCZ powder (2.88 ± 1.59, 1.8 ± 0.74). In-vivo pharmacodynamics study of diabetic rats demonstrated that GCZ-loaded SNVs has a higher % maximum decrease in blood glucose levels (MR) 58.31 ± 5.70 compared to 38.33 ± 8.18 for free drug and % total drop in blood glucose levels (TD) 25.78 ± 5.31% for GCZ-SNVs compared to 20.26 ± 6.05% for free drug. Histopathological examination revealed no cytotoxic signs in any of the examined samples.

Conclusion: Results revealed a significant rise in relative bioavailability, sustained and prolonged drug release when compared to the unprocessed GCZ powder.