Aim:

This study aims to enhance Glimepiride’s (GMP) solubility and transdermal permeability by developing a matrix-type transdermal patch to improve systemic bioavailability, circumvent first- pass metabolism and decrease dosing frequency.

Materials and Methods:

Matrix-type transdermal patches were developed using the solvent-casting method. Initially, formulations were prepared with varying concentrations of polymers and GMP. Formulations were optimized using a quality-by-design approach using response surface methodology (Box-Behnken Design) via Design of Expert (DoE) software, version 8.0.4. Final formulations included Glimepiride in two forms: (a) solid dispersions of GMP (F4) and (b) pure GMP (F7). These formulations were characterized using various analytical techniques. Quantification of Glimepiride from the Transdermal Drug Delivery System (TDS) patches was conducted using the HPLC technique.

Results:

In vivo experiments such as hypoglycaemic effect, Skin sensitization and irritations test were performed on adult C57BL6/J mice. Other hand, the in vitro drug release to be fond 99.7±0.99 % and 93.7±1.2 % respectively. Similarly, permeability rates for patch (F4 and F7) of 0.141±0.02 and 0.120±0.04 mg/cm²/hr were recorded respectively. The results demonstrated that the solid dispersion formulation of GMP (F4) exhibited superior permeation and physicochemical properties compared to the pure GMP formulation (F7).

Conclusion:

In conclusion, the proposed transdermal formulation may serve as an alternative to solid oral formulations, effectively bypassing first-pass metabolism and minimizing the frequency of dosage administration.