A Novel Emulgel-Based Oral Delivery Approach for Amlodipine Besylate: Formulation, Evaluation, and Kinetic Modelling

Background

Oral drugs like amlodipine besylate commonly have problems such as low water solubility and high first-pass metabolism, leading to changing plasma concentrations. Emulgel formulations offer a great solution as they combine the penetration and solubilizing effects of emulsions with the stability and controlled release of gels.

Materials and Methods

The present work entails the preparation of amlodipine besylate emulgel where Carbopol 934 has been used as the gelling agent. Pseudo, ternary phase diagrams were drawn using propane, 1, 2, diol, polyoxyethylene (20) sorbitan monooleate, and polyethylene glycol as the components to identify the microemulsion region. Stability tests indicated that a 2:1 ratio surfactant combination was most suitable. Six different formulations (F1, F6) were characterized for their physical characteristics, uniformity, pH, viscosity, spreadability, drug content, and drug release profile.

Results

Results of FTIR and DSC showed that drug and excipients were compatible and the stability of the formulation was ensured.

Conclusion

The formulation F4 had, among others, a good viscosity (3941 cP), pH of 6.2, drug content of 98.4%, and it was homogeneous in consistency. Its in vitro drug release was both controlled and according to the Higuchi model with a regression coefficient close to 0.99.