Formulation and characterization of Liquid Crystalline Hydrogel of Agomelatin: In vitro and Ex vivo evaluation

Objective: The aim of this investigation was the development and characterization of Agomelatin-loaded liquid crystalline (AM-LC) nanoparticles for improved topical application.

Methods: AM-LC was formulated with the glyceryl monooleate (GMO) and poloxamer 407 as structure forming agent (lipid) and surfactant respectively, by using emulsification of GMO and poloxamer in water using a hydrotrope (Cubosomes) formation method. The obtained dispersion was characterized for particle size, PDI, zeta potential, entrapment efficiency, surface morphology, in vitro studies. Further, conversion optimised formulation in to cubic gel by incorporating 0.5% w/w of carbopol 934P. The prepared gel was characterized by rheological measurements, surface pH and ex vivo permeation studies through the rat skin.

Results: The average particle size of formulations was ranging from 187.6±3.97nm to 225.8±7.54nm and ZP from -14.5±4.65 to -23.5±3.86mV. In vitro drug release from cubosomes exhibited sustained release profile and the optimized formulation (F2) showed cumulative drug release of 83.96±2.43% during 24h. Transmission electron microscopic photographs confirmed that the formed liquid crystalline nanoparticles were cubic in shape. Results suggested that cubic gel exhibited a retarded release rate (53.5 ± 3.21%) than the control gel (95.33 ± 2.28%) containing 0.1% drug solution.

Conclusion: The obtained results indicated that cubic gel would be a promising carrier for topical delivery of agomelatin into and across the skin.