Formulation and Evaluation of Solid-Self Micro Emulsifying Drug Delivery System (S-SMEDDS) of Agomelatine

• Published in: Colloid journal of the Russian Academy of Sciences 2023-04, Vol.85 (2), p.276-286
• Main Authors: Priyanka Tomar, Saji, Jiya Mary, Patel, Darshana, Thakkar, Hetal
• Format: Article
• Language: English
• Subjects: Antidepressants; Bioavailability; Chemistry; Chemistry and Materials Science; Dilution; Drug delivery systems; Globules; Polymer Sciences; Solubility; Surfaces and Interfaces; Surfactants; Thin Films; Zeta potential
• ISSN: 1061-933X; 1608-3067
• DOI: 10.1134/S1061933X22600014

The aim of this study was to create a solid-self-micro emulsifying drug delivery system (S-SMEDDS) to improve the oral bioavailability of Agomelatine, which is weakly water soluble. Agomelatine, an antidepressant medication, is rapidly absorbed (>75%) after oral administration, but it has a low water solubility and significant first-pass metabolism, resulting in a low absolute bioavailability (4%). Based on solubility of Agomelatine, Capmul MCM (oil), Kolliphor EL (surfactant), PEG 400 (co-surfactant) and Neusilin US2 (solid carrier) were selected to prepare solid SMEDDS. The optimized formulation was stable with zeta potential of –28.0 ± 0.5 mV and globule size 105.2 ± 13.7 nm, PDI 0.32, pH 7.3 ± 0.2, cloud point 65 ± 1°C and assay 98.0 ± 0.6% which corresponds to L-SMEDDS. It was robust to dilution. TEM image showed uniformly distributed globules. The result of in-vitro drug release study suggested that there was greater drug release from Agomelatine S-SMEDDS as compared to plain drug suspension. S-SMEDDS drug release followed zero order kinetics, indicating that it is unaffected by drug concentration.