Formulation and Characterization of Self-Microemulsifying Drug Delivery System (SMEDDS) of Sertraline Hydrochloride.

Background: Sertraline hydrochloride is the most widely used selective serotonin reuptake inhibitor (SSRI) for treating several depressive disorders. The applicability of Sertraline hydrochloride is limited due to the extensive metabolism and poor oral bioavailability of 44%.

Objective: The current research focused on improving the solubility and oral bioavailability of Sertraline in the form of microemulsion developed by a self-micro emulsifying drug delivery system (SMEDDS) for significant antidepressant action.

Methods: SMEDDS were developed by selecting appropriate proportions of oil, surfactant, and cosolvent, and out of them, isopropyl myristate, tween 80, and propylene glycol were selected. The emulsification zone was demonstrated by a ternary phase diagram, and the compatibility was confirmed with Fourier-transformed infrared spectroscopy (FT-IR). The formulated SMEDDS was characterized by the robustness to dilution, globule size (GS), polydispersity index (PDI), viscosity, dissolution, diffusion study, and drug release kinetics study. The Patents US 9,770,509 B2, and US 2021/0236628 A1 were available for the SMEDDS.

Results: All the batches (A1-A9) passed the quality test, and A3 was selected as an optimized batch that doesn't show phase separation and precipitation. The optimized batch A3 showed globule size (101 nm), PDI (0.319), drug content (99.14 ± 0.35%), viscosity (10.71 ± 0.02 mPa), self-emulsification time (46 sec), drug release (98.25 ± 0.22%) within eight h, release kinetics (Higuchi), and the effective antidepressant action during diffusion studies.

Conclusion: An optimized batch A3 was observed, which was circular in shape and estimated by Transmission electron microscopy (TEM), passing all the thermodynamic stability testing with a loss of 0.271 mg of the drug after 90 days, and showed marked antidepressant action with higher stability.