Spray dried self-nanoemulsifying drug delivery systems for sertraline HCl: Pharmacokinetic study in healthy volunteers

Hussein O. Ammar, Mahmoud M. Ghorab, Dina M. Mostafa, and Amira M. Ghoneim*

Purpose: The aim of this study is to improvelow oral bioavailability of sertraline HCl by formulation and characterization ofsolid self-nanoemulsifying drug delivery system [SNEDDS] using spray drying technique.

Methods: Solubility of sertraline HCl in different vehicles was determined, and ternary phase diagrams were constructed.Various formulations were prepared and characterized by morphological characterization, differential scanning calorimetry and droplet size analysis. The formulations were evaluated for in vitro release profile in comparison to the marketed product [Lustral® tablets]. The in vivo study was performed on healthy human volunteers for pharmacokinetic analysis of the optimized formulations.

Results: In vitro release data showed significant improvement of dissolution rate of sertraline HCl in form of liquid SNEDDS compared to the plain drug. Optimized liquid SNEDDS were chosen for the preparation of solid SNEDDS by spray drying technique. High dissolution efficiency values of solid SNEDDS indicated the increase in dissolution characteristics of sertraline HCL in solid SNEDDS. F6 SNEDDS, comprising Capmul® 20%, Cremophor® 53.4%, Transcutol® 26.6% showed highervalues for AUC[0-72 h], AUC [0-∞] and AUMC[0-72h] compared to Lustral® tablets.

Conclusion: The prepared formulation reveals the potentiality of incorporating sertraline HCl in a SNEDDS formulation to improve the biological performance of the drug.

Keywords: Sertraline HCl; Spray drying; Self-Nanoemulsifying; Release, Bioavailability; Pharmacokinetics; Anti-depressives

Published on: Jun 27, 2018 Pages: 9-19

Full Text PDF Full Text HTML DOI: 10.17352/ijpsdr.000017
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