Solid Nanoemulsion Preconcentrate (NanOsorb) for Oral Delivery of Sertraline: Development and Characterization

Md.      Akhlaquer Rahman; Zeenat      Iqbal; Arshad      Hussain

Abstract

The purpose of this study was to develop a solid nanoemulsion preconcentrate (NanOsorb) for poorly watersoluble drug sertraline (SRT). The liquid SNEDDS consisted of LabrafilM 2125 CS and Maisine 35-1 in 1:1 ratio as oil phase, Tween 80 as surfactant, Lauroglycol 90 as co-surfactant and active constituent sertraline free base. SRT free base, rather than commercially available hydrochloride salts (SRT.HCl) was used due to its much higher solubility in lipidic solvents. The NanOsorb formulation was prepared by adsorbing the liquid SNEDDS on different solid adsorbents. Reconstitution properties of both liquid and solid formulation demonstrate insignificant difference (p > 0.05) in the globule size. External morphology and physical state of sertraline in NanOsorb formulation were examined by TEM, DSC, and X-ray powder diffraction. In vitro release profile of NanOsorb was found to be significant (p < 0.001) in comparison to the plane SRT in pH 1.2, 4.5 and 6.8 buffers. Formulation was subjected to stability studies as per International Conference on Harmonization (ICH) guidelines and was found to be stable. No significant variations were observed in the formulation over a period of 3 months at accelerated conditions. Results deduced that NanOsorb formulation may provide an improvement in dissolution profile of poorly water-soluble drugs in the form of solid dosage form.

Keywords: Sertraline, oral delivery, solid nanoemulsion preconcentrate (NanOsorb), solid carrier, stability, SEDDS, SNEDDS, Pseudoternary Phase, co-surfactant, pseudo-ternary phase, Globule, Reconstitution, nanoemulsions, phosphotungstic acid, Diffraction