Abstract
The purpose of the study was to combine the advantages of self-nanoemulsifying drug delivery systems and tablets as a conventional dosage form. Self-nanoemulsifying drug delivery system (SNEDDS) was prepared to enhance the solubility and thus oral bioavailability of sertraline. Aqueous titration method was used to prepare the liquid SNEDDS; ternary phase diagrams were constructed and based on smaller droplet size (24.8 nm), minimum viscosity (153.63 cP) and polydispersity index (0.182), higher percentage transmittance (95%) and in vitro drug release (97%), an optimum system was designated. Liquid SNEDDS was transformed into free-flowing powder by solid adsorption technique followed by compression into tablets. In vitro release of sertraline from liquid and solid SNEDDS was found to be highly significant compared to plain sertraline (p<0.01). Pharmacokinetic studies after oral administration of liquid and solid SNEDDS in rats showed about 6-and 5-fold increased absorption of sertraline compared to the aqueous suspension of sertraline. These studies demonstrate that the solid SNEDDS are promising strategies for successful delivery of poorly water-soluble drug like sertraline.
Highlights
Sertraline (SRT) free base (Figure 1) is lipophilic, poorly water-soluble drug (3.5 mg/L) belonging to the category “Selective Serotonin Reuptake Inhibitors (SSRIs)” commercially available as hydrochloride salt with around 44% oral bioavailability
The objective of the present study was to develop and characterize an optimal stable solid Self-nanoemulsifying drug delivery system (SNEDDS) of sertraline using minimum surfactant concentration, so that nano-sized droplets could be maintained on dilution by the gastrointestinal (GI) fluids with an aim to increase its oral bioavailability. (Propylene glycol monolaurate Type II; monoesters > 90%, C12 > 95%), Labrafil® M 2125 CS (Linoleoyl polyoxyl-6 glycerides; Oleic (C18:1) 24-34%, Linoleic (C18:2) 53-63%), MaisineTM 35-1 (Glyceryl monolinoleate; C18:2 >50%; C18:1 10-35%; C18:0
The solubility of sertraline was assessed in different oily phases alone and in combination, surfactant and cosurfactant (Figure 2)
Summary
Sertraline (SRT) free base (Figure 1) is lipophilic (log P, 5.1), poorly water-soluble drug (3.5 mg/L) belonging to the category “Selective Serotonin Reuptake Inhibitors (SSRIs)” commercially available as hydrochloride salt with around 44% oral bioavailability. Modification of the physicochemical properties such as salt formation of the compound is in practice as one of the approach to improve the dissolution rate of such drugs. In general, these methods have their own limitations. The salts that are formed may convert back to their original acid or base forms leading to aggregation in the gastrointestinal tract (GIT) leads to slow/poor absorption (Serajuddin, 1999). This may be the possible reason for poor oral bioavailability of sertraline hydrochloride. The salt formation needs extra expenditure of revenue in the form of processing cost
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