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Bioavailability Amelioration of Zaleplon by developing self emulsifying drug delivery systems
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1  St. Peter's institute of pharmaceutical sciences
Academic Editor: Maria Emília Sousa (registering DOI)

The current study aims to create zaleplon-loaded self-emulsifying drug delivery systems (SEDDS) by varying the ratios of Phosal® 53 MCT, Tween 80, and Gelucire 44/14 as lipid, surfactant, and cosurfactant, respectively. The preparation of Phosal, Tween 80, and Gelucire 44/14 at 80%, 12%, and 8%, respectively, was found to be thermodynamically stable with a droplet size of 289 5 nm and charge of +13.9 1.5 mV. For the optimized formulation, dispersion properties such as particle size, viscosity, and pH of the SEDDS formulation were also measured. Diffusion studies revealed that the majority of the drug is encapsulated in the emulsion, resulting in the highest absorption capacity.

The improved in vitro dissolution behavior of zaleplon from SEDDS over control was observed, indicating its greater ability to retain zaleplon in a state of solubility. Ex vivo studies revealed a 3.65-fold increase in the level of permeation as SEDDS when compared to zaleplon alone in the pure state. SEDDS also increased bioavailability by 2.84-fold when tested in vivo against pure zaleplon suspension. The above SEDDS results show that SEDDS are capable of improving zaleplon oral bioavailability.

Keywords: Zaleplon, Phosal, Gelucire, Self emulsifying drug delivery systems, Bioavailability.