Systematic Development of Self-Emulsifying Drug Delivery Systems of Atorvastatin with Improved Bioavailability Potential

Abstract

The aim of this study was to prepare and characterize a self-emulsifying drug delivery system (SEDDS) with a high drug load of poorly water-soluble atorvastatin for the enhancement of dissolution and oral bioavailability. Solubility of atorvastatin in oil, surfactant, and cosurfactant was determined. Pseudo-ternary phase diagrams were constructed by the aqueous titration method, and formulations were developed based on the optimum excipient combinations. A high drug load (10% w/w) was achieved with a combination of oleic acid, Tween 80, and polyethylene glycol 400, ensuring the maximum dissolution property (in the case of SES6). Effects of lipids and surfactants on physical properties of SEDDS such as in vitro emulsification efficiency in terms of self-emulsification time, emulsion droplet size, and percent transmittance were measured. Multiple regression analysis revealed that a higher amount of surfactants significantly increased dissolution of ATV while decreasing emulsion droplet size and emulsification time. About a four-fold increase in dissolution was achieved by SEDDS compared to pure ATV powder. Overall, this study suggests that dissolution and oral bioavailability of ATV could be improved by SEDDS technology.

Experimental design approach for development of novel microemulsion system and immediate release self microemulsifying tablet of nebivolol HCl

“…Hence, surfactant: co-surfactant ratio (1:2) was selected for the formulation. Moreover similar phase diagram was obtained when constructed in the presence of NEB ( Figure 4F) (Khan et al, 2012).…”

“…Slight agitation was supplied by dissolution paddle rotating at 50 rpm. Time required for emulsification time was observed visually (Khan et al, 2012). Further the sample was subjected to percent transmittance analysis using double beam UV-Visible spectrophotometer using distilled water as blank at wavelength of 650 nm (Rao et al, 2013).…”

Development and Evaluation of Liquid and Solid Self-Emulsifying Drug Delivery Systems for Atorvastatin

“…When subjected to aqueous dilution under mild agitation, SEDDS should completely and rapidly disperse. Surfactants present in the SEDDS reduce the interfacial tension between oil and aqueous phases and facilitate dispersion and formation of oil-in-water emulsion [26]. The results of the emulsification study are presented in Table 3.…”

“…Low oral bioavailability of ATR (only 12% after a 40 mg oral dose) is associated with its poor solubility in water and high (above 80%) presystemic clearance [23,24,25]. Therefore, using different lipid carriers of ATR has been widely reported as a promising drug delivery system [26,27,28,29,30]. As to our best knowledge there are no papers concerning solid SEDDS for ATR, the aim of this work was to design and to obtain both liquid and solid SEDDS from the same, optimized composition for solubility enhancement of ATR.…”

Self-emulsifying drug delivery systems as a tool to improve solubility and bioavailability of resveratrol

“…Additionally, cosurfactant would augment the reduction to the interfacial tension and also influence interfacial film curvature and hence spontaneity of emulsification process. 34 , 35 The investigated SEDDS formulations resulted in the formation of stable microemulsions upon dilution and hence they were selected for further investigation.…”