The present investigations highlight the development of solid self-emulsifying drug delivery system (solid-SEDDS) for improved oral delivery of the poorly water-soluble drug; cilnidipine. Liquid SEDDS of the drug were formulated using Capryol 90 as the oil phase, Tween 80 as the surfactant, and Transcutol HP as the co-surfactant after screening various vehicles. The prepared systems were characterized for selfemulsification time, robustness to dilution, % transmittance, globule size, drug release, and thermodynamic stability. Ternary phase diagrams were plotted to identify the area of microemulsification. The optimized liquid SEDDS was transformed into a free-flowing powder using Neusilin US2 as the adsorbent. Solid selfemulsifying powder retained the self-emulsifying property of the liquid SEDDS. Differential scanning calorimetric, X-ray powder diffraction studies revealed the possibility of transformation of the crystalline form of the drug to the amorphous form in the SEDDS prepared with the carrier. The morphology of solid-SEDDS from scanning electron microscopy studies demonstrated the presence of spherical, granular particles indicating good flowing ability. Dissolution studies revealed enhanced dissolution of the drug from the solid system compared with the pure drug and its marketed formulation. Similarly, the in vitro absorption profile of the drug from the formulated SEDDS was significantly higher compared with pure drug. Thus it can be concluded that solid-SEDDS, amenable for development of solid dosage form, can be successfully developed using Neusilin US2 with the potential of enhancing the solubility, dissolution rate, and bioavailability of the drug. Key words cilnidipine; solid self-emulsifying drug delivery system (SEDDS); adsorption; crystallinity; droplet size; drug release Poorly water-soluble drug candidates often emerge from contemporary drug discovery programs, and present formulators with considerable technical challenges. The absorption of such compounds when presented in the crystalline state to the gastrointestinal tract is typically dissolution rate-limited, and the drugs are typically Biopharmaceutical Classification System (BCS) class II or class IV compounds.1) The interests on lipid-based drug delivery systems (LBDDS) have increased over the past two decades as a function of identification of these pharmaceutically difficult candidates, and increased even further after successful launch of lipid-based oral pharmaceutical products, including in particular cyclosporine A, marketed as Sandimmune and Neoral .
2)Lipid based drug delivery system such as self-emulsifying drug delivery systems (SEDDS) are mixtures of oils and surfactants, ideally isotropic, sometimes including cosolvents, which emulsify under conditions of gentle agitation, similar to those which would be encountered in the gastrointestinal tract. Hydrophobic drugs can often be dissolved in SEDDS allowing them to be encapsulated as unit dosage forms for peroral administration.3-5) When such a system is released in the lum...