Self-Emulsifying Drug Delivery Systems (SEDDS): Formulation Development, Characterization, and Applications

Abstract

Self-emulsifying drug delivery systems (SEDDS) possess unparalleled potential in improving oral bioavailability of poorly water-soluble drugs. Following their oral administration, these systems rapidly disperse in gastrointestinal fluids, yielding micro- or nanoemulsions containing the solubilized drug. Owing to its miniscule globule size, the micro/nanoemulsifed drug can easily be absorbed through lymphatic pathways, bypassing the hepatic first-pass effect. We present an exhaustive and updated account of numerous literature reports and patents on diverse types of self-emulsifying drug formulations, with emphasis on their formulation, characterization, and systematic optimization strategies. Recent advancements in various methodologies employed to characterize their globule size and shape, ability to encapsulate the drug, gastrointestinal and thermodynamic stability, rheological characteristics, and so forth, are discussed comprehensively to guide the formula-tor in preparing an effective and robust SEDDS formulation. Also, this exhaustive review offers an explicit discussion on vital applications of the SEDDS in bioavailability enhancement of various drugs, outlining an overview on myriad in vitro, in situ, and ex vivo techniques to assess the absorption and/ or permeation potential of drugs incorporated in the SEDDS in animal and cell line models, and the subsequent absorption pathways followed by them. In short, the current article furnishes an updated compilation of wide-ranging information on all the requisite vistas of the self-emulsifying formulations, thus paving the way for accelerated progress into the SEDDS application in pharmaceutical research.

Self-nanoemulsifying drug delivery system (SNEDDS) of the poorly water-soluble grapefruit flavonoid Naringenin: design, characterization,in vitroandin vivoevaluation

“…SNEDDS are isotropic mixtures of natural or synthetic oils, solid or liquid surfactants or alternatively, one or more hydrophilic solvents and co-solvents/surfactants that have a unique ability of forming fine oil-in-water (o/w) emulsions on mild agitation followed by dilution in aqueous media, such as GI fluids (Singh et al, 2009). Self-nanoemulsifying properties of SNEDDS strongly depend upon the selected lipids, surfactants and their relative amounts.…”

“…Lipid-based drug delivery systems such as nanoemulsions and SNEDDS have a great potential to improve oral bioavailability of poor water soluble drugs by presenting the drug in a solubilized state in colloidal dispersion. SNEDDS are defined as isotropic mixtures of natural or synthetic oils, solid or liquid surfactants, or alternatively, one or more hydrophilic solvents and co-solvents/surfactants that have a unique ability of forming fine oil-in-water (o/w) emulsions upon mild agitation followed by dilution in aqueous media, such as gastrointestinal (GI) fluids (Singh et al, 2009). SNEDDS have been proved to improve the bioavailability of poorly soluble drugs like Talinolol (Ghai & Sinha, 2012), Coenzyme Q10 (Nepal, 2010), Zedoary turmeric oil (ZTO) (Zhao, 2010), biphenyl dimethyl dicarboxylate (BDD) (El-Laithy, 2008).…”

Enhancing biopharmaceutical attributes of phospholipid complex-loaded nanostructured lipidic carriers of mangiferin: Systematic development, characterization and evaluation

“…The validation data of the developed method has already been previously reported by our group . To estimate the pharmacokinetic parameters, data analysis was carried out using compartmental and noncompartmental modelling options of WinNonlin software, version 5.0 (M/s Thermo Scientific, USA) (Singh et al, 2009). …”

“…The in situ SPIP study is a well-known model to investigate the absorption and permeation behaviour of a drug when administered as complex (Singh et al, 2009). As is evident from Figure 14, the PLCs showed significant improvement (P < 0.001) in he absorption number (An) by 12-fold (P < 0.001), fraction of drug absorbed (F) by 11-fold (P <0.001), effective permeability (Peff) by 8-fold (P <0.001) and wall permeability (Pwall) by 12-fold (P <0.001) vis-à-vis free Mgf or co-administered with verapamil.…”

Lipid-based systems as a promising approach for enhancing the bioavailability of poorly water-soluble drugs

“…Spontaneous formation of emulsion advantageously presents the drug in a dissolved form, and the resultant small droplet size provides a large interfacial surface area. These characteristics result in faster drug release from the emulsion in a reproducible manner, which can be designed further to make the release characteristics independent of the gastrointestinal physiology and the fed/fasted state of the patient (19). The emulsion droplets formed are positively or negatively charged.…”