Physico-chemical characterization of self-emulsifying drug delivery systems

Ujhelyi, Zoltán; Vecsernyés, Miklós; Fehér, Pálma; Kósa, Dóra; Arany, Petra; Nemes, Dániel; Sinka, Dávid; Vasvári, Gábor; Fenyvesi, Ferenc; Váradi, Judit; Bácskay, Ildikó

doi:10.1016/j.ddtec.2018.06.005

Cited by 36 publications

(21 citation statements)

References 41 publications

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“…It is suggested by literature that spontaneous emulsification is facilitated by a system that favours dispersion formation instead of increasing the surface area of the dispersion upon exposure to a change in entropy. Thus, the free energy present between SEDDS components is directly related to the energy required by the system to generate a new surface between the two immiscible phases [5,30]. This relationship between the free energy required to establish a self-emulsifying system and the energy at work at the interface is described by the following equation:…”

Section: Mechanism Of Spontaneous Emulsificationmentioning

confidence: 99%

“…Self-emulsifying drug delivery systems (SEDDSs) are isotropic blends of an active compound with a mixture of lipids, surfactants, and co-surfactants that produce spontaneous oil-in-water emulsions (dispersions) during moderate agitation in an aqueous phase, such as the upper gastrointestinal tract. A highly solubilised, thermodynamically stable phase of drug for improved drug absorption is subsequently formed [3][4][5][6][7][8]. SEDDS, however, is a comprehensive term for selected lipid-based drug delivery systems and can rather be differentiated into three categories in terms of droplet size.…”

Section: Introductionmentioning

confidence: 99%

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Development of Topical/Transdermal Self-Emulsifying Drug Delivery Systems, Not as Simple as Expected

2020

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Self-emulsifying drug delivery systems (SEDDSs) originated as an oral lipid-based drug delivery system with the sole purpose of improving delivery of highly lipophilic drugs. However, the revolutionary drug delivery possibilities presented by these uniquely simplified systems in terms of muco-adhesiveness and zeta-potential changing capacity lead the way forward to ground-breaking research. Contrarily, SEDDSs destined for topical/transdermal drug delivery have received limited attention. Therefore, this review is focused at utilising principles, established during development of oral SEDDSs, and tailoring them to fit evaluation strategies for an optimised topical/transdermal drug delivery vehicle. This includes a detailed discussion of how the authentic pseudo-ternary phase diagram is employed to predict phase behaviour to find the self-emulsification region most suitable for formulating topical/transdermal SEDDSs. Additionally, special attention is given to the manner of characterising oral SEDDSs compared to topical/transdermal SEDDSs, since absorption within the gastrointestinal tract and the multi-layered nature of the skin are two completely diverse drug delivery territories. Despite the advantages of the topical/transdermal drug administration route, certain challenges such as the relatively undiscovered field of skin metabolomics as well as the obstacles of choosing excipients wisely to establish skin penetration enhancement might prevail. Therefore, development of topical/transdermal SEDDSs might be more complicated than expected.

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Section: Mechanism Of Spontaneous Emulsificationmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Development of Topical/Transdermal Self-Emulsifying Drug Delivery Systems, Not as Simple as Expected

2020

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“…The free energy of emulsion formation is a direct function of the energy required to create a new surface between the two phases [149,150]. This self-emulsification process is defined by the equation below [151]:…”

Section: Self-emulsification Propertiesmentioning

confidence: 99%

“…Conductivity measurements determine the point of aqueous phase addition at which the system changes from having an oil-continuous to a water-continuous phase. They can be applied to monitor the percolation and phase-inversion of emulsion [151,154]. There are various types of viscometers which can evaluate the rheological properties of a microemulsion.…”

Section: Conductivity and Viscosity Measurementsmentioning

confidence: 99%

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Current Status of Supersaturable Self-Emulsifying Drug Delivery Systems

Park

Kim

2020

Pharmaceutics

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Self-emulsifying drug delivery systems (SEDDSs) are a vital strategy to enhance the bioavailability (BA) of formulations of poorly water-soluble compounds. However, these formulations have certain limitations, including in vivo drug precipitation, poor in vitro in vivo correlation due to a lack of predictive in vitro tests, issues in handling of liquid formulation, and physico-chemical instability of drug and/or vehicle components. To overcome these limitations, which restrict the potential usage of such systems, the supersaturable SEDDSs (su-SEDDSs) have gained attention based on the fact that the inclusion of precipitation inhibitors (PIs) within SEDDSs helps maintain drug supersaturation after dispersion and digestion in the gastrointestinal tract. This improves the BA of drugs and reduces the variability of exposure. In addition, the formulation of solid su-SEDDSs has helped to overcome disadvantages of liquid or capsule dosage form. This review article discusses, in detail, the current status of su-SEDDSs that overcome the limitations of conventional SEDDSs. It discusses the definition and range of su-SEDDSs, the principle mechanisms underlying precipitation inhibition and enhanced in vivo absorption, drug application cases, biorelevance in vitro digestion models, and the development of liquid su-SEDDSs to solid dosage forms. This review also describes the effects of various physiological factors and the potential interactions between PIs and lipid, lipase or lipid digested products on the in vivo performance of su-SEDDSs. In particular, several considerations relating to the properties of PIs are discussed from various perspectives.Pharmaceutics 2020, 12, 365 2 of 57 intraluminal supersaturation and the biorelevance of supersaturation assays will be addressed. Finally, we will make suggestions for the successful development of su-SEDDs.There are many review articles that give useful information about the nature and application of supersaturable drug delivery systems or conventional SEDDSs. However, these reviews cover only a limited range of su-SEDDSs. Therefore, this review, which includes the current status of technology focused only on su-SEDDSs, is a valuable addition to the previous review literature because no review article currently covers such a wide range of su-SEDDSs. Conventional Solubilized SEDDSsThere has been a steady increase in the number of new drug candidates (almost 40%) that are highly hydrophobic and poorly water-soluble. The oral bioavailability of poorly water-soluble drugs is hindered by low solubility and slow dissolution in the aqueous environment of the GIT. Thus, it is a great challenge for pharmaceutical scientists to overcome the inherent slow dissolution and poor oral absorption of hydrophobic drugs [1][2][3][4]. SEDDSs have emerged as a promising approach to improving the biopharmaceutical performance of hydrophobic drugs by enhancing their bioavailability [5,6].An SEDDS is a pre-concentrate composed of a drug, oils, surfactants, and sometimes co-solvents and/or co-surfactan...

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Baicalein self‐microemulsion based on drug–phospholipid complex for the alleviation of cytokine storm

Liao

Gao

et al. 2022

Bioengineering & Transla Med

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Cytokine storm is a phenomenon whereby the overreaction of the human immune system leads to the release of inflammatory cytokines, which can lead to multiple organ dysfunction syndrome. At present, the existing drugs for the treatment of cytokine storm have limited efficacy and severe adverse effects. Here, we report a lymphatic targeting self‐microemulsifying drug delivery system containing baicalein to effectively inhibit cytokine storm. Baicalein self‐microemulsion with phospholipid complex as an intermediate carrier (BAPC‐SME) prepared in this study could be spontaneously emulsified to form 12‐nm oil‐in‐water nanoemulsion after administration. And then BAPC‐SME underwent uptake by enterocyte through endocytosis mediated by lipid valve and clathrin, and had obvious characteristics of mesenteric lymph node targeting distribution. Oral administration of BAPC‐SME could significantly inhibit the increase in plasma levels of 14 cytokines: TNF‐α, IL‐6, IFN‐γ, MCP‐1, IL‐17A, IL‐27, IL‐1α, GM‐CSF, MIG, IFN‐β, IL‐12, MIP‐3α, IL‐23, and RANTES in mice experiencing systemic cytokine storm. BAPC‐SME could also significantly improve the pathological injury and inflammatory cell infiltration of lung tissue in mice experiencing local cytokine storm. This study does not only provide a new lymphatic targeted drug delivery strategy for the treatment of cytokine storm but also has great practical significance for the clinical development of baicalein self‐microemulsion therapies for cytokine storm.

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Physico-chemical characterization of self-emulsifying drug delivery systems

Cited by 36 publications

References 41 publications

Development of Topical/Transdermal Self-Emulsifying Drug Delivery Systems, Not as Simple as Expected

Development of Topical/Transdermal Self-Emulsifying Drug Delivery Systems, Not as Simple as Expected

Current Status of Supersaturable Self-Emulsifying Drug Delivery Systems

Baicalein self‐microemulsion based on drug–phospholipid complex for the alleviation of cytokine storm

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