Solidification to improve the biopharmaceutical performance of SEDDS: Opportunities and challenges

Joyce, Paul; Dening, Tahnee J.; Meola, Tahlia R.; Schultz, Hayley B.; Holm, René; Prestidge, Clive A.

doi:10.1016/j.addr.2018.11.006

Cited by 88 publications

(67 citation statements)

References 200 publications

(242 reference statements)

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“…The low drug-loading capacity of conventional solubilized SEDDSs is considered a main disadvantage for high-dose BCS class II and IV drugs. However, using su-SEDDS formulation strategies can contribute to increased drug loading through the stabilization of supersaturation in the formulation and/or in the GIT [30,33].…”

Section: Definition Of Su-seddssmentioning

confidence: 99%

“…In su-SEDDSs, drug molecules are either (i) encapsulated within the lipid phase at a concentration above their equilibrium solubility or (ii) formulated with excipients that generate supersaturated drug solutions when dispersed and lipolyzed in the GIT. In either case, they can only be classified as su-SEDDSs if a PI is included in the formulation [30]. The su-SEDDS differ from supersaturated SEDDS, as the latter is not thermodynamically stable and drugs in supersaturated formulations can crystallize during storage or after oral administration.…”

Section: Confusion Between Supersaturated Seddss and Su-seddssmentioning

confidence: 99%

“…Then, for su-SEDDSs, a PI is added to the pre-concentrate formulation. Finally, the liquid state su-SEDDS should be converted to a suitable dosage form [30,34].…”

Section: Selection and Application Of Pis For The Successful Developmmentioning

confidence: 99%

“…In addition, there are cases in which interactions between drugs and excipients have unwelcome effects, and the excipients themselves can affect physiological conditions, hence, modulating the fate of the drug in vivo [129]. There was a report about specific interactions between solidification excipient and lipid molecules in both SEDDS formulation and in vivo [30,130,131]. Similar to that, the interactions between a PI and a drug or lipid could influence the performance of SEDDS, including dispersion, lipid digestion, and drug supersaturation, dissolution, and absorption in the GIT.…”

Section: Potential Effect Of Pi On Stability In Vivo Emulsificationmentioning

confidence: 99%

“…Subsequently, conventional solubilized SEDDSs essentially contain high concentrations of surfactants (typically 30% w/w) [7,29]. These high doses of surfactants can lead to GI side effects that can be poorly tolerated during chronic use [5,30].…”

mentioning

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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Section: Definition Of Su-seddssmentioning

confidence: 99%

Section: Confusion Between Supersaturated Seddss and Su-seddssmentioning

confidence: 99%

“…Then, for su-SEDDSs, a PI is added to the pre-concentrate formulation. Finally, the liquid state su-SEDDS should be converted to a suitable dosage form [30,34].…”

Section: Selection and Application Of Pis For The Successful Developmmentioning

confidence: 99%

Section: Potential Effect Of Pi On Stability In Vivo Emulsificationmentioning

confidence: 99%

mentioning

confidence: 99%

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Current Status of Supersaturable Self-Emulsifying Drug Delivery Systems

Park

Kim

2020

Pharmaceutics

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Lipid‐based Formulations

O’Shea¹,

O’Driscoll²,

Griffin³

2022

Oral Drug Delivery for Modified Release Formulations

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Oral Multidrug Co‐Delivery System Targeting Differential Sites for Diabetes Mellitus Treatment

Zhang,

Wang,

et al. 2023

Adv Funct Materials

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Although regulation of the blood glucose level is a common therapy for Type 2 diabetes mellitus (T2DM), the root cause of this disease (such as the damage of pancreatic β cells) cannot be solved. Remodeling the pancreatic microenvironment and gut microbial homeostasis to improve β cells dysfunction become a potential strategy but remains challenging. Herein, a curcumin (CUR) and bifidobacterial (BI) co‐delivery system based on the self‐emulsifying technology (CUR‐BI‐SEDDS), which can generate a protective and self‐assembled coating on BI surface to achieve the above strategy is designed. CUR‐loaded oil phase coating endows BI with resistance against gastric invasion and helps BI colonize to positively regulate the abundance of gut microbiota. Following oral ingestion, the CUR‐loaded oil phase is self‐emulsified into nano‐emulsion, separated from BI, and delivers CUR to pancreas via the chylomicron pathway to remodel the inflammatory pancreatic microenvironment. As a result, CUR‐BI‐SEDDS showed excellent efficacy in restoring the islet β cell function, thus maintaining the systemic glucose homeostasis via only once administration every day. This study not only provides a promising regimen for thorough T2DM therapy but also explores a versatile oral co‐delivery platform for combination of chemo‐drugs and living biotherapeutics, which can exert potency at diverse target sites.

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Solidification to improve the biopharmaceutical performance of SEDDS: Opportunities and challenges

Cited by 88 publications

References 200 publications

Current Status of Supersaturable Self-Emulsifying Drug Delivery Systems

Current Status of Supersaturable Self-Emulsifying Drug Delivery Systems

Lipid‐based Formulations

Oral Multidrug Co‐Delivery System Targeting Differential Sites for Diabetes Mellitus Treatment

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