Zeta potential changing self-emulsifying drug delivery systems containing phosphorylated polysaccharides

Griesser, Janine; Burtscher, Stephanie; Köllner, S.; Nardin, Isabelle; Prüfert, Felix; Bernkop‐Schnürch, Andreas

doi:10.1016/j.ejpb.2017.06.025

Cited by 47 publications

(18 citation statements)

References 19 publications

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“…The in vitro studies showed a 12.3% release of the total phosphate, the ex vivo experiment (rat intestine) suggested a fast release of 23.1% [129]. Further work reported by Griesser showed that SEDDS, comprising phosphorylated polysaccharides (hydroxypropyl starch phosphate and maize starch phosphate), achieved higher mucus permeation as compared to control groups due to the net negative charge provided by the phosphate groups [130]. Subsequently, these phosphate groups were cleaved down by IAP at the intestinal epithelia which inverted the surface charge from negative to positive and thus could facilitate intestinal absorption in vivo.…”

Section: Zeta Potential Inverting Seddsmentioning

confidence: 89%

Self-emulsifying drug delivery system: Mucus permeation and innovative quantification technologies

Abdulkarim

Sharma

Gumbleton

2019

Advanced Drug Delivery Reviews

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Mucus is a dynamic barrier which covers and protects the underlying mucosal epithelial membrane against bacteria and foreign particles. This protection mechanism extends to include therapeutic macromolecules and nanoparticles (NPs) through trapping of these particles. Mucus is not only a physical barrier that limiting particles movements based on their sizes but it selectively binds with particles through both hydrophilic and lipophilic interactions. Therefore, nano-carriers for mucosal delivery should be designed to eliminate entrapment by the mucus barrier. For this reason, different strategies have been approached for both solid nano-carriers and liquid core nano-carriers to synthesise muco-diffusive nano-carrier. Among these nano-strategies, Self-Emulsifying Drug Delivery System (SEDDS) was recognised as very promising nano-carrier for mucus delivery. The system was introduced to enhance the dissolution and bioavailability of orally administered insoluble drugs. SEDDS has shown high stability against intestinal enzymatic activity and more importantly, relatively rapid permeation characteristics across mucus barrier. The high diffusivity of SEDDS has been tested using various in vitro measurement techniques including both bulk and individual measurement of droplets diffusion within mucus. The selection and processing of an optimum in vitro technique is of great importance to avoid misinterpretation of the diffusivity of SEDDS through mucus barrier. In conclusion, SEDDS is a system with high capacity to diffuse through intestinal mucus even though this system has not been studied to the same extent as solid nano-carriers.

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Section: Zeta Potential Inverting Seddsmentioning

confidence: 89%

Self-emulsifying drug delivery system: Mucus permeation and innovative quantification technologies

Abdulkarim

Sharma

Gumbleton

2019

Advanced Drug Delivery Reviews

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“…Currently, most of these drugs have to be applied parenterally due to a very limited bioavailability after oral administration. However, zeta potential changing drug delivery systems could be a solution and different approaches to this concept have been evaluated in recent publications (4)(5)(6)(7)(8)(9)(10).…”

Section: Discussionmentioning

confidence: 99%

“…However, the oral delivery of such medicines faces several challenges, such as the mucus gel layer covering the epithelial surface (1), enzymatic degradation (2), and minor cellular uptake (3). A promising approach to overcome these challenges are zeta potential changing drug delivery systemsa concept that has been evaluated in different recent publications (4)(5)(6)(7)(8)(9)(10). These nanocarriers are equipped with certain side chains that are substrate for membrane-bound intestinal enzymes.…”

Section: Introductionmentioning

confidence: 99%

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Development and In Vitro Evaluation of Stearic Acid Phosphotyrosine Amide as New Excipient for Zeta Potential Changing Self-Emulsifying Drug Delivery Systems

et al. 2020

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PURPOSEDevelopment of zeta potential changing SEDDS containing newly synthesized derivative stearic acid phosphotyrosine amide. METHODSStearoyl chloride was conjugated with phosphotyrosine, which is substrate for the brush border enzyme intestinal alkaline phosphate. The synthesized derivative was implemented in different SEDDS formulations and the zeta potential changing properties and the concluding mucus diffusion abilities were evaluated. RESULTSStearic acid phosphotyrosine amide was successfully synthesized and incorporated into SEDDS. A SEDDS formulation containing the new derivative showed a zeta potential of −14 mV before, and + 2 mV after enzymatic cleavage by intestinal alkaline phosphatase. Experiments on a Caco-2 monolayer demonstrated that the phosphate cannot only be cleaved by isolated enzyme, but also by enzyme, which was expressed by cells. The mucus diffusion abilities of the untreated, negatively charged SEDDS were significantly higher compared to the enzymatically cleaved, positively charged SEDDS. CONCLUSIONThe developed stearic acid phosphotyrosine represents a promising excipient for zeta potential changing SEDDS. KEYWORDSSEDDS . zeta potential changing drug delivery systems . phosphotyrosine . phosphatase ABBREVIATIONS DMSO Dimethyl sulfoxide FDA Fluorescein diacetate GIT Gastrointestinal tract HBS HEPES-buffered Saline IAP Intestinal alkaline phosphatase MEM Minimum essential medium PBS Phosphate-buffered saline PTyr Phosphotyrosine SA-PTyr Stearic acid phosphotyrosine amide SEDDS Self-emulsifying drug delivery system

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“…Mucoadhesive nanoparticles and mucus-penetrating nanoparticles have been designed to overcome the mucus barrier 26 . Microemulsions coated with a dense PEG shell significantly avoid the hindrance of mucus, and several mucus-penetrating microemulsions have been reported 27 , 28 , 29 . Moreover, some reports demonstrated that partially intact lipid-based nanoparticles diffuse through the mucus layer, including the intestinal epithelium 30 , 31 .…”

Section: Introductionmentioning

confidence: 99%

In situ monitoring of the structural change of microemulsions in simulated gastrointestinal conditions by SAXS and FRET

Zhang

et al. 2018

Acta Pharmaceutica Sinica B

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Microemulsions are promising drug delivery systems for the oral administration of poorly water-soluble drugs. However, the evolution of microemulsions in the gastrointestinal tract is still poorly characterized, especially the structural change of microemulsions under the effect of lipase and mucus. To better understand the fate of microemulsions in the gastrointestinal tract, we applied small-angle X-ray scattering (SAXS) and fluorescence resonance energy transfer (FRET) to monitor the structural change of microemulsions under the effect of lipolysis and mucus. First, the effect of lipolysis on microemulsions was studied by SAXS, which found the generation of liquid crystalline phases. Meanwhile, FRET spectra indicated micelles with smaller particle sizes were generated during lipolysis, which could be affected by CaCl2, bile salts and lecithin. Then, the effect of mucus on the structural change of lipolysed microemulsions was studied. The results of SAXS and FRET indicated that the liquid crystalline phases disappeared, and more micelles were generated. In summary, we studied the structural change of microemulsions in simulated gastrointestinal conditions by SAXS and FRET, and successfully monitored the appearance and disappearance of the liquid crystalline phases and micelles.

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Zeta potential changing self-emulsifying drug delivery systems containing phosphorylated polysaccharides

Cited by 47 publications

References 19 publications

Self-emulsifying drug delivery system: Mucus permeation and innovative quantification technologies

Self-emulsifying drug delivery system: Mucus permeation and innovative quantification technologies

Development and In Vitro Evaluation of Stearic Acid Phosphotyrosine Amide as New Excipient for Zeta Potential Changing Self-Emulsifying Drug Delivery Systems

In situ monitoring of the structural change of microemulsions in simulated gastrointestinal conditions by SAXS and FRET

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