Development and In Vitro Evaluation of Stearic Acid Phosphotyrosine Amide as New Excipient for Zeta Potential Changing Self-Emulsifying Drug Delivery Systems
| العنوان: | Development and In Vitro Evaluation of Stearic Acid Phosphotyrosine Amide as New Excipient for Zeta Potential Changing Self-Emulsifying Drug Delivery Systems |
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| المؤلفون: | Franz Fischer, Sergey Zaichik, Andreas Bernkop-Schnürch, Christina Leichner, Felix Prüfert |
| المصدر: | Pharmaceutical Research |
| بيانات النشر: | Springer Science and Business Media LLC, 2020. |
| سنة النشر: | 2020 |
| مصطلحات موضوعية: | zeta potential changing drug delivery systems, Cell Survival, Surface Properties, Phosphatase, Pharmaceutical Science, Excipient, Conjugated system, phosphatase, Excipients, chemistry.chemical_compound, Drug Delivery Systems, Amide, Stearates, medicine, Zeta potential, Animals, Humans, Pharmacology (medical), Intestinal Mucosa, Pharmacology, Drug Carriers, Chromatography, Organic Chemistry, phosphotyrosine, Amides, chemistry, Emulsifying Agents, Drug delivery, SEDDS, Molecular Medicine, Alkaline phosphatase, Cattle, Emulsions, Stearic acid, Caco-2 Cells, Research Paper, Biotechnology, medicine.drug |
| الوصف: | Abstract Purpose Development of zeta potential changing SEDDS containing newly synthesized derivative stearic acid phosphotyrosine amide. Methods Stearoyl 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. Results Stearic 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. Conclusion The developed stearic acid phosphotyrosine represents a promising excipient for zeta potential changing SEDDS. |
| تدمد: | 1573-904X 0724-8741 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1378d3941cef76719384330b19f2b6b6 https://doi.org/10.1007/s11095-020-02802-2 |
| حقوق: | OPEN |
| رقم الأكسشن: | edsair.doi.dedup.....1378d3941cef76719384330b19f2b6b6 |
| قاعدة البيانات: | OpenAIRE |
Find this article in full text from Springer Verlag. | تدمد: | 1573904X 07248741 |
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