N-Hydroxysulfosuccinimide Esters versus Thiomers: A Comparative Study Regarding Mucoadhesiveness
| العنوان: | N-Hydroxysulfosuccinimide Esters versus Thiomers: A Comparative Study Regarding Mucoadhesiveness |
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| المؤلفون: | Andreas Bernkop-Schnürch, Christina Leichner, Randi Angela Baus, Ronald Gust, Sina Katharina Götzfried, Claudia Menzel, Patrizia Wulz |
| المصدر: | Molecular Pharmaceutics. 16:1211-1219 |
| بيانات النشر: | American Chemical Society (ACS), 2019. |
| سنة النشر: | 2019 |
| مصطلحات موضوعية: | Cell Survival, Swine, Acrylic Resins, Succinimides, Pharmaceutical Science, 02 engineering and technology, Hemolysis, 030226 pharmacology & pharmacy, 03 medical and health sciences, chemistry.chemical_compound, Drug Delivery Systems, 0302 clinical medicine, Drug Stability, Intestinal mucosa, Tensile Strength, Drug Discovery, Mucoadhesion, Animals, Humans, Cysteine, Intestinal Mucosa, Fourier transform infrared spectroscopy, Acrylic acid, chemistry.chemical_classification, Viscosity, Thiomer, Hydrolysis, Polyacrylic acid, Adhesiveness, Drug Synergism, Esters, Adhesion, Polymer, biochemical phenomena, metabolism, and nutrition, 021001 nanoscience & nanotechnology, Mucus, chemistry, Chemical engineering, Molecular Medicine, Caco-2 Cells, 0210 nano-technology |
| الوصف: | The objective of the study was to compare poly(acrylic acid)- N-hydroxysulfosuccinimide reactive esters (PAA-Sulfo-NHS) and poly(acrylic acid)-cysteine conjugates (PAA-Cys) regarding their mucoadhesiveness. Polymer conjugates were synthesized in a water free environment and characterized by UV-vis spectroscopy and FTIR. Water uptake studies were performed, and the polymers were further examined for their mucoadhesive properties and cohesiveness using the rotating cylinder method. Tensile force measurements were conducted to define the strength of adhesion to porcine intestinal mucosa. Additionally, polymer-mucus mixtures were assessed for rheological synergism by measuring the increase in dynamic viscosity. Both modifications led to a prolonged adhesion time compared to unmodified PAA. Fast dissolution of PAA-Sulfo-NHS derivatives was monitored, whereas PAA-Cys tended to extensively swell while exhibiting high cohesive properties. Measurements of tensile force revealed up to 2.7-fold (PAA-Sulfo-NHS) and 2.3-fold (PAA-Cys) enhancement of the maximum detachment force and 7.6-fold (PAA-Sulfo-NHS) and 3.6-fold (PAA-Cys) increase in the total work of adhesion. Formation of a gel network between polymer and mucus was confirmed by a 10.8-fold (PAA-Sulfo-NHS) and 20.8-fold (PAA-Cys) increase in viscosity. Both types of polymers show high mucoadhesive properties due to the formation of covalent bonds with the mucus. As thiolated polymers are capable of forming stabilizing disulfide bonds within their polymeric network, they are advantageous over PAA-Sulfo-NHS. |
| تدمد: | 1543-8392 1543-8384 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8970def60f3b4176cd5d6301dde8d4bd https://doi.org/10.1021/acs.molpharmaceut.8b01183 |
| حقوق: | CLOSED |
| رقم الأكسشن: | edsair.doi.dedup.....8970def60f3b4176cd5d6301dde8d4bd |
| قاعدة البيانات: | OpenAIRE |
Find this issue from the American Chemical Society | تدمد: | 15438392 15438384 |
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