Estudio de la interacción de triptanos con membranas lipídicas y su encapsulación en micelas poliméricas mediante simulaciones de dinámica molecular
Triptans are anti-migraine drugs designed based on serotonin (5-HT). They act as selective 5-HT1 receptor agonists, however they do not cross the blood brain barrier (BBB) to reach central receptors. Although the prototype sumatriptan is still the most used triptan and it is available in different f...
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| Formato: | Tesis doctoral acceptedVersion |
| Lenguaje: | Español |
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Facultad de Farmacia y Bioquímica
2016
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| Acceso en línea: | http://repositoriouba.sisbi.uba.ar/gsdl/cgi-bin/library.cgi?a=d&c=posgraafa&cl=CL1&d=HWA_1399 http://repositoriouba.sisbi.uba.ar/gsdl/collect/posgraafa/index/assoc/HWA_1399.dir/1399.PDF |
| Aporte de: |
| Sumario: | Triptans are anti-migraine drugs designed based on serotonin (5-HT). They act as selective 5-HT1 receptor agonists, however they do not cross the blood brain barrier (BBB) to reach central receptors. Although the prototype sumatriptan is still the most used triptan and it is available in different forms, could be needed to optimize its effectiveness and safety. Taking into account the suitability of poloxamers as drug delivery nanomaterials, an improvement on sumatriptan pharmacokinetics, potentially membrane permeation and prolonged release could be expected by encapsulation.\nWe performed computer simulations to understand the behavior of triptans in model membranes. The interphase played a key role in the anchoring of indolic compounds: choline and phosphate groups favor the interphacial distribution through several interactions. These results were experimentally confirmed. The observed behavior indicates that these compounds do not easily diffuse through lipid membranes, as BBB, thus another transport mechanism could be need.\nWe also studied the poloxamers aggregation in water and sumatriptan encapsulation in polymeric micelles (they were suitable). The studied poloxamers have interacted with phosphatidylcholine depending on environment and hydrophilic-lipophilic balance. Further studies will be needed to consider different conditions to understand permeation mechanisms favored by these poloxamers. |
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