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Fármacos anfifílicos: auto-agregação e interação com membranas e tensioativos. Aspetos físico-químicos e biológicos
| Name: | Description: | Size: | Format: | |
|---|---|---|---|---|
| PPG_21593 | 1.71 MB | Adobe PDF |
Advisor(s)
Abstract(s)
Muitos fármacos possuem uma natureza anfifílica/anfipática pois possuem dois grupos com solubilidade diametralmente opostas. São vários os fármacos anfifílicos que possuem a capacidade de se auto-agregar e de formar micelas. Os fármacos anfifílicos, tal como os tensioativos clássicos, possuem ação superficial porque interagem com as membranas causando a sua interrupção e originando lise celular.
A literatura sobre fármacos anfifílicos com atividade à superfície da membrana celular é muito extensa e inclui fármacos analgésicos, antibióticos, antibióticos poliénicos, anestésicos, anestésicos locais, antidepressivos, antimicrobianos, anti-histamínicos, anticolinérgicos, anti-hipertensivos, tranquilizantes, inibidores da bomba de protões, antipsicóticos - fenotiazinas, ansiolíticos e hipnóticos, esteroides, prostaglandinas e vitaminas.
A utilização de micelas mistas e poliméricas podem ajudar a superar problemas relacionados com a toxicidade ou absorção em relação às micelas simples. A modulação das propriedades físico-químicas dos fármacos por auto-agregação e associação membranar é discutido ao longo deste trabalho.
Os mecanismos de solubilização de fármacos por tensioativos são analisados de um ponto de vista físico-químico e em relação ao transporte e absorção de fármacos pelo organismo.
Many drugs have an amphiphilic/amphipathic nature because they have two groups with diametrically opposed solubility. Several amphiphilic drugs that have the ability to self-aggregate and to form micelles. The amphiphilic drugs such as classical surfactants possess surface activity because they interact with the membranes causing their disruption and cell lysis. The literature on amphiphilic agents with activity at the cell membrane surface is extensive and includes analgesics, antibiotics, polyene antibiotics, anesthetics, local anesthetics, antidepressants, antihistamines, antihypertensives, anticholinergics, tranquilizers, proton pump inhibitors, antipsychotics - phenothiazines, anxiolytics and hypnotics, steroids, prostaglandins and vitamins. The use of mixed polymeric micelles and may help to overcome problems related to toxicity, or uptake relative simple micelles. The modulation of the physicochemical properties of drugs by self-association and membrane association is discussed throughout this work. Drug mechanisms solubilization by surfactants are analyzed the physical-chemical point of view and in relation to transport drugs and absorption by the organism.
Many drugs have an amphiphilic/amphipathic nature because they have two groups with diametrically opposed solubility. Several amphiphilic drugs that have the ability to self-aggregate and to form micelles. The amphiphilic drugs such as classical surfactants possess surface activity because they interact with the membranes causing their disruption and cell lysis. The literature on amphiphilic agents with activity at the cell membrane surface is extensive and includes analgesics, antibiotics, polyene antibiotics, anesthetics, local anesthetics, antidepressants, antihistamines, antihypertensives, anticholinergics, tranquilizers, proton pump inhibitors, antipsychotics - phenothiazines, anxiolytics and hypnotics, steroids, prostaglandins and vitamins. The use of mixed polymeric micelles and may help to overcome problems related to toxicity, or uptake relative simple micelles. The modulation of the physicochemical properties of drugs by self-association and membrane association is discussed throughout this work. Drug mechanisms solubilization by surfactants are analyzed the physical-chemical point of view and in relation to transport drugs and absorption by the organism.
Description
Keywords
Fármacos anfifílicos Auto-agregação Micela Agentes tensioativos Atividade superficial Amphiphilic drugs Self-aggregation Micellles Surfactants Surface activity