Nanopartículas sensibles a estímulos para el transporte eficaz de fármacos a órganos y tejidos diana
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Sáez-Fernández, E.; Martínez-Soler, G.I.; Pérez-Artacho, Beatriz; Ruiz Martínez, María A.; Arias Mediano, José LuisEditorial
Universidad de Granada, Facultad de Farmacia
Materia
Farmacoterapia Pharmacotherapy Hipertermia Hyperthermia Luz Light Magnetismo Magnetism Nanopartículas sensibles a estímulos Stimuli-sensitive nanoparticles pH Sistemas enzimáticos Enzymatic systems Transporte activo Active targeting Ultrasonidos Ultrasounds
Date
2010Referencia bibliográfica
Sáez-Fernández, E.; et al. Nanopartículas sensibles a estímulos para el transporte eficaz de fármacos a órganos y tejidos diana. Ars Pharm 2010; 51.Suplemento 3: 165-169. [http://hdl.handle.net/10481/26413]
Abstract
Las nanopartículas utilizadas en el transporte de fármacos pueden, en principio, alcanzar la masa
tumoral de forma “pasiva” (estrategias de transporte pasivo). Sin embargo, para asegurar un efecto
farmacológico óptimo debe controlarse el destino biológico del coloide transportador de fármacos. De
esta manera, cualquier sistema de este tipo debe ser capaz de responder a estímulos fisiológicos o
físicos, para así aumentar la acumulación del principio activo en el lugar de acción. Para ello, es
necesario un adecuado control de los factores biomecánicos que regulan la liberación de fármaco y el
mantenimiento de unas concentraciones plasmáticas dentro del margen terapéutico de la molécula
activa. Ante esto, se han desarrollado materiales sensibles a estímulos que aseguran una
biodistribución modificada del fármaco vehiculizado y, así, una farmacoterapia más eficiente.
Entre las estrategias de transporte activo basadas en coloides sensibles a estímulos destacan el
transporte activo de fármacos controlado por entornos (pHs) ácidos, hipertermia, gradientes
magnéticos, luz, sistemas enzimáticos y ultrasonidos. Se espera que su introducción en clínica permita
mejorar significativamente la actividad farmacológica de los principios activos. Si bien se han logrado
resultados preclínicos muy prometedores, el futuro de esta estrategia depende de un Nanoparticulate drug delivery systems can in principle passively target tumors. However, in order to
assure an optimal drug activity, it is needed the control of the biological fate of the colloid. Thus, drug
carriers should be capable of responding to physiological or physical stimuli, as well as able to
enhance the delivery of active agents to targeted tissues. This involves the need for an effective drug
transport into the site of action, an adequate control of the biochemical factors regulating drug release,
and the maintenance of drug levels under the minimum toxic concentration. Special approaches based
on stimuli-sensitive materials are expected to assure the modification of the biodistribution of loaded
drugs and, thus, resulting in a more efficient pharmacotherapy. The main objective of this work is to
analyze the most important approaches in the formulation of stimuli-sensitive materials for active drug
targeting to the specific site of action.
Stimuli-sensitive drug carriers can alter their physical properties (swelling/deswelling,
disruption/aggregation, etc.) under exposure to a stimulus. This property is widely used to trigger drug
release at the targeted site, but can also be utilized to accumulate the drug at the non-healthy tissue or
cell before allowing its release (e.g., magnetically responsive carriers). In both cases, the systemic
distribution of the drug is minimized (and, subsequently, the undesired side effects), meanwhile its
therapeutic activity is enhanced. Very promising active targeting strategies involving the use of
stimuli-sensitive carriers include acid-triggered drug release, hyperthermia-induced drug delivery,magnetic drug targeting, light-triggered drug release, enzyme-triggered drug release, and ultrasoundmediated
delivery. The introduction of the wide variety of stimuli-sensitive strategies in clinic is
expected to significantly enhance the pharmacotherapy. Even though the very promising preclinical
results, the future of the strategy will depend on a better understanding of the stability,
physicochemistry, toxicity, and biological fate of such kind of colloids.