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1.
J Drug Target ; 28(3): 259-270, 2020 03.
Artículo en Inglés | MEDLINE | ID: mdl-31491352

RESUMEN

Nanocrystals and lipid-based nanosystems have the potential to play a crucial role in a significant shift in the treatment of ophthalmic diseases. These drug delivery systems allow overcoming the barriers imposed by anatomy and physiology of the organ of vision. This review aims to present new perspectives for these innovative preparations, emphasising the applications of the nanocrystal and lipid-based nanosystem while outlining their advantages and the drawbacks. The in vivo performance of the lipid-based nanosystems was highlighted. Lipid-based nanosystems and nanocrystals showed a prolonged effect, improved ocular bioavailability, upper therapeutic efficacy, higher permeation, prolonged residence time, and sustained drug release, compared to the current applications. Well-established and innovative developments updates of these systems are highlighted herein.


Asunto(s)
Sistemas de Liberación de Medicamentos , Oftalmopatías/tratamiento farmacológico , Nanopartículas , Administración Oftálmica , Animales , Disponibilidad Biológica , Preparaciones de Acción Retardada , Humanos , Lípidos/química
2.
Eur J Med Chem ; 162: 378-395, 2019 Jan 15.
Artículo en Inglés | MEDLINE | ID: mdl-30453246

RESUMEN

Thiazole, thiosemicarbazone and semicarbazone moieties are privileged scaffolds (acting as primary pharmacophores) in many compounds that are useful to treat several diseases, mainly tropical infectious diseases. In this review article, we critically analyzed the contribution of these scaffolds to medicinal chemistry in the last five years, focusing on tropical infectious diseases, such as Chagas disease, human African trypanosomiasis (HAT), leishmaniasis, and malaria. We also present perspectives for their use in drug design in order to contribute to the development of new drugs.


Asunto(s)
Infecciones por Protozoos/tratamiento farmacológico , Semicarbazonas/uso terapéutico , Tiazoles/uso terapéutico , Tiosemicarbazonas/uso terapéutico , Animales , Enfermedad de Chagas/tratamiento farmacológico , Diseño de Fármacos , Humanos , Leishmaniasis/tratamiento farmacológico , Malaria/tratamiento farmacológico , Tripanosomiasis Africana/tratamiento farmacológico
3.
Curr Med Chem ; 21(23): 2599-609, 2014.
Artículo en Inglés | MEDLINE | ID: mdl-24533804

RESUMEN

The treatment of central nervous system (CNS) diseases is a major challenge. The presence of the barrier intended to protect the brain from unwanted molecules also impairs the efficacy of CNS-targeted drugs. The discovery of drug targets for CNS diseases opens a door for the selective treatment of these diseases. However, the physicochemical properties of drugs, including their hydrophilic properties and their peripheral metabolism, as well as the blood-brain barrier, can adversely affect the therapeutic potential of CNS-targeted drugs. Although peptides are often metabolized by enzymes, they are of particular interest for the treatment of CNS diseases or as carriers to deliver drugs to the brain. In this review, we discuss the use of peptides as potential prodrugs for the treatment of CNS diseases.


Asunto(s)
Péptidos/uso terapéutico , Profármacos/uso terapéutico , Animales , Barrera Hematoencefálica/metabolismo , Enfermedades del Sistema Nervioso Central/tratamiento farmacológico , Fenómenos Químicos , Humanos , Péptidos/química , Péptidos/metabolismo , Profármacos/química , Profármacos/metabolismo
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