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1.
Soft Matter ; 12(7): 2166-76, 2016 Feb 21.
Artículo en Inglés | MEDLINE | ID: mdl-26754164

RESUMEN

The ability to self-assemble was evaluated for a large variety of amphiphilic block copolymers, including poly(ethyleneoxide-b-ε-caprolactone), poly(ethyleneoxide-b-d,l-lactide), poly(ethyleneoxide-b-styrene), poly(ethyleneoxide-b-butadiene) and poly(ethyleneoxide-b-methylmethacrylate). Different methods of formation are discussed, such as cosolvent addition, film hydration or electroformation. The influence of experimental parameters and macromolecular structures on the size and morphology of the final self-assembled structures is investigated and critically compared with the literature. The same process is carried out regarding the characterization of these structures. This analysis demonstrates the great care that should be taken when dealing with such polymeric assemblies. If the morphology of such assemblies can be predicted to some extent by macromolecular parameters like the hydrophilic/hydrophobic balance, those parameters cannot be considered as universal. In addition, external experimental parameters (methods of preparation, use of co-solvent, …) appeared as critical key parameters to obtain a good control over the final structure of such objects, which are very often not at thermodynamic equilibrium but kinetically frozen. A principal component analysis is also proposed, in order to examine the important parameters for forming the self-assemblies. Here again, the hydrophilic/hydrophobic fraction is identified as an important parameter.


Asunto(s)
Lactonas/química , Metacrilatos/química , Poliésteres/química , Polietilenglicoles/química , Poliestirenos/química , Interacciones Hidrofóbicas e Hidrofílicas , Cinética , Micelas , Estructura Molecular , Tamaño de la Partícula , Análisis de Componente Principal , Solubilidad , Propiedades de Superficie , Termodinámica
2.
Curr Med Chem ; 22(26): 3014-24, 2015.
Artículo en Inglés | MEDLINE | ID: mdl-26242256

RESUMEN

Nowadays, nanomedicine brings new opportunities for diagnosis and treatment through innovative combinations of materials structured at the nanoscale, biomolecules and physicochemical processes. If the intrinsic properties of nanomaterials appear of major importance in this new discipline, the functionalization of these nanotools with biomolecules improves both their biocompatibility and efficacy. This is the case of carbohydrate derivatives, natural or synthetic, which are increasingly being used in nanostructures for medical purposes. As in current medicine, sugars are used to mimic their physiological roles. Indeed, carbohydrates enhance the solubility and reduce the clearance of drugs. They are used to mask immunogenic components of nano-objects and escape the body defenses and finally facilitate the delivery to the target tissue. All these properties explain the growing importance of sugars in nanomedicine.


Asunto(s)
Antineoplásicos , Carbohidratos , Portadores de Fármacos , Nanomedicina/métodos , Animales , Antineoplásicos/química , Carbohidratos/química , Portadores de Fármacos/química , Humanos
3.
Curr Med Chem ; 20(15): 1946-55, 2013.
Artículo en Inglés | MEDLINE | ID: mdl-23409718

RESUMEN

In this mini-review, we focus on different strategies to bring nanotools specifically to cancer cells. We discuss about a better targeting of tumor, combining the characteristics of tumor environment, the increase in nanoparticles life time, the biomarkers overexpressed on cancer cells and different physical methods for non invasive therapies. Here we detail the necessity of a synergy between passive and active targeting for an actual specificity of cancer cells.


Asunto(s)
Antineoplásicos/administración & dosificación , Sistemas de Liberación de Medicamentos/métodos , Nanopartículas/análisis , Neoplasias/tratamiento farmacológico , Animales , Humanos , Neoplasias/irrigación sanguínea , Neoplasias/metabolismo , Oxígeno/metabolismo , Microambiente Tumoral
4.
Curr Med Chem ; 14(28): 2945-53, 2007.
Artículo en Inglés | MEDLINE | ID: mdl-18220730

RESUMEN

The cation-independent mannose 6-phosphate receptor is a multifunctional protein which binds at the cell surface to two distinct classes of ligands, the mannose 6-phosphate (M6P) bearing proteins and IGF-II. Its major function is to bind and transport M6P-enzymes to lysosomes, but it can also modulate the activity of a variety of extracellular M6P-glycoproteins (i.e., latent TGFbeta precursor, urokinase-type plasminogen activator receptor, Granzyme B, growth factors, Herpes virus). The purpose of this review is to highlight the synthesis and potential use of high affinity M6P analogues able to target this receptor. Several M6P analogues with phosphonate, carboxylate or malonate groups display a higher affinity and a stronger stability in human serum than M6P itself. These derivatives could be used to favour the delivery of specific therapeutic compounds to lysosomes, notably in enzyme replacement therapies of lysosomal diseases or in neoplastic drug targeting. In addition, their potential applications in preventing clinical disorders, which are associated with the activities of other M6P-proteins involved in wound healing, cell growth or viral infection, will be discussed.


Asunto(s)
Manosafosfatos/uso terapéutico , Receptor IGF Tipo 2/metabolismo , Sitios de Unión , Glicoproteínas/metabolismo , Humanos , Lisosomas/metabolismo , Lisosomas/patología , Manosafosfatos/química , Manosafosfatos/metabolismo , Neoplasias/tratamiento farmacológico , Receptor IGF Tipo 2/agonistas , Receptor IGF Tipo 2/química
5.
Bioorg Med Chem ; 4(8): 1227-35, 1996 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-8879544

RESUMEN

A new series of alkylating agents, 2-chloroethylnitrososulfamides (CENS), were developed on the model of 2-chloroethylnitrosoureas. Starting from chlorosulfonyl isocyanate, a four-step synthesis (carbamoylation-sulfamoylation, Mitsunobu alkylation, deprotection, and nitrosation) gives the title compounds in a 47-58% overall yield. The selection of the nitrosation site can be directed through an alternative route. The pharmacological evaluation shows a significant oncostatic activity towards both A549 and MCF7 cell lines.


Asunto(s)
Antineoplásicos Alquilantes/síntesis química , Etilnitrosourea/análogos & derivados , Ácidos Sulfónicos/química , Supervivencia Celular/efectos de los fármacos , Dimetilsulfóxido , Etilnitrosourea/química , Humanos , Espectroscopía de Resonancia Magnética , Masculino , Persona de Mediana Edad , Nitrosación , Células Tumorales Cultivadas
6.
Klin Monbl Augenheilkd ; 168(1): 24-32, 1976 Jan.
Artículo en Francés | MEDLINE | ID: mdl-979030

RESUMEN

This work is a survey of 82 cases of keratoconus which have been followed up for 1 to 12 years. Among them only 66 were fitted with contact lenses. The contra-indications for them are: 1. a better visual acuity with spectacles than with contact lenses, 2. advanced cases (4th degree of Amsler) whose fitting is impossible, 3. unilateral keratoconus, 4. associated diseases such as trachomatous pannus, allergic kerato-conjunctivitis. Hard corneal lenses are now in use in most of the cases. Scleral lenses are much less used than they were 10 years ago, owing probably to the great improvement of the corneal lenses during this time. These hard corneal lenses have a short Ro (4 to 7 mm), an overall diameter between 8 and 11 mm, and an optic diameter of 5 mm. They are fitted under fluorescein control. The mobility must be good too. One case was fitted with soft lenses. The visual acuity is good and so is the tolerance: 80% of the patients wear their lenses 10 hours a day or more. Contact lenses do not affect the progression of keratoconus thus finally a keratoplasty must be performed in many cases. After the operation a contact lens is very often necessary, but its daily wearing time must be divided by two, to avoid corneal neo-vascularisation. Soft corneal lenses may be used in some cases of keratoconus. They are indicated when the hard lenses are no longer tolerated and before a keratoplasty. The base curves of these soft lenses are not related to the radii of the conic cornea. In most of the cases they are between 7.50 and 8.60 mm. The diameter is large: 14 or 15 mm. The lenses must not move too much: 1 mm up or down when the patient blinks. The edge of the lens must not depress the bulbar conjunctiva and there must be no air bubble under the lens. In many cases a cylindrical spectacle lens is necessary to obtain a good visual acuity. Some authors prefer to fit a hard corneal lens over the soft one: this is the "piggy back" method. Sometimes keratoconus has appeared in patients already fitted during several years to correct a myopic astigmatism. It is not clear whether these keratoconus have been produced or not be the contact lenses.


Asunto(s)
Lentes de Contacto , Queratocono/rehabilitación , Adolescente , Adulto , Niño , Preescolar , Lentes de Contacto Hidrofílicos , Femenino , Humanos , Queratocono/etiología , Masculino , Métodos , Persona de Mediana Edad , Agudeza Visual
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