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1.
Curr Drug Targets ; 21(14): 1495-1510, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-32538725

RESUMEN

About 40% of newly-discovered entities are poorly soluble in water, and this may be an obstacle in the creation of new drugs. To address this problem, the present review article examines the structure and properties of cyclodextrins and the formation and potential uses of drug - cyclodextrin inclusion complexes. Cyclodextrins are cyclic oligosaccharides containing six or more D-(+)- glucopyranose units linked by α-1,4-glycosidic bonds, which are characterized by a favourable toxicological profile, low local toxicity and low mucous and eye irritability; they are virtually non-toxic when administered orally. They can be incorporated in the formulation of new drugs in their natural form (α-, ß-, γ-cyclodextrin) or as chemically-modified derivatives. They may also be used as an excipient in drugs delivered by oral, ocular, dermal, nasal and rectal routes, as described in the present paper. Cyclodextrins are promising compounds with many beneficial properties, and their use may be increasingly profitable for pharmaceutical scientists.


Asunto(s)
Ciclodextrinas/administración & dosificación , Ciclodextrinas/química , Tecnología Farmacéutica , Ciclodextrinas/farmacocinética , Ciclodextrinas/toxicidad , Portadores de Fármacos/química , Sistemas de Liberación de Medicamentos , Excipientes , Humanos , Impresión Tridimensional
2.
Molecules ; 21(2)2016 Feb 06.
Artículo en Inglés | MEDLINE | ID: mdl-26861275

RESUMEN

As many substances are poorly soluble in water and thus possess decreased bioavailability, creating orally administered forms of these substances is a challenge. The objective of this study was to determine whether the solubility of megestrol acetate, a Biopharmaceutical Classification System (BCS) class II drug, can be improved by using a newly-synthesized surfactant (Rofam 70: a rapeseed methyl ester ethoxylate) and compare it with two references surfactants (Tween 80, Pluronic F68) at three different pH values. Spectrophotometry was used to compare the solubility profiles in the presence of three tested surfactants at pH 5.0, 7.4 and 9.0. Rapeseed methyl ester ethoxylate was found to improve the solubility of the BCS Class II drug and increase its bioavailability; It increased drug solubility more effectively than Pluronic F68. Its cytotoxicity results indicate its possible value as a surfactant in Medicine and Pharmacy.


Asunto(s)
Biopolímeros/química , Acetato de Megestrol/química , Nanopartículas/química , Línea Celular Tumoral , Humanos , Concentración 50 Inhibidora , Acetato de Megestrol/farmacología , Poloxámero/química , Polisorbatos/química , Solubilidad , Tensoactivos/química
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