Cyclodextrins and their pharmaceutical applications

Loftsson, Þorsteinn; Duchêne, Dominique

doi:10.1016/j.ijpharm.2006.10.044

Cited by 1,456 publications

(861 citation statements)

References 60 publications

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“…La diferencia en la CI 50 puede estar asociada con la mayor solubilidad y estabilidad fisicoquímica producto de la inclusión en la beta-ciclodextrina del complejo de paladio (II) (24,32). Otros autores han propuesto diferentes metodologías para mejorar la actividad de los complejos de paladio (II), por ejemplo, la modificación de la proporción del ligando de las tiosemicarbazonas, con una CI 50 de 0,13 µM (10), comparable con las reportadas en este estudio en la línea celular MCF-7, y la del complejo [Pd(MePhPzTSC)2] parcialmente incluido en la beta-ciclodextrina, con una CI 50 de 0,14 µM.…”

Section: Discussionunclassified

Cytotoxic effect of palladium (II) inclusion compounds in beta-cyclodextrin

et al. 2016

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Introducción. Las tiosemicarbazonas y sus complejos de paladio (II) poseen actividad antineoplásica con pocos efectos secundarios, por lo cual se las considera como una nueva alternativa terapéutica. Sin embargo, existen diferencias en los rangos de la concentración inhibitoria media (CI50) asociada a la divergencia estructural y la solubilidad de los complejos, así como a la sensibilidad de los blancos celulares. La inclusión de fármacos en la beta-ciclodextrina con fines terapéuticos ha mejorado su solubilidad y estabilidad, pero los efectos de su combinación con los complejos de paladio (II) y las tiosemicarbazonas no se han comprobado aún.Objetivo. Estudiar el efecto citotóxico de los complejos de paladio en la beta-ciclodextrina.Materiales y métodos. La actividad citotóxica de los complejos de paladio en la beta-ciclodextrina se evaluó en la línea celular de cáncer de mama (MCF-7), empleando el método de la sulforodamina B.Resultados. Los ligandos MePhPzTSC y Ph2PzTSC, sus complejos de paladio (II) libres e incluidos en la beta-ciclodextrina y el cisplatino mostraron actividad citotóxica en la línea celular MCF-7; sin embargo, la citotoxicidad fue mayor con la inclusión en la beta-ciclodextrina ([Pd(MePhPzTSC)2]•ß-CD y [Pd(Ph2PzTSC)2]•ß-CD). La concentración inhibitoria media (CI50) para estos complejos se obtuvo en concentraciones de 0,14 y 0,49 μM, y con dosis hasta cinco veces inferiores comparadas con las concentraciones de los ligandos libres (1,4 y 2,9 μM), de los complejos de paladio (II) libres (0,57 y 1,24 μM) y del cisplatino (6,87 μM).Conclusiones. El uso de la beta-ciclodextrina mejoró significativamente la actividad citotóxica de las tiosemicarbazonas y sus complejos de paladio (II), lo cual probablemente está asociado al incremento de la solubilidad y biodisponibilidad del compuesto, estrategia que se puede sugerir para el diseño de futuros fármacos antineoplásicos.

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Section: Discussionunclassified

Cytotoxic effect of palladium (II) inclusion compounds in beta-cyclodextrin

et al. 2016

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“…To improve the solubility and to reduce some of the few toxicological risks (e.g. the nephrotoxicity after parenteral administration of β-CD) numerous CD derivatives have been prepared 27,[32][33][34][35] . Among industrially produced, standardized, and available β-CD derivatives, currently the most important ones are the heterogeneous, amorphous, highly water-soluble methylated β-CDs, 2-hydroxypropylated β-CDs (HP-β-CD) and sulfobutylether β-CD (SBE-β-CD).…”

Section: Cyclodextrinsmentioning

confidence: 99%

Polysaccharides in Oral Drug Delivery — Recent Applications and Future Perspectives

Klein

2009

Polysaccharide Materials: Performance by Design

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“…Other methods used to improve drug solubility include complexation [17], liquisolid techniques [18,19] and salt formation [20,21]. Several authors have classed the solid dispersion approach as one of the most effective method of improving dissolution of drugs [5,8,22].…”

Section: Introductionmentioning

confidence: 99%

Solid-state, triboelectrostatic and dissolution characteristics of spray-dried piroxicam-glucosamine solid dispersions

Adebisi

Kaialy

Hussain

et al. 2016

Colloids and Surfaces B: Biointerfaces

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Solid-state, triboelectrostatic and dissolution characteristics of spray-dried piroxicam-glucosamine solid dispersions, Colloids and Surfaces B: Biointerfaces http://dx.doi.org/10. 1016/j.colsurfb.2016.07.032 This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain. 4. GLU improved the handling of PXM as it significantly reduced its charge in all the spray dried formulations. Technique could be used to determine appropriate formulations that improve handling AbstractThis work explores the use of both spray drying and D-glucosamine HCl (GLU) as a hydrophilic carrier to improve the dissolution rate of piroxicam (PXM) whilst investigating the electrostatic charges associated with the spray drying process. Spray dried PXM:GLU solid dispersions were prepared and characterised (XRPD, DSC, SEM). Dissolution and triboelectric charging was also conducted. The results showed that the spray dried PXM alone, without GLU produced some PXM form II (DSC results) with no enhancement in solubility relative to that of the parent PXM.XRPD results also showed the spray drying process to decrease the crystallinity of GLU and solid dispersions produced. The presence of GLU improved the dissolution rate of PXM. Spray dried PXM: GLU at a ratio of 2:1 had the most improved dissolution. The spray drying process generally yielded PXM-GLU spherical particles of around 2.5 µm which may have contributed to the improved dissolution. PXM showed a higher tendency for charging in comparison to the carrier GLU (-3.8 versus 0.5 nC/g for untreated material and -7.5 versus 3.1 nC/g for spray dried materials). Spray dried PXM and spray dried GLU demonstrated higher charge densities than untreated PXM and untreated GLU, respectively. Regardless of PXM:GLU ratio, all spray dried PXM:GLU solid dispersions showed a negligible charge density (net-CMR: 0.1 -0.3 3 nC/g). Spray drying of PXM:GLU solid dispersions can be used to produce formulation powders with practically no charge and thereby improving handling as well as dissolution behaviour of PXM.

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Cyclodextrins and their pharmaceutical applications

Cited by 1,456 publications

References 60 publications

Cytotoxic effect of palladium (II) inclusion compounds in beta-cyclodextrin

Cytotoxic effect of palladium (II) inclusion compounds in beta-cyclodextrin

Polysaccharides in Oral Drug Delivery — Recent Applications and Future Perspectives

Solid-state, triboelectrostatic and dissolution characteristics of spray-dried piroxicam-glucosamine solid dispersions

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