It is known that hydrocortisone can be converted to a potent angiogenesis inhibitor by coadministration with heparin or with a sulfated cyclodextrin. The activity of tetrahydrocortisol-S, a purely angiostatic corticosteroid, can be potentiated by beta-cyclodextrin tetradecasulfate as shown in this study. This drug "pair" and other pairs of corticosteroids and beta-cyclodextrin tetradecasulfate ...

Fexofenadine is a selective histamine H(1) receptor antagonist, used for relief of the symptoms of allergy. However its aqueous solubility is very poor. Solid inclusion complexes of fexofenadine and β-cyclodextrin were prepared at the molar ratios of 1:1 and 1:2 by kneading, and coprecipitation methods to improve its solubility. Characterization of the complexes was performed using infrared spe...

Feeding states may affect the performance of colonic prodrugs. The aim is to investigate the influence of feeding regimen in Wistar rats on: (i) distribution and pH contents along the gut and (ii) metabolism of two colonic prodrugs, diclofenac-β-cyclodextrin and a commercially available control, sulfasalazine, within the caecal and colonic contents. Male Wistar rats were subject to four differe...

UNLABELLED BACKGROUND Recently, various metallocenes were synthesized and analyzed by biological activity point of view (such as antiproliferative properties): ruthenocenes, cobaltoceniums, titanocenes, zirconocenes, vanadocenes, niobocenes, molibdocenes etc. Two main disadvantages of metallocenes are the poor hydrosolubility and the hydrolytic instability. These problems could be resolved i...

Amphiphilic cyclodextrin–fullerene conjugates have potential biological activity, due to their water solubility. In order to study the influence of the linker of these conjugates on solubility and aggregation, a permethylated β-cyclodextrin–C60 conjugate with a short linker –(CH2)2NHCO–, which is attached to the secondary face of β-cyclodextrin was synthesized. Its solubility in water and its U...

Three distinct viologen derivatives have been designed and successively synthesized. They are shown to form 1:1 or 2:1 host−guest inclusion complexes with β-cyclodextrin (β-CD) in aqueous solution. In comparison with...

Cyclodextrin (CD) are cyclic oligosaccharides consisting of glucopyranosyl units linked by α-(1,4) bonds. The widely used natural cyclodextrins are α-, βand γ-cyclodextrin consisting of 6, 7 and 8 glucopyranose units, respectively. The cyclodextrin molecules have a unique structure with a hydrophobic cavity and a hydrophilic surface which can form inclusion complex with a wide variety of guests...

The solubility enhancement of diazepam and nitrazepam in water was analyzed depending on temperature and amount of α-cyclodextrin (α-CD), β-cyclodextrin (β-CD) and 2-hydroxypropyl-β-cyclodextrin (2-HP-β-CD). The interactions of drug-cyclodextrin in solution were investigated by the phase-solubility analysis. Diazepam (nitrazepam) content in aqueous complexation medium was analyzed UV spectropho...

Menkes disease (MD) is a neurodegenerative disorder characterized by copper deficiency. It is caused by defective intestinal absorption of copper resulting from a deficiency of a copper-transporting ATPase, ATP7A. We investigated the effects of combination therapy with copper and disulfiram, a known lipophilic chelator. We synthesized a copper-disulfiram complex (Cu-DSF) and determined its crys...