Cyclodextrin-functionalized biomaterials loaded with miconazole prevent Candida albicans biofilm formation in vitro.

Polyethylene (PE) and polypropylene (PP) were functionalized at their surfaces with cyclodextrins (CDs) in order to prevent the adhesion and proliferation of Candida albicans on medical devices made from these polymers. The surface functionalization involved the grafting of glycidyl methacrylate (GMA) after oxidative gamma-ray pre-irradiation, followed by the attachment of beta-CD and HP-beta-CD to PE-g-GMA and PP-g-GMA surfaces. The yield of CD functionalization directly depended on the amount of GMA grafted. The presence of CDs on the surface of the polymers did not compromise their cell compatibility, but remarkably changed their protein adsorption profile. In contrast to unmodified PE and PP that adsorb significant amounts of fibrinogen ( approximately 0.047 mg cm(-2)) but not albumin, the CD-modified polyethers promoted the adsorption of albumin (between 0.015 and 0.155 mg cm(-2)) and reduced the adsorption of fibrinogen. Furthermore, functionalization with CDs provided PE and PP with the capability to incorporate the anti-fungal drug miconazole (up to 0.27 mg cm(-2)), leading to reduced biofilm formation by C. albicans in an in vitro biofilm model system. Overall, the results of the work indicate that the novel approach for functionalization of PE and PP is potentially useful to reduce the likelihood of foreign body-related infections.

Functionalization of acrylic hydrogels with alpha-, beta- or gamma-cyclodextrin modulates protein adsorption and antifungal delivery.

Poly(hydroxyethyl methacrylate) (pHEMA) hydrogels were functionalized with pendant alpha-, beta- and gamma-cyclodextrins (CD) with the aim of improving the biocompatibility and increasing the ability to host drug molecules. Pendant alpha-, beta- and gamma-CDs did not affect swelling of the hydrogels but slightly decreased the water contact angle. Protein deposition was notably dependent on the nature of the CD, due to their different affinities for hydrophobic moieties of proteins. Lysozyme and albumin sorption was hindered by gamma-CD. Functionalization with beta-CD also reduced protein sorption, although less so, while alpha-CD decreased lysozyme deposition but enhanced albumin sorption compared with control pHEMA hydrogels. Loading of the hydrogels with miconazole was carried out by immersion in drug suspension followed by autoclaving. Functionalization with gamma-CD doubled the affinity of the network for the drug and resulted in the highest amount loaded (up to 170 mgg(-1)). Sustained delivery was observed for several days. Some miconazole-loaded hydrogels completely prevented Candida albicans biofilm formation as assayed in an in vitro microbiological test.

Chiral separation strategy in polar organic solvent chromatography and performance comparison with normal-phase liquid and supercritical-fluid chromatography.

A strategy, including a rapid screening and several optimisation steps, for the separation of chiral molecules of pharmaceutical interest by polar organic solvent chromatography (POSC), using four polysaccharide-based stationary phases, is proposed and compared with previously reported strategies in normal-phase (NPLC) and supercritical fluid chromatography (SFC). In a first part of this paper, different examples demonstrate the effectiveness of the POSC strategy for fast method development. Optimisation is based on the use of experimental design to map the experimental domain in an efficient way. In the second part, the best screening results, obtained after performance of earlier defined chromatographic screening strategies in NPLC and SFC, are compared to those obtained in POSC. The three techniques show complementary separation results and allowed baseline separation of 23 of 25 compounds. POSC is found to be a very interesting separation mode compared to NPLC, because of the many fast (< 10 min) baseline separations obtained.