No abstract

The effect of the laser irradiation (532 nm) on films prepared from Citrobacter freundii mixed with erythrosine dye was investigated by using atomic force microscopy. It was observed that morphological changes of bacterial surfaces after irradiations, which were attributed to cellular damage of the outer membranes, are a result of a photodynamic effect. The results suggested that the combination of erythrosine and laser light at 532 nm could be a candidate to a photodynamic therapy against C. freundii.

Films from congo red (CR) alternated with poly(allylamine hydrochloride), PAH, were prepared by layer-by-layer and alternative spray techniques. In order to investigate the change of roughness induced by laser light irradiation (532 nm), both kinds of films were characterized by using UV-visible spectroscopy and atomic force microscopy (AFM). At different irradiation times, layer-by-layer, LbL, films showed small changes in the roughness and irregular behavior, whereas spray films exhibited higher and a regular decreasing of roughness with increasing irradiation time. The higher roughness of spray films as compared with the LbL ones was attributed to different formation mechanisms of the films. The decreasing of the roughness as a function of the irradiation time (exhibited by the spray films) was associated to surface relaxation due to the interplay between photoisomerization of congo red dye and the heating of the sample during the laser light irradiation. The results suggested that the alternative spray technique is the best choose to control of roughness of the films by using light irradiation.

This study aimed to investigate whether hot-melt extrusion (HME) processing can promote molecular encapsulation of a multi-component natural product composed of volatile and pungent hydrophobic substances (ginger oleoresin, OR) with cyclodextrins. 6-gingerol and 6-shogaol, the biomarkers of ginger OR, were quanti ed by HPLC. Phase-solubility studies were performed using β-cyclodextrin (βCD) and hydroxypropyl-β-cyclodextrin (HPβCD) for ginger OR complexation. Solid complexes were then prepared by thermal (HME) and solvent (slurry, SL)-based methods. Morphology, thermal behavior, solubility, in vitro dissolution, and in vivo anti-in ammatory activity were evaluated. HPβCD gave rise to AL-type complexes with ginger OR, whereas βCD led to materials with limited solubility. Ginger OR was complexed with HPβCD by HME without signi cant change in gingerol and shogaol content. Additionally, TGA suggested higher volatile retention in HME complexes than SL ones. Shogaol and gingerol solubility and dissolution signi cantly increased from SL and HME complexes compared with ginger OR. In turn, 1: 2 OR/HPβCD HME complex showed higher 6-shogaol solubility than SL, associated with a gradual release. The carrageenan-induced pleurisy test showed that the anti-in ammatory activity of ginger OR was maintained after complexation with HPβCD. The complexes signi cantly decrease the levels of IL-1β and inhibit cell migration. HME complex showed performance equivalent to the positive control and superior to the SL material. Taken together, these results indicate that HME can be useful for promoting the molecular encapsulation of complex natural products that contain volatile and thermolabile substances. HME complexes showed better in vivo and in vitro performance than complexes prepared using the solvent-based method.

This study aims to investigate the effect of the preparation of solid dispersions using supercritical CO2 (scCO2) on the physicochemical properties and the performance of supramolecular gels based on polymer-cyclodextrin (CD) interactions (named poly(pseudo)rotaxanes, PPR) envisaging a transdermal administration. Solid dispersions containing Soluplus®, the antihypertensive drug carvedilol (CAR), and CD (αCD or HPβCD) were prepared and characterized by HPLC, XRPD, FTIR, and DSC. PPRs prepared from solid dispersions (SCF gels) and the corresponding physical mixtures (PM gels) were analyzed regarding rheology, morphology, in vitro drug diffusion, and ex vivo drug skin permeation. The application of scCO2 led to the loss of the crystalline lattice of CAR while preserving its chemical identity. On the contrary, αCD crystals were still present in the SCF solid dispersions. SCF gels were more uniform than their corresponding PM, and the supercritical treatment resulted in changes in the rheological behavior, reducing the viscosity. CAR in vitro diffusion was significantly higher (p < 0.05) for the αCD-based SCF gel than its corresponding PM gel. Drug skin permeation showed a significant increase in drug flux from CD-based SCF gels (containing αCD or HPβCD) compared to corresponding PM gels. Additionally, the pretreatment of the skin with αCD exhibited increased CAR permeation, suggesting an interaction between αCD and the skin membrane. Results evidenced that SCF processing decisively modified the properties of the supramolecular gels, particularly those prepared with αCD. Graphical Abstract