Taken together, these data reveal that nanonization of nystatin provides a novel approach to enhancing its efficacy in the treatment of oral candidiasis.

An extemporaneous formulation consisting of lansoprazole microgranules in Ora-Blend maintained acceptable quality attributes when stored for three days at 4.5-5.5 °C.

Drugs and proteins with poor intestinal permeability have a limited oral bioavailability. To remediate this problem, a receptor-mediated endocytosis and transcytosis approach was explored. Indeed, the non-toxic β subunit of cholera toxin (CTB) can cross the intestinal barrier by binding to receptor GM1. In this study, we explored the use of GM1-binding peptides and CTB as potential covalent carriers of poorly permeable molecules. GM1-binding peptides (G23, P3) and CTB were conjugated to poorly permeable fluorescent probes such as FITC and albumin-FITC using triethylene glycol spacers and click chemistry.The affinity of the peptide conjugates with receptor GM1 was confirmed by isothermal titration calorimetry or microscale thermophoresis and the results suggested the involvement of non-specific interactions. Conjugating the model drugs to G23 and P3 improved the internalization into Caco-2 and T84 cells, although the process was not dependent of the amount of GM1 receptor. However, conjugation of BSA-FITC to CTB increased the internalization in the same cells in a GM1-dependent pathway.Peptides conjugates demonstrated a limited permeability through a Caco-2 monolayer, whereas G23-and CTB-conjugates slightly enhanced permeability through a T84 cell monolayer compared to model drugs alone. Since CTB can improve the permeability of large macromolecules such as albumin, it is an interesting carrier for the improvement of oral bioavailability of various other macromolecules such as heparins, proteins and siRNAs.

The crystal preparation and structure of a cyclic derivative of γ-amino­butyric acid, GABA, is reported.