The Activity Coefficients of Amino Acids and Peptides in Aqueous Solutions Containing Guanidinium Chloride

Six systems of the type amino acid- or peptide-guanidinium chloride-water have been investigated over wide solute molality ranges using vapor pressure osmometry. The amino acids used were glycine and L-leucine, while the peptides were diglycine, triglycine, glycyl-L-leucine and L-leucyl-L-leucine. Equations for the ratios of the activity coefficients of these compounds in the salt solutions and water, respectively, were obtained in terms of the molalities of the solutes. The activity coefficient ratios for glycine are not much below one, whereas those for i.-leucine are considerably smaller reflecting the presence of the leucyl side chain. The activity coefficient ratios for the peptides are generally smaller than those for the amino acids which can be attributed to . the presence of the peptide group

Interactions of a-Chymotrypsinogen A with Some Alkylureas

The interactions of a-chymotrypsinogen A with urea, methyl-, N,N\u27-dimethyl-, ethyl-, N,N\u27-diethyl-, and propylurea were studied by means of calorimetry and circular dichroism. It has been found that the enthalpies of interaction of the alkylureas, with the exception of methylurea, with a-chymotrypsinogen A are distinctly from those of urea. Thus the transfer of the protein from water to aqueous urea and methylurea solutions is accompanied by release of heat, · i.e., the overall reaction is exothermic, whereas the transfer of the same protein to solutions of other alkylureas is characterized by consumption of heat, i.e., the overall reaction is endothermic. By examining the far UV CD spectra it can also be concluded that the alkylureas are clearly less efficient denaturants than urea. The difference in behavior reflects the presence of the hydrophobic moiety in the urea molecule

Sustained release of antimicrobials from double-layer nanofiber mats for local treatment of periodontal disease, evaluated using a new micro flow-through apparatus

Periodontal disease is a widespread chronic condition associated with degradation of periodontal tissues that requires more effective approaches for its treatment. Thus, the aim was to develop a nanodelivery system for local application of antimicrobials, with evaluation in vitro using a newly developed micro flow-through apparatus that simulates local in-vivo conditions in the periodontal pocket: small resting volume, and low gingival crevicular fluid flow rate. We successfully developed a double-layer nanofiber mat composed of a chitosan/ poly(ethylene) oxide nanofiber layer with 30% ciprofloxacin, and a poly(ε-caprolactone) nanofiber layer with 5% metronidazole. The precisely designed composition enabled sustained in-vitro release of the antimicrobials according to their specific drug release mechanisms. The rate-limiting step of ciprofloxacin release was its own low solubility at pH 7.4, when there was excess of solid drug present in the delivery system. In contrast, sustained release of metronidazole was due to slow penetration of dissolution medium through the hydrophobic poly(ε-caprolactone) nanofiber layer. The double-layer nanofiber mat developed showed antibacterial activity against Escherichia coli and Aggregatibacter actinomycetemcomitans based on plate antibiogram assays. The antimicrobial concentrations released from the nanofiber mats determined using the developed apparatus were above the minimal inhibitory concentrations against the periodontal pathogens for up to 7 days, which is valuable information for prediction of the efficacy of the nanodelivery system. Although this apparatus was specifically designed for characterization of formulations associated with treatments for periodontal disease, its applicability is much wide, as for development of any delivery system for application at target sites that have similar local conditions