betadex and salvin

Of all the active compounds in rosemary extract, carnosic acid (CaA) has the most potent antimicrobial and antioxidant activity; however, its low solubility limits its applications. We developed complexing systems using cycloamylose (CA), branched dextrin (BD), and β-cyclodextrin (βCD) to improve the solubility of CaA and compared it to the use of maltodextrin (MD). The complexes formed with CA, BD, βCD, and MD improved the water solubility of CaA by as much as 2.8-fold, 2.1-fold, 1.75-fold, and 2.06-fold, respectively. The antioxidant capacity of CaA in aqueous solutions was also enhanced in the complexes due to the increased water solubility. Interestingly, the antimicrobial activity was improved more dramatically upon complexation with CA (7.27-fold) compared to the improvement when complexed with BD (4.82-fold), βCD (2.87-fold), and MD (3.83-fold). This may be due to the improvement of the antimicrobial potential of the functional groups of CaA by complexation with flexible cyclic glucans.

Topics: Abietanes; Anti-Infective Agents; Antioxidants; beta-Cyclodextrins; Cyclodextrins; Food Additives; Food Preservatives; Free Radical Scavengers; Glucans; Plant Extracts; Polysaccharides; Rosmarinus; Solubility

The potential of intranasally administered carnosic acid to enhance the endogenous levels of neurotrophins [nerve growth factor and brain-derived neurotrophic factor] in the brain was investigated. Hydroxypropyl-β-cyclodextrin (HP-β-CD) was used to enhance the aqueous solubility of carnosic acid. The effect of different concentrations of chitosan on the permeation of carnosic acid was investigated across the bovine olfactory mucosa using Franz diffusion cell setup. The formulations were administered [intranasal (i.n.)/subcutaneous route] in Sprague-Dawley rats, and the neurotrophins were sampled from the brain by microdialysis after the treatment period and measured by enzyme-linked immunosorbent assay. Phase solubility studies revealed that the solubility of carnosic acid was enhanced significantly with increase in the concentration of HP-β-CD. The neurotrophin levels were enhanced significantly upon i.n. administration of carnosic acid with chitosan, which was approximately 1.5-2-fold more over the parenteral route. Nose-to-brain delivery of carnosic acid along with chitosan is a potential approach for treating disorders associated with depletion of neurotrophins.

Topics: 2-Hydroxypropyl-beta-cyclodextrin; Abietanes; Administration, Intranasal; Animals; beta-Cyclodextrins; Brain; Brain-Derived Neurotrophic Factor; Cattle; Chitosan; Drug Carriers; Excipients; Hippocampus; In Vitro Techniques; Microdialysis; Molecular Structure; Nerve Growth Factor; Olfactory Mucosa; Plant Extracts; Rats; Rats, Sprague-Dawley; Solubility; Up-Regulation