betadex and baicalin

Baicalin (BCL) has potential therapeutic benefits, but its clinical outcomes are restricted mainly because of low water solubility. This study sought to improve the water solubility of BCL by the formation of inclusion complex with β-cyclodextrin (β-CD).. The inclusion complex was studied by solubility test, differential scanning calorimeter (DSC), Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD),. The DSC, FTIR, XRD,. β-cyclodextrin complex can be used as an effective formulation strategy for development of BCL-loaded delivery system with better therapeutic outcomes.

Topics: Animals; beta-Cyclodextrins; Biological Availability; Calorimetry, Differential Scanning; Chemistry, Pharmaceutical; Chromatography, High Pressure Liquid; Flavonoids; Hydrophobic and Hydrophilic Interactions; Male; Molecular Docking Simulation; Rats; Rats, Sprague-Dawley; Solubility; Spectroscopy, Fourier Transform Infrared; X-Ray Diffraction

In this study, 2,6-dimethyl-β-cyclodextrin (DM-β-CD) functionalized graphene nanosheets (DM-β-CD-GNs) were successfully synthesized by a simple wet-chemical strategy. The as obtained DM-β-CD-GNs were characterized by UV-vis spectroscopy, Fourier transform Infrared (FT-IR) spectroscopy, atomic force microscopy (AFM) and transmission electron microscopy (TEM). The new nanocomposite possesses the unique properties of graphene (large surface area and high conductivity) and DM-β-CD (high supramolecular recognition and enrichment capability). Based on the above properties, a highly sensitive electrochemical sensor was developed to detect two flavonoid drugs (isoquercitrin and baicalin). At the DM-β-CD-GNs modified glassy carbon electrode (DM-β-CD-GNs/GCE), the peak currents of the two drugs increased dramatically compared with that on the bare GCE and GNs/GCE which due to the synergetic effects of GNs and DM-β-CD molecules. The linear response ranges for isoquercitrin and baicalin are 10nM-3.0μM and 0.04μM -3.0μM, with the detection limits of 4nM and 10nM, respectively. The method might open up a new possibility for the widespread use of electrochemical sensors for monitoring of ultra-trace flavonoid drugs owing to its advantages of simple preparation, low cost, high sensitivity, good stability and reproducibility.

Topics: beta-Cyclodextrins; Biosensing Techniques; Conductometry; Electrodes; Equipment Design; Equipment Failure Analysis; Flavonoids; Graphite; Nanoparticles; Quercetin; Surface Properties

The formation of the complexes of BG with beta-CD and HP-beta-CD was studied by UV-vis absorption spectroscopy, fluorescence spectra, Phase-solubility measurements and nuclear magnetic resonance spectroscopy (NMR) in solution. The formation constants (K) of complexes were determined by fluorescence method and Phase-solubility measurements. The results showed that the inclusion ability of beta-CD and its derivatives was the order: HP-beta-CD>beta-CD. In addition, the experimental resulted confirmed the existence of 1:1 inclusion complex of BG with CDs. The antioxidant ability studies of BG and CDs complexes were done. The results obtained indicated that the BG/HP-beta-CD complex was the most reactive form, and then was the BG/beta-CD complex; the last was BG. Special configuration of complex has been proposed on NMR technique.

Topics: 2-Hydroxypropyl-beta-cyclodextrin; Antioxidants; beta-Cyclodextrins; Biphenyl Compounds; Excipients; Flavonoids; Free Radicals; Magnetic Resonance Spectroscopy; Molecular Structure; Picrates; Scutellaria baicalensis; Solubility; Spectrometry, Fluorescence; Spectrophotometry, Ultraviolet

To increase drug concentration in the head through intranasal administration, we have investigated the excised animal nasal mucosa permeability and nasal toxicity of the baicalin drug carrier systems, such as baicalin liposomes, beta-cyclodextrin inclusion compound, and phospholipid complex. A transport of baicalin drug carrier systems through nasal mucosa was simulated in diffusion chamber in vitro, and swine, caprine and rabbit nasal mucosa was used, the concentration of drug in the receptor was determined by HPLC. By taking the apparent permeability coefficients as evaluation standard, investigated the isolated animal nasal mucosa permeability of different baicalin drug systems was investigated for screening the best baicalin drug carrier system through nasal cavity administration. Toxicity of baicalin and its phospholipids complex on toad palate mucosal cilia movement and rats nasal mucosa long-term toxicity were studied in vivo. The apparent permeability coefficient of three kinds of baicalin drug carrier systems was better than that of baicalin (P < 0.05), and its lag-time was obviously shortened. At the same time, the apparent permeability coefficient of phospholipid complex was higher than those of other two drug carrier systems (P < 0.05). The results showed that the baicalin phospholipids complex nasal mucosa permeability was obviously superior to the other two drug systems. Baicalin phospholipids complex had no toxicity to ciliary movement, and had no irritation to rat nasal mucosa. The results show that baicalin phospholipid complex was the best baicalin drug carrier system, it could significantly enhance the permeability of baicalin across nasal mucosa, had no toxicity to nasal mucosa, and could be used for intranasal administration.

Topics: Administration, Intranasal; Animals; beta-Cyclodextrins; Bufo bufo; Drug Carriers; Drug Delivery Systems; Female; Flavonoids; Goats; Liposomes; Male; Nasal Mucosa; Palate; Permeability; Phospholipids; Rabbits; Random Allocation; Rats; Swine