betadex and isoborneol

Monoterpenes are non-polar secondary metabolites widely used by industry due to their excellent therapeutic, food-ingredient and cosmetic properties. However, their low solubility in water limits their use. In this sense, cyclodextrins (CDs) have been widely used to solve these technological challenges. Thus, this study aims to use (-)-borneol as a monoterpene model to prepare inclusion complexes between β-CD and hydroxypropyl-β-CD (HP-β-CD) through different ways and characterize them in order to choose the best inclusion method to improve physicochemical properties of monoterpenes. To achieve this goal, the samples were prepared by physical mixture (PM), paste complex (PA) and freeze-drying complex (FD) and then, extensively characterized by thermal analysis, Fourier-transform infrared spectroscopy, scanning electron microscopy, size particle, X-ray diffraction and nuclear magnetic resonance. The physicochemical results showed that freeze-drying was more effective to form inclusion complexes between (-)-borneol with both CDs. This research highlights the importance of recognizing the best method to prepare inclusion complexes, including food additives as (-)-borneol, to achieve better results in food preparations.

Topics: 2-Hydroxypropyl-beta-cyclodextrin; beta-Cyclodextrins; Calorimetry, Differential Scanning; Camphanes; Food Ingredients; Freeze Drying; Magnetic Resonance Spectroscopy; Microscopy, Electron, Scanning; Monoterpenes; Particle Size; Solubility; Spectroscopy, Fourier Transform Infrared; X-Ray Diffraction

This study's primary purpose was to develop a new technique to stabilize high value-added bioactive volatile compounds present in essential oils to ensure their usability as chemical raw materials with enhanced stability. Selective isolation and encapsulation of various volatile compounds by changing the electrospraying process parameter, including voltage, flow rate, and β-Cyclodextrin concentration, were attributed to the formation of inclusion complexes between β-cyclodextrin and volatile compounds. Investigations regarding the effects of independent process variables on simultaneous isolation and selective encapsulation of volatile compounds during electrospraying of β-cyclodextrins were carried out mainly with TLC analyses. The TLC analyses were confirmed with GC, GC-MS, and

Topics: Aldehydes; Benzoates; beta-Cyclodextrins; Bicyclic Monoterpenes; Camphanes; Chemistry Techniques, Analytical; Chromatography, Gas; Chromatography, Thin Layer; Cistus; Gas Chromatography-Mass Spectrometry; Hydrogen Bonding; Hydrophobic and Hydrophilic Interactions; Magnetic Resonance Spectroscopy; Microscopy, Atomic Force; Nanoparticles; Nigella sativa; Oils, Volatile; Palmitic Acid; Solubility; Spectrometry, Mass, Electrospray Ionization; Volatile Organic Compounds

Topics: Alzheimer Disease; Amyloid beta-Peptides; Animals; beta-Cyclodextrins; Blood-Brain Barrier; Camphanes; Cell Line, Tumor; Cells, Cultured; Delayed-Action Preparations; Drug Delivery Systems; Drug Evaluation, Preclinical; Drug Synergism; Humans; Mice; Nanoconjugates; Oxidation-Reduction; Porosity; Protein Aggregation, Pathological; Reactive Oxygen Species; Resveratrol; Selenium; Specific Pathogen-Free Organisms

To study the interaction of drugs of different properties, namely puerarin, borneol and catalpol in the process of in- clusion, in order to explore the inclusion regularity of multi-component and multi-property traditional Chinese medicine compound in- clusions. With HP-β-CD as the inclusion material, the freeze-drying method was used to prepare the inclusion. The inclusion between puerarin, borneol and catalpol was tested by measuring the inclusion concentration, DSC and X-ray diffraction. According to the find- ings, when insoluble drugs puerarin and borneol were included simultaneously, and puerarin was overdosed, puerarin included was almost equal to puerarin included, and borneol was not included. When puerarin was under-dosed, and HP-β-CD was overdosed, borne- ol was included, and the simultaneous inclusion was lower than the separate inclusion of borneol. When water-soluble drug catalpol was jointly included with puerarin or borneol, the simultaneous inclusion was almost the same with their separate inclusion, without charac- teristic peak of catalpol in DSC and X-ray diffraction patterns. There is a competition in the simultaneous inclusion between water-solu- ble drugs puerarin and borneol and a stronger competition in puerarin. The water-soluble drug catalpol could be included with HP-β-CD with no impact on the inclusion of puerarin or borneol.

Topics: 2-Hydroxypropyl-beta-cyclodextrin; beta-Cyclodextrins; Brain Ischemia; Camphanes; Drug Compounding; Freeze Drying; Iridoid Glucosides; Isoflavones; Solubility

The aims of this study were to prepare a thermosensitive composite hydrogel (TCH) by mixing 24% (w/v) poloxamer 407 (P407), 16% (w/v) poloxamer 188 (P188) and 0.1% (w/v) carbopol 940 (C940), and to determine the effect of natural borneol/ (2-hydroxypropyl)-β-cyclodextrin (NB/HP-β-CD) inclusion complex on the phase transition temperature, mechanical, rheological properties, and release behaviors of the TCH using the tube inversion method, a texture analyzer, a rheometer, and in vitro release , respectively. The results showed that as the concentration of NB/HP-β-CD increased, the phase transition temperature of the TCH was increased from 37.26 to 38.34 °C and the mechanical properties of the TCH showed that the hardness, cohesiveness, strength, and adhesiveness were increased from 0.025 to 0.064 kg, 0.022 to 0.064 kg, 0.110 to 0.307 kg and 0.036 to 0.105 kg, respectively, but the rheological properties of the TCH showed that G', G'' and η were decreased from 7,760 to 157.50 Pa, 1,274 to 36.28 Pa and 1,252 to 25.37 Pas, respectively. The in vitro release showed that an increasing NB/HP-β-CD concentration decreased the release rate of NB from the TCH, but the amount of NB released was more than 96% at 60 min, which showed the TCH had good release behavior.

Topics: Acrylic Resins; Adhesiveness; beta-Cyclodextrins; Camphanes; Elasticity; Hardness; Hydrogels; Poloxamer; Rheology; Transition Temperature; Viscosity

The aims of this study were to optimize the preparation conditions of natural borneol/β-cyclodextrin (NB/β-CD) inclusion complex by ultrasound method, and to investigate its improvement of stability and solubility. The complex was characterized by different various spectroscopic techniques including Fourier transform infrared spectroscopy, X-ray diffractometry, and differential scanning calorimetry. The results demonstrate that NB could be efficiently loaded into β-CD to form an inclusion complex by ultrasound method at a molar ratio of 1: 1and mass ratio of 1: 6. The complex exhibited different physicochemical characteristics from that of free NB. Typically, formation of β-CD inclusion significantly enhanced the stability and aqueous solubility of NB.. Natural borneol (NB) has the potential to be widely used in the fields of medical and functional food, due to its specificity. However, the disadvantages of unstability in the preparation and storage process due to its easy sublimation and the low water solubility limit its application. This research provides an effective way to improve the solubility and stability of NB by preparing NB/β-CD inclusion complex. Furthermore, theoretical basis is also provided for the application development of NB.

Topics: Anti-Bacterial Agents; Anti-Inflammatory Agents, Non-Steroidal; beta-Cyclodextrins; Calorimetry, Differential Scanning; Camphanes; Chemical Phenomena; Coordination Complexes; Food Additives; Food Storage; Food Technology; Foods, Specialized; Hydrophobic and Hydrophilic Interactions; Medicine, Traditional; Solubility; Sound; Spectroscopy, Fourier Transform Infrared; Sublimation, Chemical; X-Ray Diffraction

Natural borneol (NB)/2-hydroxypropyl-β-cyclodextrin (HP-β-CD) inclusion complex has been prepared, and characterized by differential scanning calorimetry (DSC), X-ray diffractometry (XRD) and Fourier transform infrared spectroscopy (FT-IR). The phase solubility and release of NB, and its effect on the absorption of tetramethylpyrazine phosphate (TMPP) in mice were also measured. The results demonstrated that NB could be efficiently loaded into HP-β-CD to form an inclusion complex at a mass ratio of 1 : 6, and the inclusion complex had different physicochemical characteristics from free NB. The profile of phase solubility displayed a typical A(L)-type, indicating the formation of 1 : 1 stoichiometric inclusion complex. Additionally, the stability of the inclusion complex was greatly improved compared with that of NB. The results of absorption of TMPP in mouse indicated that NB/HP-β-CD enhanced the absorption of TMPP and the concentration of TMPP in brain tissue, especially in the early period. Both TMPP plasma and brain concentration-time courses in mice were fitted to open two-compartment model with first-order absorption after oral administration of TMPP with NB/HP-β-CD. However, the use of NB/HP-β-CD did not change the in vivo behavior of TMPP. Our results suggest the application potential of NB/HP-β-CD inclusion in pharmaceutics.

Topics: 2-Hydroxypropyl-beta-cyclodextrin; Absorption; Animals; beta-Cyclodextrins; Biological Availability; Calorimetry, Differential Scanning; Camphanes; Drug Stability; Mice; Pyrazines; Solubility; X-Ray Diffraction

To study the effects of penetration enhancers and their combinations on the curcumine transdermal drug delivery (CUR-TDDS).. The penetration rate of curcumin through rat skin in vitro was measured using Valia-Chien diffusion cells, and orthogonal design method was set up for experimental design.. The optimum penetration enhancers were: 3% hydroxypropyl beta cyclodextrins (HP-beta-CD), 9% borneol and 3% peppermint oil.. The HP-beta-CD has the most potent enhancing effect.

Topics: 2-Hydroxypropyl-beta-cyclodextrin; Administration, Cutaneous; Animals; beta-Cyclodextrins; Camphanes; Chemistry, Pharmaceutical; Curcumin; Drug Carriers; Drug Delivery Systems; In Vitro Techniques; Mentha piperita; Mice; Mice, Inbred ICR; Permeability; Plant Oils; Skin; Skin Absorption; Transdermal Patch

A series of modified beta-cyclodextrins with nucleobase substituents, that is, mono(6-ade-6-deoxy)-beta-cyclodextrin (2) and mono(6-ura-6-deoxy)-beta-cyclodextrin (3) as well as mono(6-thy-6-deoxy)-beta-cyclodextrin (4), were selected as molecular receptors to investigate their conformation and inclusion complexation behaviors with some chiral molecules, that is, (+)-camphor, (-)-camphor, (+)-borneol, and (-)-borneol, by spectrophotometric and microcalorimetric titrations in aqueous phosphate buffer solution (pH 7.2) at 298.15 K. Circular dichroism and NMR studies demonstrated that these nucleobase-modified beta-cyclodextrins adopted a co-inclusion mode upon complexation with guest molecules; that is, the originally self-included nucleobase substituents of the host did not move out from the beta-cyclodextrin cavity, but coexisted with guest molecule in the beta-cyclodextrin cavity upon inclusion complexation. Significantly, these nucleobase-modified beta-cyclodextrins efficiently enhanced the molecular binding ability and the chiral recognition ability of native beta-cyclodextrin, displaying enantioselectivity up to 3.7 for (+)-camphor/(-)-camphor pair by 2 and 3.5 for (-)-borneol/(+)-borneol pair by 3. The enhanced molecular/chiral recognition abilities of 2-4 toward (+/-)-camphor were mainly attributed to the increased entropic gains due to the extensive desolvation effects, while the favorable enthalpic gains originating from the good size-fit relationship as well as the hydrogen bond interactions between host and guest result in the enhanced molecular/chiral recognition abilities of 2-4 toward (+/-)-borneol.

Topics: Adenine; beta-Cyclodextrins; Calorimetry; Camphanes; Camphor; Circular Dichroism; Magnetic Resonance Spectroscopy; Models, Molecular; Protein Binding; Stereoisomerism; Thermodynamics; Thymine

To study the volatile regularity of menthol and borneol in granule and lozenge at different temperature.. Kinetic method with GC being detection technique.. The volatility of menthol and borneol acts as a pseudo first-order reaction in open system. Under the same condition, the volatile rate of menthol and borneol in granule is four times as fast as that in lozenge, and the volatile rate of borneol is faster than that of menthol.. This study can be applied to improve the quality of lozenges containing menthol or/and borneol.

Topics: beta-Cyclodextrins; Camphanes; Cyclodextrins; Drug Carriers; Drug Stability; Drugs, Chinese Herbal; Menthol; Tablets; Temperature; Volatilization

Topics: Adamantane; Alcohols; beta-Cyclodextrins; Calorimetry; Camphanes; Circular Dichroism; Cyclodextrins; Cyclohexanols; Cyclooctanes; Dimethyl Sulfoxide; HSP70 Heat-Shock Proteins; Models, Chemical; Molecular Chaperones; Molecular Structure; Octanols; Saccharomyces cerevisiae Proteins; Spectrophotometry, Atomic; Stereoisomerism