scholarly journals Improvement of Water Solubility of Josamycin by Inclusion Complex with -Cyclodextrin

2012 ◽  
Vol 2012 ◽  
pp. 1-6 ◽  
Author(s):  
J. El Harti ◽  
Y. Cherrah ◽  
A. Bouklouze
Keyword(s):  
Inclusion Complex ◽  
Water Solubility ◽  
Inclusion Complexation ◽  
Infrared Spectrometry ◽  
Resonance Spectroscopy ◽  
Phase Solubility ◽  
X Ray Diffraction ◽  
The Family ◽  
The Stability ◽  
Low Solubility

Josamycin propionate (JMP) is an antibiotic belonging to the family of macrolide. According to the Biopharmaceutical Classification System (BCS), this compound can be classed in class II, low solubility and high permeability. In order to increase its apparent water solubility, inclusion complexation between Josamycin propionate and γ-cyclodextrin (γ-CD) was studied. UV spectrophotometric method was employed to investigate the phase-solubility profile and the stability constant of the complexation in aqueous medium. Solid state of the binary system prepared by coevaporation (in 50%-50% ethanol/water) has been characterized using powder X-ray diffraction (XRD) and Fourier transformation-infrared spectrometry (FTIR). These techniques indicate that JMP forms an association complex with γ-CD. The shift in the nuclear magnetic resonance spectroscopy (1H NMR) confirms the existence of the inclusion complex. Also the results obtained showed an enhancement of the solubility in water of Josamycin propionate.

scholarly journals Preparation and Characterization of Functional Films Based on Chitosan and Corn Starch Incorporated Tea Polyphenols

Coatings ◽  
2021 ◽  
Vol 11 (7) ◽  
pp. 817
Author(s):  
Lepeng Gao ◽  
Tao Zhu ◽  
Fuyang He ◽  
Zhiqiang Ou ◽  
Jian Xu ◽  
...  
Keyword(s):  
Moisture Content ◽  
Water Solubility ◽  
Corn Starch ◽  
Morphological Characteristics ◽  
Tea Polyphenols ◽  
Infrared Spectrometry ◽  
X Ray Diffraction ◽  
Blend Films ◽  
The Stability ◽  
Water Swelling

The functional films based on chitosan and corn starch incorporated tea polyphenols were developed through mixing the chitosan and starch solution and the powder of tea polyphenols by the casting method. The objective of this research was to investigate the effect of different concentrations of tea polyphenols on the functional properties of the films. Attenuated total reflectance Fourier transform infrared spectrometry and X-ray diffraction were used to investigate the potential interactions among chitosan, corn starch and tea polyphenols in the blend films. Physical properties of the blend films, including density, moisture content, opacity, color, water solubility and water swelling, as well as morphological characteristics, were measured. The results demonstrated that the incorporation of tea polyphenols caused the blend films to lead to a darker appearance. The water solubility of the blend film increased with the increase of tea polyphenol concentrations, while moisture content and swelling degree decreased. The hydrogen bonding between chitosan, starch and tea polyphenols restricted the movement of molecular chains and was helpful to the stability of the blend films. The results suggested that these biodegradable blend films could potentially be used as packaging films for the food and drug industries to extend the shelf life to maintain their quality and safety.

Preparation and Characterization of a Novel Flame Retardant

2008 ◽  
Vol 47-50 ◽  
pp. 294-297 ◽  
Author(s):  
Xiu Wei Jia ◽  
Min Zhi Rong ◽  
Ming Qiu Zhang
Keyword(s):  
Flame Retardant ◽  
Sol Gel ◽  
Average Molecular Weight ◽  
Regular Structure ◽  
Gel Permeation Chromatography ◽  
Helical Conformation ◽  
Infrared Spectrometry ◽  
Resonance Spectroscopy ◽  
X Ray Diffraction

A novel flame retardant polymethylsilsesquioxane (PMSQ) was successfully obtained via combination of non-hydrolytic and hydrolytic sol-gel routes. Chemical structure of the resultant PMSQ was determined by nuclear magnetic resonance spectroscopy, Fourier-transform infrared spectrometry and powder X-ray diffraction, respectively. All the measurements demonstrated that the product possessed regular structure with chain-to-chain width of 0.87nm and chain thickness of 0.40nm. Weight average molecular weight of PMSQ was measured to be 3.5×105 using gel permeation chromatography. Numerical simulations of the molecular structure suggested that PMSQ should exhibit cis-isotactic configuration and double helical conformation at undisturbed condition.

scholarly journals Preparation, Characterization, and Bioavailability of Host-Guest Inclusion Complex of Ginsenoside Re with Gamma-Cyclodextrin

Molecules ◽  
2021 ◽  
Vol 26 (23) ◽  
pp. 7227
Author(s):  
Hui Li ◽  
Guolei Zhang ◽  
Wei Wang ◽  
Changbao Chen ◽  
Lili Jiao ◽  
...  
Keyword(s):  
Inclusion Complex ◽  
Water Solubility ◽  
Area Under The Curve ◽  
Relative Bioavailability ◽  
Docking Studies ◽  
Solubility Parameters ◽  
Phase Solubility ◽  
Scanning Calorimetry ◽  
Ginsenoside Re

This work aimed at improving the water solubility of Ginsenoside (G)-Re by forming an inclusion complex. The solubility parameters of G-Re in alpha (α), beta (β), and gamma (γ) cyclodextrin (CD) were investigated. The phase solubility profiles were all classified as AL-type that indicated the 1:1 stoichiometric relationship with the stability constants Ks which were 22 M−1 (α-CD), 612 M−1 (β-CD), and 14,410 M−1 (γ-CD), respectively. Molecular docking studies confirmed the results of phase solubility with the binding energy of −4.7 (α-CD), −5.10 (β-CD), and −6.70 (γ-CD) kcal/mol, respectively. The inclusion complex (IC) of G-Re was prepared with γ-CD via the water-stirring method followed by freeze-drying. The successful preparation of IC was confirmed by powder X-ray diffraction (XRD), Fourier transform-infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), and scanning electron microscopy (SEM). In-vivo absorption studies were carried out by LC-MS/MS. Dissolution rate of G-Re was increased 9.27 times after inclusion, and the peak blood concentration was 2.7-fold higher than that of pure G-Re powder. The relative bioavailability calculated from the ratio of Area under the curve AUC0–∞ of the inclusion to pure G-Re powder was 171%. This study offers the first report that describes G-Re’s inclusion into γ-CD, and explored the inclusion complex’s mechanism at the molecular level. The results indicated that the solubility could be significantly improved as well as the bioavailability, implying γ-CD was a very suitable inclusion host for complex preparation of G-Re.

Evaluation of the phase solubility of inclusion complexes of diisopropylphenol (INN) with hydroxypropyl-β-cyclodextrin

2021 ◽  
pp. 27-32
Author(s):  
Olga Mikhailovna Balakhonova ◽  
Viktoriya Sergeevna Tyukova ◽  
Stanislav Anatolievich Kedik
Keyword(s):  
Aqueous Solution ◽  
Inclusion Complex ◽  
Inclusion Complexes ◽  
Tween 80 ◽  
Phase Solubility ◽  
Cyclodextrin Inclusion ◽  
Solubility Method ◽  
Cyclodextrin Inclusion Complex ◽  
The Stability ◽  
Solubility Profiles

The paper presents the results of a study of the stability of aqueous solutions of inclusion complexes of hydroxypropyl-β-cyclodextrin with diisopropylphenol in various systems by the Higuchi-Connors phase solubility method. The phase solubility profiles for each system corresponding to the AN type are determined graphically, and the stability constants of the resulting inclusion complexes are calculated. An aqueous solution containing 0.2 % Tween 80 and 0.2 % mannitol was selected as the optimal condition for obtaining the hydroxypropyl-β-cyclodextrin inclusion complex with diisopropylphenol.

scholarly journals Enhanced Solubility, Stability, and Herbicidal Activity of the Herbicide Diuron by Complex Formation with β-Cyclodextrin

Polymers ◽  
2019 ◽  
Vol 11 (9) ◽  
pp. 1396 ◽  
Author(s):  
Shuang Gao ◽  
Jing-Yu Jiang ◽  
Yan-Yan Liu ◽  
Ying Fu ◽  
Li-Xia Zhao ◽  
...  
Keyword(s):  
Inclusion Complex ◽  
1H Nmr ◽  
Water Solubility ◽  
Herbicidal Activity ◽  
Environmental Damage ◽  
Phase Solubility ◽  
Scanning Calorimetry ◽  
Enhanced Solubility ◽  
Phase Solubility Study ◽  
Herbicide Diuron

The herbicide diuron is hardly soluble in water and most organic solvents and is usually made into a wettable powder or mixed with soil when used, which causes environmental risk and a reduction in herbicidal efficacy. In this study, the physicochemical properties were changed by using β-cyclodextrin (β-CD) to encapsulate diuron to form an inclusion complex. Some key technologies, including X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and nuclear magnetic resonance (1H NMR), were used to characterize the inclusion complex. The stoichiometry of the inclusion complex was determined by recording the 1H NMR spectrum or by using a diagram of inclusion ratios. A phase solubility study proved that the formed inclusion complex exhibited higher water solubility. Thermogravimetric analysis (TGA) demonstrated that the formed inclusion complex exhibited better thermal stability. Biological activity studies indicated that the herbicidal activity, in terms of herbicide removal, of the formed inclusion complex was higher than that of the original diuron. In general, the formation of the inclusion complex could reduce the environmental damage caused by diuron and enhance its herbicidal activity, providing an environmentally friendly method for using diuron.

scholarly journals Functional Supramolecular of Inclusion Complex of Herbicide Fluroxypyr with HPβCD

Polymers ◽  
2018 ◽  
Vol 10 (12) ◽  
pp. 1294 ◽  
Author(s):  
Shuang Gao ◽  
Chao Bie ◽  
Yanyan Liu ◽  
Tianyu Zhang ◽  
Ying Fu ◽  
...  
Keyword(s):  
Thermal Stability ◽  
Inclusion Complex ◽  
Solution Method ◽  
Water Solubility ◽  
Herbicidal Activity ◽  
Saturated Solution ◽  
Phase Solubility ◽  
Bioactivity Assay ◽  
Ft Ir ◽  
Tga Analysis

In this study, hydroxypropyl-β-cyclodextrin (HPβCD) was used to form an inclusion complex with fluroxypyr to enhance water solubility and thermal stability. The inclusion complex was prepared by a saturated solution method and characterized by FT-IR, SEM, TGA, and XRD. All results indicated that fluroxypyr successfully entered the HPβCD cavity. In addition, the study of phase solubility identifies that the water solubility of fluroxypyr was greatly improved after the formation of the inclusion complex, and TGA analysis suggested that the formation of the inclusion complex improved the thermal stability. Bioactivity assay tests showed that the inclusion complex still had strong herbicidal activity. Our research showed that HPβCD was a promising carrier for improving the properties of fluroxypyr and, thus, expanding its use in agrochemical formulations.

scholarly journals Encapsulation of l-menthol in hydroxypropyl-β-cyclodextrin and release characteristics of the inclusion complex

2016 ◽  
Vol 18 (3) ◽  
pp. 110-116 ◽  
Author(s):  
Guangyong Zhu ◽  
Zuobing Xiao ◽  
Guangxu Zhu ◽  
Yunwei Niu ◽  
Keyword(s):  
Inclusion Complex ◽  
Preexponential Factor ◽  
Binding Energies ◽  
Stable Complex ◽  
X Ray Diffraction ◽  
Molecular Mechanics Calculations ◽  
Cyclodextrin Inclusion Complexes ◽  
Cyclodextrin Inclusion ◽  
High Volatility ◽  
The Stability

Abstract l-menthol has been widely used in flavour, food and pharmaceuticals. Because of its high volatility and whisker growth, l-menthol-hydroxypropyl-β-cyclodextrin inclusion complex was produced to improve shelf-life, provide protection, and enhance the stability of l-menthol. The inclusion complex was characterized by Fourier transform infrared spectroscopy, X-ray diffraction. The results show that l-menthol was successfully encapsulated in hydroxypropyl-β-cyclodextrin. l-menthol loading capacity is about 8.44%. Geometries and binding energies of l-menthol-hydroxypropyl-β-cyclodextrin inclusion complexes were investigated using molecular mechanics calculations. The shape and orientation of the most stable complex, and the minimum binding energy were determined. L-menthol release from complex was determined by thermogravimetric analysis. Two l-menthol release rate peaks were observed at 69.3 and 279.1°C. The l-menthol release reaction order, release activation energy and the preexponential factor were obtained.

Polypseudorotaxane Hydrogels Based on F127 Block-Selected Inclusion Complexation with α-Cyclodextrin

2012 ◽  
Vol 482-484 ◽  
pp. 1898-1903
Author(s):  
Ying Xue Zhou ◽  
Xiao Dong Fan ◽  
Dan Xue
Keyword(s):  
Thermal Stability ◽  
Inclusion Complex ◽  
Inclusion Complexation ◽  
Wide Angle ◽  
Acryloyl Chloride ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Thermal Stability Of ◽  
Channel Type

Supramolecular hydrogels were formed through F127, acryloyl chloride modified F127 inclusion complex with α-cyclodextrin, respectively. The structure of modified copolymers and inclusion complex was characterized by Fourier transform infrared spectroscopy (FTIR) and hydrogen nuclear magnetic resonance (1H-NMR). Hydrogels formed from supramolecular inclusion are imparted channel-type structure investigated by wide angle x-ray diffraction (WAXRD). Differential scanning calorimetry (DSC) and TG experiments showed that thermal stability of hydrogels depend on the nature of axis polymer. The relative model was proposed to elucidate the inclusion complexes and hydrogels formation.

Host–Guest Inclusion System of Luteolin with Polyamine-β-cyclodextrin: Preparation, Characterisation, Anti-oxidant and Anti-cancer Activity

2016 ◽  
Vol 69 (2) ◽  
pp. 174 ◽  
Author(s):  
Manshuo Liu ◽  
Rongqiang Liao ◽  
Yulin Zhao ◽  
Bo Yang
Keyword(s):  
Water Solubility ◽  
Inclusion Complexation ◽  
2D Nmr ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
2D Nmr Spectroscopy ◽  
Binding Ability ◽  
Anti Cancer ◽  
Anti Oxidant ◽  
Cancer Activity

The characterisation, inclusion complexation behaviours, and binding ability of inclusion complexes of luteolin (LU) with four polyamine-modified β-cyclodextrins (NH2-βCD, EN-βCD, DETA-βCD, TETA-βCD; where EN = ethylenediamine; DETA = diethylenediamine; TETA = triethylenetetramine) were investigated in both the solid and solution forms by photoluminescence spectroscopy, 1H and 2D NMR spectroscopy, differential scanning calorimetry, X-ray diffraction, and scanning electron microscopy. The results showed that the water solubility, and the anti-oxidant activity and anti-cancer activity of LU were significantly increased in the inclusion complex with polyamine-β-cyclodextrin. The LU/CDs complex will be useful for its application as herbal medicine or healthcare product.

scholarly journals Physicochemical Characterization and Cyclodextrin Complexation of the Anticancer Drug Lapatinib

2017 ◽  
Vol 2017 ◽  
pp. 1-9 ◽  
Author(s):  
Gergő Tóth ◽  
Ádám Jánoska ◽  
Gergely Völgyi ◽  
Zoltán-István Szabó ◽  
Gábor Orgován ◽  
...  
Keyword(s):  
Water Solubility ◽  
Kinase Inhibitor ◽  
Structural Information ◽  
Uv Spectroscopy ◽  
Physicochemical Characterization ◽  
Drug Formulation ◽  
Variation Method ◽  
Phase Solubility ◽  
Inhibitor Drug ◽  
The Stability

Lapatinib (LAP), the tyrosine kinase inhibitor drug with moderate bioavailability, was characterized in terms of physicochemical properties: acid-base characteristics, lipophilicity, and solubility. The highly lipophilic nature of the drug and its extremely low water solubility (S0=0.82 nM) limit the development of a parenteral formulation. In order to enhance solubility and bioavailability, inclusion complex formation with cyclodextrins (CDs) is a promising method of choice. Therefore, LAP-CD interactions were also studied by a multianalytical approach. The stability constants of LAP with native cyclodextrins, determined by UV spectroscopy, identified the seven-membered β-CD as the most suitable host. Continuous variation method (Job’s plot) by 1H NMR showed a 1 : 1 stoichiometry for the complexes. The geometry of the complex was elucidated by 2D ROESY NMR measurements and molecular modeling, indicating that the partial molecular encapsulation includes the fluorophenyl ring of LAP. Phase-solubility studies with four CDs, β-CD, (2-hydroxypropyl)-β-cyclodextrin (HP-β-CD), randomly methylated-β- (RAMEB-) cyclodextrin, and sulfobutylether-β-cyclodextrin (SBE-β-CD), show an AL type diagram and highly increased solubility via CD complexation. The results are especially promising with SBE-β-CD, exerting more than 600-fold gain in solubility. The equilibrium and structural information presented herein can offer the molecular basis for an improved drug formulation with enhanced bioavailability.

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