scholarly journals Physicochemical characterization of zofenopril inclusion complex with hydroxypropyl-β-cyclodextrin

2015 ◽  
Vol 80 (4) ◽  
pp. 485-497 ◽  
Author(s):  
Lucreţia Udrescu ◽  
Laura Sbârcea ◽  
Adriana Fuliaş ◽  
Ionuţ Ledeţi ◽  
Titus Vlase ◽  
...  
Keyword(s):  
Inclusion Complex ◽  
Water Solubility ◽  
Physicochemical Characterization ◽  
Absorption Spectrometry ◽  
Spectroscopic Techniques ◽  
X Ray Diffraction ◽  
Solubility Profile ◽  
Kneading Method ◽  
Fourier Transform Ir ◽  
First Time

Zofenopril calcium (ZOF)is one of the newest angiotensin converting enzyme (ACE) inhibitor, is one of the highly lipophilic newest angiotensin and with low water solubility. This research investigates the interaction between ZOF and a ?-cyclodextrin chemically modified derivative, 2-hydroxypropyl-?-cyclodextrin (HPBCD), in order to prove the formation of an inclusion complex with an enhanced water solubility profile of ZOF. In this research is reported for the first time the physicochemical characterization and the solubility profile of an inclusion complex between ZOF and HPBCD. Different spectroscopic techniques (UV absorption spectrometry, powder X-ray diffraction, attenuated total reflectance Fourier transform IR spectroscopy) were applied in order to prove the formation of the ZOF/HPBCD inclusion complex, both in water and in solid state, backed by thermal analysis (TGA/DTG/HF). The obtained results confirm that the physicochemical properties of the ZOF/HPBCD binary system, prepared using the kneading method, are different in comparison both with the parent substances and the corresponding physical mixture, thus suggesting that an inclusion complex was formed. After the formation of the inclusion complex with HPBCD, the solubility test indicated that the water solubility of ZOF was increased by 5 times.

NMR Studies of the Inclusion Complexes Between Ezetimibe and Cyclodextrins

2018 ◽  
Vol 69 (7) ◽  
pp. 1838-1841
Author(s):  
Hajnal Kelemen ◽  
Angella Csillag ◽  
Bela Noszal ◽  
Gabor Orgovan
Keyword(s):  
Inclusion Complex ◽  
Inclusion Complexes ◽  
Water Solubility ◽  
Solution Nmr ◽  
Spectroscopic Techniques ◽  
Nmr Studies ◽  
The Poor ◽  
Poor Water Solubility

Ezetimibe, the antihyperlipidemic drug of poor bioavailability was complexed with native and derivatized cyclodextrins.The complexes were characterized in terms stability, stoichiometry and structure using various 1D and 2D solution NMR spectroscopic techniques. The complexes were found to be of moderate stability (logK[3). The least stable inclusion complex is formed with b-cyclodextrin, while the ezetimibe-methylated-b--cyclodextrin has a 7-fold higher stability. The results can be useful to improve the poor water-solubility and the concomitant bioavailability of ezetimibe.

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 Physicochemical Characterization of a Diclofenac Sodium-Dual Layer Polyvinyl Alcohol Patch

Polymers ◽  
2021 ◽  
Vol 13 (15) ◽  
pp. 2459
Author(s):  
Shafizah Sa’adon ◽  
Mohamed Nainar Mohamed Ansari ◽  
Saiful Izwan Abd Razak ◽  
Joseph Sahaya Anand ◽  
Nadirul Hasraf Mat Nayan ◽  
...  
Keyword(s):  
Mechanical Properties ◽  
Diclofenac Sodium ◽  
Physicochemical Characterization ◽  
Xrd Analysis ◽  
Tensile Tests ◽  
Spectroscopic Techniques ◽  
X Ray Diffraction ◽  
Water Contact ◽  
Freeze Thaw

The aim of this study is to prepare a dual layer polyvinyl (PVA) patch using a combination of electrospinning techniques and cryogelation (freeze-thaw process) then subsequently to investigate the effect of freeze-thaw cycles, nanofiber thickness, and diclofenac sodium (DS) loading on the physicochemical and mechanical properties and formulation of dual layer PVA patches composed of electrospun PVA nanofibers and PVA cryogel. After the successful preparation of the dual layer PVA patch, the prepared patch was subjected to investigation to assess the effect of freeze-thaw cycles, nanofiber thickness and percentages of DS loading on the morphology, physiochemical and mechanical properties. Various spectroscopic techniques such as scanning electron microscopy (SEM), X-ray diffraction (XRD), Fourier transform infrared (FTIR), water contact angle, and tensile tests were used to evaluate the physicochemical and mechanical properties of prepared dual layer PVA patches. The morphological structures of the dual layer PVA patch demonstrated the effectiveness of both techniques. The effect of freeze-thaw cycles, nanofiber thickness, and DS percentage loading on the crystallinity of a dual layer PVA patch was investigated using XRD analysis. The presence of a distinct DS peak in the FTIR spectrum indicates the compatibility of DS in a dual layer PVA patch through in-situ loading. All prepared patches were considered highly hydrophilic because the data obtained was less than 90°. The increasing saturation of DS within the PVA matrix increases the tensile strength of prepared patches, however decreased its elasticity. Evidently, the increasing of electrospun PVA nanofibers thickness, freeze-thaw cycles, and the DS saturation has improved the physicochemical and mechanical properties of the DS medicated dual layer PVA patches, making them a promising biomaterial for transdermal drug delivery applications.

Physicochemical Characterization of the Inclusion Complex of Diosmetin with Hydroxypropyl-β-Cyclodextrin

2013 ◽  
Vol 295-298 ◽  
pp. 298-302
Author(s):  
Yan Zhang ◽  
Korbanjhon Brad
Keyword(s):  
Differential Scanning Calorimetry ◽  
Inclusion Complex ◽  
Physicochemical Properties ◽  
Water Solubility ◽  
Physicochemical Characterization ◽  
Infrared Spectrometry ◽  
Scanning Calorimetry ◽  
Covalent Bonds ◽  
X Ray

In this study, the inclusion complex of diosmetin with hydroxypropyl-β- -cyclodextrin (HP-β-CD) was prepared to improve the water solubility of diosmetin by the solvent method. The content of diosmetin in the complex was determined by UV. And the physicochemical properties of the complex were analyzed by ultraviolet-visible spectrometry (UV), infrared spectrometry (IR), X-ray diffractometry (XRD), differential scanning calorimetry (DSC). The results showed that the physical phase of diosmetin had been changed. It was completely dispersed in HP-β-CD. HP-β-CD and diosmetin were combined by non-covalent bonds.

scholarly journals Physicochemical Characterization and Antioxidant Activity Evaluation of Idebenone/Hydroxypropyl-β-Cyclodextrin Inclusion Complex †

Biomolecules ◽  
2019 ◽  
Vol 9 (10) ◽  
pp. 531 ◽  
Author(s):  
Valentina Venuti ◽  
Vincenza Crupi ◽  
Barbara Fazio ◽  
Domenico Majolino ◽  
Giuseppe Acri ◽  
...  
Keyword(s):  
Fourier Transform ◽  
Inclusion Complex ◽  
Water Solubility ◽  
Ex Vivo ◽  
Morphological Changes ◽  
Physicochemical Characterization ◽  
Infrared Light ◽  
Phase Solubility ◽  
Theoretical Approaches

Idebenone (IDE) is an antioxidant drug active at the level of the central nervous system (CNS), whose poor water solubility limits its clinical application. An IDE/2-hydroxypropyl-β-cyclodextrin (IDE/HP-β-CD) inclusion complex was investigated by combining experimental methods and theoretical approaches. Furthermore, biological in vitro/ex vivo assays were performed. Phase solubility studies showed an AL type diagram, suggesting the presence of a 1:1 complex with high solubility. Scanning electron microscopy (SEM) allowed us to detect the morphological changes upon complexation. The intermolecular interactions stabilizing the inclusion complex were experimentally characterized by exploring the complementarity of Fourier-transform infrared spectroscopy in attenuated total reflectance geometry (FTIR-ATR) with mid-infrared light, Fourier-transform near-infrared (FT-NIR) spectroscopy, and Raman spectroscopy. From the temperature evolution of the O–H stretching band of the complex, the average enthalpy ΔHHB of the hydrogen bond scheme upon inclusion was obtained. Two-dimensional (2D) rotating frame Overhauser effect spectroscopy (ROESY) analysis and computational studies involving molecular modeling and molecular dynamics (MD) simulation demonstrated the inclusion of the quinone ring of IDE inside the CD ring. In vitro/ex vivo studies evidenced that complexation produces a protective effect of IDE against the H2O2-induced damage on human glioblastoma astrocytoma (U373) cells and increases IDE permeation through the excised bovine nasal mucosa.

scholarly journals Synthesis of Two Novel Azilsartan Cocrystals: Preparation, Physicochemical Characterization and Solubility Studies

Crystals ◽  
2020 ◽  
Vol 10 (9) ◽  
pp. 739
Author(s):  
Lei Gao ◽  
Xian-Rui Zhang
Keyword(s):  
Water Solubility ◽  
Physicochemical Characterization ◽  
Dimensional Structure ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
One Dimensional ◽  
X Ray ◽  
Solubility Study ◽  
Solution Crystallization

Azilsartan is a novel angiotension II receptor blocker primarily used to treat high blood pressure. This is not a formulation-friendly molecule largely due to the inherent water-solubility pitfalls. In this paper, two novel cocrystals of azilsartan (AZ) were studied (AZ-BIP, AZ-BPE; BIP = 4,4′-bipyridine, BPE = trans-1,2-bis (4-pyridyl) ethylene) by solution crystallization. The structures of these two cocrystals were characterized by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA), including the single-crystal structure determination of AZ-BIP and AZ-BPE. In the cocrystals AZ-BIP (2:1) and AZ-BPE (2:1), two AZ molecules and one coformer formed a sandwich structure through N-H…N interactions. These sandwich structures were extended into a one-dimensional structure through O-H…N hydrogen bonds. The equilibrium solubility study demonstrated that the AZ-BIP and AZ-BPE cocrystals both showed higher solubility than azilsartan in water.

scholarly journals Mechanochemical Synthesis and Physicochemical Characterization of Previously Unreported Praziquantel Solvates with 2-Pyrrolidone and Acetic Acid

Pharmaceutics ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 1606
Author(s):  
Debora Zanolla ◽  
Lara Gigli ◽  
Dritan Hasa ◽  
Michele R. Chierotti ◽  
Mihails Arhangelskis ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Water Solubility ◽  
Physicochemical Characterization ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Pxrd Pattern ◽  
Intrinsic Dissolution ◽  
Ft Ir ◽  
Biopharmaceutical Properties

Two new solvates of the widely used anthelminthic Praziquantel (PZQ) were obtained through mechanochemical screening with different liquid additives. Specifically, 2-pyrrolidone and acetic acid gave solvates with 1:1 stoichiometry (PZQ-AA and PZQ-2P, respectively). A wide-ranging characterization of the new solid forms was carried out by means of powder X-ray diffraction, differential scanning calorimetry, FT-IR, solid-state NMR and biopharmaceutical analyses (solubility and intrinsic dissolution studies). Besides, the crystal structures of the two new solvates were solved from their Synchrotron-PXRD pattern: the solvates are isostructural, with equivalent triclinic packing. In both structures acetic acid and 2-pyrrolidone showed a strong interaction with the PZQ molecule via hydrogen bond. Even though previous studies have shown that PZQ is conformationally flexible, the same syn conformation as the PZQ Form A of the C=O groups of the piperazinone-cyclohexylcarbonyl segment is involved in these two new solid forms. In terms of biopharmaceutical properties, PZQ-AA and PZQ-2P exhibited water solubility and intrinsic dissolution rate much greater than those of anhydrous Form A.

scholarly journals Extraction and Physicochemical Characterization of Chitin from Cicada orni Sloughs of the South-Eastern French Mediterranean Basin

Molecules ◽  
2020 ◽  
Vol 25 (11) ◽  
pp. 2543 ◽  
Author(s):  
Aurelia Poerio ◽  
Chloé Petit ◽  
Jean-Philippe Jehl ◽  
Elmira Arab-Tehrany ◽  
João F. Mano ◽  
...  
Keyword(s):  
Mediterranean Basin ◽  
Physicochemical Characterization ◽  
Extraction Process ◽  
X Ray Diffraction ◽  
The South ◽  
South Eastern ◽  
Degree Of Acetylation ◽  
High Degree ◽  
Promising Source ◽  
First Time

Chitin is a structural polysaccharide of the cell walls of fungi and exoskeletons of insects and crustaceans. In this study, chitin was extracted, for the first time in our knowledge, from the Cicada orni sloughs of the south-eastern French Mediterranean basin by treatment with 1 M HCl for demineralization, 1 M NaOH for deproteinization, and 1% NaClO for decolorization. The different steps of extraction were investigated by Fourier Transform Infrared Spectroscopy (FTIR), X-ray Diffraction (XRD), Thermogravimetric Analysis (TGA), and Scanning Electron Microscopy (SEM). Results demonstrated that the extraction process was efficiently performed and that Cicada orni sloughs of the south-eastern French Mediterranean basin have a high content of chitin (42.8%) in the α-form with a high degree of acetylation of 96% ± 3.4%. These results make Cicada orni of the south-eastern French Mediterranean basin a new and promising source of chitin. Furthermore, we showed that each step of the extraction present specific characteristics (for example FTIR and XRD spectra and, consequently, distinct absorbance peaks and values of crystallinity as well as defined values of maximum degradation temperatures identifiable by TGA analysis) that could be used to verify the effectiveness of the treatments, and could be favorably compared with other natural chitin sources.

Novel Structure of Fullerenes and Endohedral Fullerenes

2003 ◽  
Vol 775 ◽  
Author(s):  
Chun-Ru Wang ◽  
Chun-Li Bai ◽  
Hisanori Shinohara
Keyword(s):  
Molecular Magnet ◽  
Spectroscopic Techniques ◽  
Hplc Separation ◽  
X Ray Diffraction ◽  
Endohedral Fullerenes ◽  
X Ray ◽  
Metal Atoms ◽  
Novel Structure ◽  
First Time ◽  
Novel Structures

AbstractBy using Krätschmer-Huffman synthesis and HPLC separation method we have isolated a series of novel fullerenes and endohedral fullerenes. Various spectroscopic techniques, e.g., MS, NMR, UV-vis-NIR, TEM, X-ray diffraction spectrometry etc., were adopted to characterize the isolated fullerenes. Several fullerenes were revealed to hold novel structures and electronic properties. For examples, C80(D5d) was isolated and characterized to have an ellipsoidal structure which is in fact one of the shortest SW-nanotubes; The isolation of Sc2@C66 breaks the well-known isolated-pentagon-rule (IPR) for the first time, which shows that the unconventional fullerenes may be dramatically stabilized through encaging metal atoms; Sc2C2@C84 is a novel molecular endohedral fullerene in which the Sc2C2 cluster rotates rapidly along the main C2 axis of C84(D2d). This fullerene is predicted to be a molecular magnet and may be used as nano-switcher in electronics.

Influence of pH on the DSSC Performance of Template Assisted SnO2 Nanostructures

2021 ◽  
Author(s):  
vasanthapriya R ◽  
NEELAKANDESWARI N ◽  
K. Uthayarani ◽  
M. Chitra
Keyword(s):  
Tin Oxide ◽  
Dye Sensitized Solar Cells ◽  
Spectroscopic Techniques ◽  
Sno2 Nanostructures ◽  
X Ray Diffraction ◽  
Oxide Nanostructures ◽  
Current Voltage ◽  
Tin Oxide Nanoparticles ◽  
First Time ◽  
Sensitized Solar Cells

Abstract This paper reports the performance of alizarin based SnO2 dye-sensitized solar cells. A novel template assisted method has been applied for the preparation of tin oxide nanoparticles. For the first time, onion (Allium cepa) was used as a template for the synthesis of tin oxide nanostructures at different pH values. Tin oxide nanostructures were used for the photoanode preparation. A sandwich cell was prepared by using the dye soaked SnO2 film as a photoanode and platinum as a counter electrode. The structural, morphological and optical properties of the nanoparticles were studied using powder X-ray diffraction (XRD), Scanning Electron microscope (SEM), Photoluminescence (PL), Attenuated Total Reflectance (ATR) spectra and UV-visible spectroscopic techniques. Current-voltage (I-V) characteristics have been measured using electrochemical workstation under the presence of solar illumination. Characteristic parameters of the fabricated cell were determined on the basis of the measured I-V curves.

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