1 H NMR of compounds with low water solubility in the presence of erythrocytes: effects of emulsion phase separation

2001 ◽  
Vol 30 (1) ◽  
pp. 69-74 ◽  
Author(s):  
Poul Erik Hansen ◽  
Ulrik Skibsted ◽  
Jan Nissen ◽  
Caroline D. Rae ◽  
Philip W. Kuchel

2020 ◽  
Vol 17 ◽  
Author(s):  
Mas Amira Idayu Abdul Razak ◽  
Haslinda Abdul Hamid ◽  
Raja Nor Izawati Raja Othman ◽  
Shaik Alaudeen Mohd Moktar ◽  
Azizi Miskon

Introduction: Bioconjugations are swiftly progressing and are being applied to solve several limitations of conventional drug delivery systems (DDS) such as lack of water solubility, non-specific, and poor bioavailability. The main goals of DDS are to achieve greater drug effectiveness and minimize toxicity to the healthy tissues. Objectives: In this study, D-glucose was conjugated with eugenol to target the cancer cells. To identify the implication of the anticancer effect, osteosarcoma (K7M2) cells were cultured and the anti-proliferative effect was performed using MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay] test in order to evaluate the viability and toxicity on cells with various concentrations of eugenol and D-glucose-eugenol conjugate in 24-hour incubation. Results: It was found that, the successful confirmation of the conjugation between D-glucose and eugenol was obtained by 1 H NMR spectroscopy. MTT assay showed inhibitory concentration (IC50 value) of D-glucose-eugenol was at 96.2 µg/ml and the decreased of osteosarcoma cell survival was 48%. Conclusion: These findings strongly indicate that K7M2 cells would be affected by toxicity of D-glucose-eugenol. Therefore, the present study suggests that D-glucose-eugenol has high potential to act as an anti-proliferative agent who may promise a new modality or approach as the drug delivery treatment for cancer or chemotherapeutic agent.



2013 ◽  
Vol 34 (12) ◽  
pp. NA-NA ◽  
Author(s):  
Yung-Sheng Lin ◽  
Wei-Lung Chou ◽  
Chih-Hui Yang ◽  
Keng-Shiang Huang ◽  
Eng-Chi Wang ◽  
...  


2010 ◽  
Vol 10 (16) ◽  
pp. 7795-7820 ◽  
Author(s):  
A. Zuend ◽  
C. Marcolli ◽  
T. Peter ◽  
J. H. Seinfeld

Abstract. Semivolatile organic and inorganic aerosol species partition between the gas and aerosol particle phases to maintain thermodynamic equilibrium. Liquid-liquid phase separation into an organic-rich and an aqueous electrolyte phase can occur in the aerosol as a result of the salting-out effect. Such liquid-liquid equilibria (LLE) affect the gas/particle partitioning of the different semivolatile compounds and might significantly alter both particle mass and composition as compared to a one-phase particle. We present a new liquid-liquid equilibrium and gas/particle partitioning model, using as a basis the group-contribution model AIOMFAC (Zuend et al., 2008). This model allows the reliable computation of the liquid-liquid coexistence curve (binodal), corresponding tie-lines, the limit of stability/metastability (spinodal), and further thermodynamic properties of multicomponent systems. Calculations for ternary and multicomponent alcohol/polyol-water-salt mixtures suggest that LLE are a prevalent feature of organic-inorganic aerosol systems. A six-component polyol-water-ammonium sulphate system is used to simulate effects of relative humidity (RH) and the presence of liquid-liquid phase separation on the gas/particle partitioning. RH, salt concentration, and hydrophilicity (water-solubility) are identified as key features in defining the region of a miscibility gap and govern the extent to which compound partitioning is affected by changes in RH. The model predicts that liquid-liquid phase separation can lead to either an increase or decrease in total particulate mass, depending on the overall composition of a system and the particle water content, which is related to the hydrophilicity of the different organic and inorganic compounds. Neglecting non-ideality and liquid-liquid phase separations by assuming an ideal mixture leads to an overestimation of the total particulate mass by up to 30% for the composition and RH range considered in the six-component system simulation. For simplified partitioning parametrizations, we suggest a modified definition of the effective saturation concentration, Cj*, by including water and other inorganics in the absorbing phase. Such a Cj* definition reduces the RH-dependency of the gas/particle partitioning of semivolatile organics in organic-inorganic aerosols by an order of magnitude as compared to the currently accepted definition, which considers the organic species only.



2021 ◽  
Author(s):  
Feijie Liu ◽  
Zhimin Xue ◽  
Xue Lan ◽  
Zhenghui Liu ◽  
Tiancheng Mu

CO2 switchable imidazole-based deep eutectic solvents (DESs) were formed and used for reversible phase separation of emulsions generated between DESs and oil.



2017 ◽  
Vol 2017 ◽  
pp. 1-9 ◽  
Author(s):  
E. Manuela Garrido ◽  
Daniela Rodrigues ◽  
Nuno Milhazes ◽  
Fernanda Borges ◽  
Jorge Garrido

The herbicide terbuthylazine (TBA) is widely used for preemergence or postemergence control of many grass and broadleaf weeds and has, besides other issues, a poor aqueous solubility profile that results in reduced bioavailability. Cyclodextrins and modified cyclodextrins were considered, among other substances, appropriate agents for improving pesticide water solubility. Therefore, the inclusion complex formation of terbuthylazine withβ-cyclodextrin (β-CD) and hydroxypropyl-β-cyclodextrin (HP-β-CD) was studied to attain its aqueous solubility enhancement. Their characterization was accomplished with different analytical techniques, namely, by UV-Vis, DSC, FTIR, and1H NMR. From the analysis of the complexation performance of the herbicide it was concluded that the interaction of terbuthylazine with CDs leads to the formation of inclusion complexes with a stoichiometry of 1 : 1. The association constants of the TBA/β-CD and TBA/HP-β-CD complexes were determined by UV. The mean values obtained for the stability constants are 460.4 ± 26.5 and 532.1 ± 27.6 to TBA/β-CD and TBA/HP-β-CD, respectively.1H NMR data corroborate the formation of the TBA/β-CD and TBA/HP-β-CD complexes synthesized by the kneading method. A formulation incorporating TBA cyclodextrin complexes might lead to an improvement in terbuthylazine bioavailability. The development of TBA-CD formulations may be interesting since it would enable, through their inclusion into the hydrophobic cavity of CDs, enhancement of solubility, bioavailability, and stability of the herbicide.



1994 ◽  
Vol 32 (S1) ◽  
pp. S3-S7 ◽  
Author(s):  
M. Wilhelm ◽  
S. Lehmann ◽  
C. Jäger ◽  
H. W. Spiess ◽  
R. Jerome
Keyword(s):  


2020 ◽  
Author(s):  
Anderson Fiamingo ◽  
Sergio Paulo Campana Filho ◽  
Osvaldo Novais Oliveira Junior

<p>The preparation of chitosans soluble in physiological conditions has been sought for years, but so far solubility in non-acidic aqueous media has only been achieved at the expense of lowering chitosan molecular weight. In this work, we applied the multistep ultrasound-assisted deacetylation process (USAD process) to β-chitin and obtained extensively deacetylated chitosans with high molecular weights (Mw ≥ 1,000,000 g mol<sup>-1</sup>). The homogeneous <i>N</i>-acetylation of a chitosan sample resulting from three consecutive USAD procedures allowed us to produce chitosans with a high weight average degree of polymerization (DPw ≈ 6,000) and tunable degrees of acetylation (DA from 5 to 80%). <i>N</i>-acetylation was carried out under mild conditions to minimize depolymerization, while preserving a predominantly random distribution of 2-amino-2-deoxy-D-glucopyanose (<i>GlcN</i>) and 2-acetamido-2-deoxy-D-glucopyanose (<i>GlcNAc</i>) units. This close to random distribution, inferred with deconvolution of nuclear magnetic resonance (<sup>1</sup>H NMR) spectra, is considered as responsible for the solubility within a wide pH range. Two of the highly <i>N</i>-acetylated chitosans (DA ≈ 60 % and ≈ 70 %) exhibited full water solubility even at neutral pH, which can expand the biomedical applications of chitosans. </p>



2020 ◽  
Vol 18 (4) ◽  
pp. 80
Author(s):  
L.A. Kovaleva ◽  
R.R. Zinnatullin ◽  
R.F. Sultanguzhin ◽  
A.F. Gabdrafikov ◽  
E.F. Gainetdinov ◽  
...  


2019 ◽  
Vol 2019 ◽  
pp. 1-6
Author(s):  
Bing Ren Tian ◽  
Jia Yue Liu ◽  
Hu Rong Ge ◽  
Zhi Zhong Wang ◽  
Shao Yun Huang ◽  
...  

A novel series of resveratrol modified by γ-aminobutyric acid esters were designed and synthesized. Then, the products were characterized by 1H-NMR, 13C-NMR, and MS, and the melting point was determined. Molecular water solubility, polar surface area, and octanol-water partition were calculated, which correlated well with molecular transport through membranes and, therefore, enabled prediction of transport properties of drugs.



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