scholarly journals Evaluation of Antioxidant Ability In Vitro and Bioavailability oftrans-Cinnamic Acid Nanoparticle by Liquid Antisolvent Precipitate

2016 ◽  
Vol 2016 ◽  
pp. 1-11 ◽  
Author(s):  
Wengang Li ◽  
Xiuhua Zhao ◽  
Xiaoli Sun ◽  
Yuangang Zu ◽  
Ying Liu ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Water Solubility ◽  
Hydroxypropyl Methylcellulose ◽  
Food Additives ◽  
Volume Ratio ◽  
Solution Concentration ◽  
Ethanol Solution ◽  
Preparation Conditions ◽  
Ft Ir

TCD is a kind of organic acid that is isolated from cinnamon bark or benzoin. TCD has significant antioxidant activity and is widely used in pharmaceutical, cosmetic, and food additives. But TCD has shortcomings of low bioavailability due to poor water solubility. Therefore, we use ethanol as a solvent, deionized water as antisolvent, and hydroxypropyl methylcellulose (HPMC) as the surfactant to prepare TCD nanoparticle powder. The optimum preparation conditions were determined as follows: TCD-ethanol solution concentration was 170 mg/mL, the volume ratio of antisolvent was 4 times that of solvent, and the amount of the surfactant was 0.3% stirred for 10 min by 2500 rpm; TCD nanoparticle with a mean particle size (MPS) of130±12.5 nm is obtained under the optimum conditions. SEM, FT-IR, LC-MS/MS, XRD, and DSC were used to characterize the TCD nanoparticle. The results showed that the chemical structure of TCD nanoparticle was not changed, but the crystallization was significantly reduced. Solubility, dissolution rate, antioxidant activity, the in vitro transdermal penetration, and bioavailability of TCD nanoparticles were all much better than these of the raw TCD. These results suggested that TCD nanoparticle might have potential value to become a new oral or transdermal TCD formulation with high bioavailability.

scholarly journals The Systems of Naringenin with Solubilizers Expand Its Capability to Prevent Neurodegenerative Diseases

2022 ◽  
Vol 23 (2) ◽  
pp. 755
Author(s):  
Anna Stasiłowicz-Krzemień ◽  
Michał Gołębiewski ◽  
Anita Płazińska ◽  
Wojciech Płaziński ◽  
Andrzej Miklaszewski ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Water Solubility ◽  
Solid Dispersions ◽  
Apparent Permeability ◽  
In Silico Studies ◽  
Apparent Permeability Coefficient ◽  
Ft Ir ◽  
Low Solubility ◽  
Permeability Assay

Background: Naringenin (NAR) is a flavonoid with excellent antioxidant and neuroprotective potential that is limited by its low solubility. Thus, solid dispersions with β-cyclodextrin (β-CD), hydroxypropyl-β-cyclodextrin (HP-β-CD), hydroxypropylmethylcellulose (HPMC), and microenvironmental pH modifiers were prepared. Methods: The systems formation analysis was performed by X-Ray Powder Diffraction (XRPD) and Fourier-transform infrared spectroscopy (FT-IR). Water solubility and dissolution rates were studied with a pH of 1.2 and 6.8. In vitro permeability through the gastrointestinal tract (GIT) and the blood-brain barrier (BBB) was assessed with the parallel artificial membrane permeability assay (PAMPA) assay. The antioxidant activity was studied with the 2,2′-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid (ABTS) and cupric ion reducing antioxidant capacity (CUPRAC) assays, while in vitro enzymes studies involved the inhibition of acetylcholinesterase, butyrylcholinesterase, and tyrosinase. For the most promising system, in silico studies were conducted. Results: NAR solubility was increased 458-fold by the solid dispersion NAR:HP-β-CD:NaHCO3 in a mass ratio of 1:3:1. The dissolution rate was elevated from 8.216% to 88.712% in a pH of 1.2 and from 11.644% to 88.843% in a pH of 6.8 (within 3 h). NAR GIT permeability, described as the apparent permeability coefficient, was increased from 2.789 × 10−6 cm s−1 to 2.909 × 10−5 cm s−1 in an acidic pH and from 1.197 × 10−6 cm s−1 to 2.145 × 10−5 cm s−1 in a basic pH. NAR BBB permeability was established as 4.275 × 10−6 cm s−1. The antioxidant activity and enzyme inhibition were also increased. Computational studies confirmed NAR:HP-β-CD inclusion complex formation. Conclusions: A significant improvement in NAR solubility was associated with an increase in its biological activity.

scholarly journals Microwave-Assisted Synthesis, Characterization, Antimicrobial and Antioxidant Activity of Some New Isatin Derivatives

2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
G. Kiran ◽  
T. Maneshwar ◽  
Y. Rajeshwar ◽  
M. Sarangapani
Keyword(s):  
Antioxidant Activity ◽  
Free Radical ◽  
Radical Scavenging ◽  
Microwave Assisted Synthesis ◽  
Stable Free Radical ◽  
Ft Ir ◽  
Antimicrobial And Antioxidant Activity ◽  
New Compounds ◽  
Isatin Derivatives

A series of β-Isatin aldehyde-N,N′-thiocarbohydrazone derivatives were synthesized and assayed for theirin vitroantimicrobial and antioxidant activity. The new compounds were characterized based on spectral (FT-IR, NMR, MS) analyses. All the test compounds possessed a broad spectrum of activity having MIC values rangeing from 12.5 to 400 μg/ml against the tested microorganisms. Among the compounds3e,3jand3nshow highest significant antimicrobial activity. The free radical scavenging effects of the test compounds against stable free radical DPPH (α,α-diphenyl-β-picryl hydrazyl) and H2O2were measured spectrophotometrically. Compounds3j,3n,3l, and3e, respectively, had the most effective antioxidant activity against DPPH and H2O2scavenging activity.

Biodegradable polymers-based nanoparticles to enhance the antifungal efficacy of fluconazole against Candida albicans

2021 ◽  
Vol 22 ◽  
Author(s):  
Noha Saleh ◽  
Soha Elshaer ◽  
Germeen Girgis
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Encapsulation Efficiency ◽  
Water Solubility ◽  
In Vitro Release ◽  
Double Emulsion ◽  
Dilution Method ◽  
Ft Ir ◽  
Antifungal Efficacy

Background: Fluconazole (FLZ), a potent antifungal medication, is characterized by poor water solubility that reduced its antifungal efficacy. Objective: This study aimed to prepare FLZ-loaded polymeric nanoparticles (NPs) by using different polymers and techniques as a mean of enhancing the antifungal activity of FLZ. Methods: NP1, NP2, and NP3 were prepared by the double emulsion/solvent evaporation method using PLGA, PCL, and PLA, respectively. The ionotropic pre-gelation technique was applied to prepare an alginate/chitosan-based formulation (NP4). Particle size, zeta potential, encapsulation efficiency, and loading capacity were characterized. FT-IR spectra of FLZ, the polymers, and the prepared NPs were estimated. NP4 was selected for further in-vitro release evaluation. The broth dilution method was used to assess the antifungal activity of NP4 using a resistant clinical isolate of Candida albicans. Results: The double emulsion method produced smaller-sized particles (<390 nm) but with much lower encapsulation efficiency (< 12%). Alternatively, the ionic gelation method resulted in nanosized particles with a markedly higher encapsulation efficiency of about 40%. The FT-IR spectroscopy confirmed the loading of the FLZ molecules in the polymeric network of the prepared NPs. The release profile of NP4 showed a burst initial release followed by a controlled pattern up to 24 hours with a higher percent released relative to the free FLZ suspension. NP4 was able to reduce the value of MIC of FLZ by 20 times. Conclusion: The antifungal activity of FLZ against C. albicans was enhanced markedly via its loading in the alginate/chitosan-based polymeric matrix of NP4.

scholarly journals A Micellar Mitotane Formulation with High Drug Loading and Solubility: Physico-Chemical Characterization and Cytotoxicity Studies in 2D and 3D in Vitro Tumor Models.

2019 ◽  
Author(s):  
Malik Salman Haider ◽  
Jochen Schreiner ◽  
Sabine Kendl ◽  
Matthias Kroiß ◽  
Robert Luxenhofer
Keyword(s):  
Water Solubility ◽  
Drug Loading ◽  
Plasma Concentrations ◽  
Ethanol Solution ◽  
Comparable Efficacy ◽  
Scanning Calorimetry ◽  
High Drug ◽  
Cytotoxicity Studies ◽  
High Drug Loading

Adrenocortical carcinoma (ACC) is a rare tumor and prognosis is overall poor but heterogeneous. Mitotane (MT) has been used for treatment of ACC for decades, either alone or in combination with cytotoxic chemotherapy. Even at doses up to 6 g per day, more than half of the patients do not achieve targeted plasma concentration (14-20 mg/L) even after many months of treatment which is caused by low water solubility and unfavorable pharmacokinetic properties such as poor bioavailability and high volume of distribution of MT. The clinical need and previously reported extraordinary high drug loading of poly(2-methyl-2-oxazoline)-block-poly(2-butyl-2-oxazoline)-block-poly(2-methyl-2-oxazoline) (A-pBuOx-A) based micelles for paclitaxel (PTX), led us to develop MT loaded micelles which may enable an injectable formulation. We successfully solubilized up to 6 g/L of MT in an aqueous formulation. The MT loaded nanoformulations were characterized by Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC) and powder X-ray<br> <p>diffraction (XRD), confirmed the amorphous nature of drug in the formulations. The polymer itself did not show cytotoxicity in adrenal and liver cell lines. By using the ACC model cell line NCI-H295 both in monolayers and tumor cell spheroids, we demonstrated micellar MT to exhibit comparable efficacy to its ethanol solution. We postulate that this formulation would be suitable for i.v. application and more rapid attainment of therapeutic plasma concentrations. In conclusion, we consider our micellar formulation a promising tool to alleviate major drawbacks of current MT treatment while retaining bioactivity towards ACC in vitro.</p>

scholarly journals Synthesis, Spectroscopic Study and Radical Scavenging Activity of Kaempferol Derivatives: Enhanced Water Solubility and Antioxidant Activity

2019 ◽  
Vol 20 (4) ◽  
pp. 975 ◽  
Author(s):  
Sui-Ping Deng ◽  
Yi-Li Yang ◽  
Xing-Xing Cheng ◽  
Wen-Rong Li ◽  
Ji-Ye Cai
Keyword(s):  
Antioxidant Activity ◽  
Water Solubility ◽  
High Resolution Mass Spectrometry ◽  
Antioxidant Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Dependent Manner ◽  
Thermal Methods ◽  
Vis Spectroscopy

Kaempferol (Kae) is a natural flavonoid with potent antioxidant activity, but its therapeutic use is limited by its low aqueous solubility. Here, a series of Kae derivatives were synthesized to improve Kae dissolution property in water and antioxidant activity. These compounds included sulfonated Kae (Kae-SO3), gallium (Ga) complexes with Kae (Kae-Ga) and Kae-SO3 (Kae-SO3-Ga). The compound structures were characterized by high-resolution mass spectrometry (HRMS), nuclear magnetic resonance (NMR) spectroscopy, ultraviolet-visible (UV-Vis) spectroscopy, Fourier transform infrared (FT-IR) spectroscopy and thermal methods (TG/DSC). The results showed that a sulfonic group (-SO3) was successfully tethered on the C3’ of Kae to form Kae-SO3. And in the metal complexation, 4-CO and 3-OH of the ligand participated in the coordination with Ga(III). The metal-to-ligand ratio 1:2 was suggested for both complexes. Interestingly, Kae-SO3-Ga was obviously superior to other compounds in terms of overcoming the poor water-solubility of free Kae, and the solubility of Kae-SO3-Ga was about 300-fold higher than that of Kae-Ga. Furthermore, the evaluation of antioxidant activities in vitro was carried out for Kae derivatives by using α,α-diphenyl-β-picrylhydrazyl (DPPH) and 2,2’-azino-bis(3-ethylbenzo-thiazoline-6-sulfonic acid) diammonium salt (ABTS) free radical scavenging. The results showed that Kae-SO3-Ga was also optimal for scavenging free radicals in a dose-dependent manner. These data demonstrate that sulfonate kaempferol-gallium complex has a promising future as a potential antioxidant and as a potential therapeutic agent for further biomedical studies.

Chemical composition and antioxidant activity of Carob pulp (Ceratonia Siliqua L.) extracts

2015 ◽  
Vol 5 (2) ◽  
pp. 76-83
Author(s):  
Yasmina Mokhtaria Boufadia ◽  
Manel Elaoufi ◽  
Fatiha Tabet ◽  
Mohamed Benali ◽  
Ali Riazi
Keyword(s):  
Antioxidant Activity ◽  
Food Additives ◽  
Ethanolic Extract ◽  
Natural Food ◽  
Ceratonia Siliqua ◽  
Total Blood ◽  
Pre Treatment ◽  
Ceratonia Siliqua L

  The role of polyphenols and flavonoids in prevention of cellular damages carried out with the oxidative stress is well documented. In the present experiment, we determined the polyphenols and flavonoids concentrations of three extracts (ethanol 70%: V/V, methanol 80%: V/V and distilled water extracts) of carob pulp mature (Ceratonia siliqua L.) and their in vitro and in vivo antioxidant activity. A significant dose-dependent anti-free radical activ-ity of ethanolic extract of carob (EEC) was related to the highest polyphenol content (44.74 mg QE/mL) and to the in vitro antioxidant activity (EC50 = 0.28 mg/mL) of this extract. LC-MS /MS analysis of the EEC have shown the presence of several phenolic compounds as well as many types of flavonoids. The in vivo experiment brought out the significant effect of the daily EEC oral pre-treatment of rats, 30 min before AlCl3 administration for 28 d on the improvement of the total blood antioxidant capacity. These results suggest that the carob pulp contain many substances having in vitro and in vivo antioxidant effects, and which could be used as natural food additives in order to preserve food quality.

scholarly journals Synthesis, Characterization, and Antioxidant Evaluation of Novel Pyridylurea-Functionalized Chitosan Derivatives

Polymers ◽  
2019 ◽  
Vol 11 (6) ◽  
pp. 951 ◽  
Author(s):  
Jingjing Zhang ◽  
Wenqiang Tan ◽  
Lijie Wei ◽  
Fang Dong ◽  
Qing Li ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Structural Characteristics ◽  
Radical Scavenging ◽  
Cytotoxicity Test ◽  
Chitosan Derivatives ◽  
Ester Exchange ◽  
1H Nuclear Magnetic Resonance ◽  
Ft Ir ◽  
Ester Exchange Reaction

In order to improve the bioactivity of chitosan, we synthesized a novel series of chitosan derivatives: firstly, chitosan was reacted with methylclhlorofonmate obtaining N-methoxyformylated chitosan (1), which was then converted into N-pyridylurea chitosan derivatives (2a-2c) by amine-ester exchange reaction. In addition, N-pyridylurea chitosan derivatives were conducted by reacting with iodomethane to obtain quaternized N-pyridylurea chitosan derivatives (3a-3c). The structural characteristics of as-prepared chitosan derivatives were confirmed by fourier transform infrared (FT-IR), 1H nuclear magnetic resonance (1H NMR), elemental analysis, and scanning electron microscope (SEM). Meanwhile, the antioxidant activity of the chitosan derivatives was assessed in vitro. As shown in this paper, the antioxidant activity decreased in the order: c > b > a. Moreover, after the quaternization with iodomethane, quaternized N-pyridylurea chitosan derivatives immediately exhibited enhanced antioxidant capacity compared with N-pyridylurea chitosan derivatives. For example, in 1,1-Diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assay, the scavenging activities of 3a-3c were 91.75%, 93.63%, and 97.63% while 2a-2c were 42.32%, 42.97%, and 43.07% at 0.4 mg/mL. L929 cells were also adopted for cytotoxicity test of chitosan and synthesized derivatives by CCK-8 assay and all samples showed decreased cytotoxicity. These results suggested that the novel pyridylurea-functionalized chitosan derivatives could be an ideal biomaterial.

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