Current Techniques of Water Solubility Improvement for Antioxidant Compounds and Their Correlation with Its Activity: Molecular Pharmaceutics

Antioxidants, Journal Year: 2023, Volume and Issue: 12(2), P. 378 - 378

Published: Feb. 4, 2023

The aqueous solubility of a drug is important in the oral formulation because can be absorbed from intestinal sites after being dissolved gastrointestinal fluid, leading to its bioavailability. Almost 80% active pharmaceutical ingredients are poorly water-soluble, including antioxidant compounds. This makes activity inefficient preventing disease, particularly for orally administered formulations. Although several investigations have been carried out improve compounds, there still limited research fully discussing subject. Therefore, this study aimed provide an overview and discussion issues related methods that used Articles were found using keywords “antioxidant” “water improvement” Scopus, PubMed, Google Scholar databases. selected articles published within last five years ensure all information was up-to-date with same objectives. most popular strategies employed solid dispersion, co-amorphous, nanoparticle delivery systems, which enhance These produced impressive results, detailed mechanism improvement compounds developed. review shows increase successfully improved their enhanced free radical scavenging abilities.

Language: Английский

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Simultaneous Improvement of Dissolution Behavior and Oral Bioavailability of Antifungal Miconazole via Cocrystal and Salt Formation

Pharmaceutics, Journal Year: 2022, Volume and Issue: 14(5), P. 1107 - 1107

Published: May 22, 2022

Miconazole shows low oral bioavailability in humans due to poor aqueous solubility, although it has demonstrated various pharmacological activities such as antifungal, anti-tubercular and anti-tumor effects. Cocrystal/salt formation is one of the effective methods for solving this problem. In study, different (liquid-assisted grinding, slurrying lyophilization) were used investigate their impact on miconazole multicomponent crystals with succinic, maleic dl-tartaric acids. The solid state prepared powder was characterized by differential scanning calorimetry, X-ray diffraction electron microscopy. It found that lyophilization not only promotes partial amorphization both salts but also allows obtaining a new polymorph salt acid. lyophilized compared same samples two other showed better dissolution rates stability during studies rapid recrystallization. Overall, determined preparation method affects solid-state characteristics physicochemical properties significantly. vivo revealed indicated higher peak blood concentration area under curve from 0 32 h values 2.4-, 2.9- 4.6-fold than pure drug. Therefore, study are promising formulations enhancing poorly soluble compounds.

Language: Английский

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New insights on transition metal coordination compounds with biological active azole and nitroimidazole derivatives

Coordination Chemistry Reviews, Journal Year: 2023, Volume and Issue: 494, P. 215360 - 215360

Published: Aug. 1, 2023

Language: Английский

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Revolutionizing Antiviral Therapeutics: Unveiling Innovative Approaches for Enhanced Drug Efficacy

International Journal of Nanomedicine, Journal Year: 2024, Volume and Issue: Volume 19, P. 2889 - 2915

Published: March 1, 2024

Abstract: Since the beginning of coronavirus pandemic in late 2019, viral infections have become one top three causes mortality worldwide. Immunization and use immunomodulatory drugs are effective ways to prevent treat infections. However, primary therapy for managing remains antiviral antiretroviral medication. Unfortunately, these often limited by physicochemical constraints such as low target selectivity poor aqueous solubility. Although several modifications been made enhance characteristics efficacy drugs, there few published studies that summarize compare modifications. Our review systematically synthesized discussed drug modification reports from publications indexed Scopus, PubMed, Google Scholar databases. We examined various approaches were investigated address issues increase activity, including liposomes, cocrystals, solid dispersions, salt modifications, nanoparticle delivery systems. impressed how well each strategy addressed improved activity. In conclusion, represent a promising way improve characteristics, functionality, effectiveness antivirals clinical therapy. Keywords: current system, properties

Language: Английский

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Influence of Solvent Polarity on the Conformer Ratio of Bicalutamide in Saturated Solutions: Insights from NOESY NMR Analysis and Quantum-Chemical Calculations

International Journal of Molecular Sciences, Journal Year: 2024, Volume and Issue: 25(15), P. 8254 - 8254

Published: July 28, 2024

The study presents a thorough and detailed analysis of bicalutamide’s structural conformational properties. Quantum chemical calculations were employed to explore the properties molecule, identifying significant energy differences between conformers. Analysis revealed that hydrogen bonds stabilise conformers, with notable variations in torsion angles. Conformers classified into ‘closed’ ‘open’ types based on relative orientation cyclic fragments. NOE spectroscopy different solvents (CDCl3 DMSO-d6) was used preferences molecule. NOESY experiments provided predominance conformers non-polar presence polar solvents. proportions open 22.7 ± 3.7% CDCl3 59.8 6.2% DMSO-d6, while closed accounted for 77.3 40.2 6.2%, respectively. This comprehensive underscores solvent environment’s impact its behaviour. findings significantly contribute deeper understanding dynamics, stimulating further exploration drug development.

Language: Английский

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Pharmaceutical Multicomponent Crystals of Antifungal Drugs with Improved Dissolution Performance

Crystal Growth & Design, Journal Year: 2021, Volume and Issue: 21(12), P. 7285 - 7297

Published: Nov. 15, 2021

New multicomponent crystals of climbazole (CLB) with fumaric acid (FumAc) and tioconazole (TCL) oxalic (OxlAc), malonic (MlnAc), fumaric, dl-tartaric (TartAc) acids were obtained by liquid-assisted grinding. The single CLB for the first time, crystal structure was characterized. structures four studied─[CLB + FumAc] cocrystal (2:1), [TCL MlnAc] salt (1:1), TartAc H2O] (1:1:1)─the which slow evaporation form solution determined. influence coformer on TCL conformational flexibility discussed. A thermal analysis studied carried out. (1:1:1) dehydration mechanism analyzed differential scanning calorimetry, a thermogravimetric method, thermomicroscopy. It established that completion process followed melting eutectic mixture crystallization TartAc] (1:1). study solubility out in phosphate buffer at pH 6.8. Cocrystallization/salt formation active pharmaceutical ingredients dicarboxylic not only significantly improved their but also maintained level supersaturation quite long time.

Language: Английский

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Computational evaluation of halogen-bonded cocrystals enables prediction of their mechanochemical interconversion reactions

Chemical Science, Journal Year: 2023, Volume and Issue: 14(12), P. 3140 - 3146

Published: Jan. 1, 2023

Periodic density-functional theory (DFT) calculations were used to predict the thermodynamic stability and likelihood of interconversion between a series halogen-bonded cocrystals. The outcomes mechanochemical transformations in excellent agreement with theoretical predictions, demonstrating power periodic DFT as method for designing solid-state reactions prior experimental work. Furthermore, calculated energies compared dissolution calorimetry measurements, marking first such benchmark accuracy modelling molecular crystals.

Language: Английский

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Pharmaceutical Salts of Azole Anti-fungal Drugs: Physicochemical Behaviour and Activity Studies

RSC Pharmaceutics, Journal Year: 2024, Volume and Issue: 1(4), P. 705 - 715

Published: Jan. 1, 2024

We report the pharmaceutical salts of ketoconazole and miconazole to address drug-resistance through drug modification. The resultant exhibit improved physicochemical behaviour more versatile activity than commercial antifungals.

Language: Английский

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Preparation and structure analysis of non-covalent interactions mediated 2D-3D supramolecular adducts from 6-methylnicotinamide and carboxylic acids

Journal of Molecular Structure, Journal Year: 2022, Volume and Issue: 1264, P. 133135 - 133135

Published: April 22, 2022

Language: Английский

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Preparation and structure analysis of non-covalent interactions directed 11 adducts from 2-amino-5-methylthiazole and organic acids

Journal of Molecular Structure, Journal Year: 2022, Volume and Issue: 1263, P. 133031 - 133031

Published: April 19, 2022

Language: Английский

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