Electrochemical and spectral characterization of the host-guest inclusion complex of the antiparasitic drug nitazoxanide with β-cyclodextrin

Radi, Abd-Elgawad; Nassef, Hossam M.; El-Naggar, Abd-Elrahman

doi:10.1007/s00706-013-1109-1

Cited by 6 publications

(3 citation statements)

References 34 publications

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“…3), traditionally an antiparasitic drug, has also demonstrated in vitro antiviral activity against MERS and SARS-CoV-2 (Padmanabhan, 2020). Its interaction with β-CD has been studied by different physicochemical methods, showing that it forms inclusion complexes with 1:1 stoichiometry (Radi et al, 2014). Camostat mesylate ( Fig.…”

Section: Cyclodextrins In Formulations Against Sars-cov-2mentioning

confidence: 99%

The Lord of the NanoRings: Cyclodextrins and the battle against SARS-CoV-2

Garrido

Calvelo

Blanco-González

et al. 2020

International Journal of Pharmaceutics

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Elsevier has created a COVID-19 resource centre with free information in English and Mandarin on the novel coronavirus COVID-19. The COVID-19 resource centre is hosted on Elsevier Connect, the company's public news and information website. Elsevier hereby grants permission to make all its COVID-19-related research that is available on the COVID-19 resource centre-including this research content-immediately available in PubMed Central and other publicly funded repositories, such as the WHO COVID database with rights for unrestricted research re-use and analyses in any form or by any means with acknowledgement of the original source. These permissions are granted for free by Elsevier for as long as the COVID-19 resource centre remains active.

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Section: Cyclodextrins In Formulations Against Sars-cov-2mentioning

confidence: 99%

The Lord of the NanoRings: Cyclodextrins and the battle against SARS-CoV-2

Garrido

Calvelo

Blanco-González

et al. 2020

International Journal of Pharmaceutics

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“…5 Although NTZ is an agent with diverse pharmacological activities and minimal toxicity, it has unfavorable physicochemical and biopharmaceutical properties, in particular very poor aqueous solubility 6 and low bioavailability, 4 and this provided the motivation for discovering new solid forms which may improve its solubility, dissolution rate, and bioavailability, and thus provide improved therapeutic options for patients. In fact, NTZ has been in the focus of pharmaceutical research to discover and prepare alternative solid forms such as cyclodextrin complexes, 7,8 solid dispersions, 9 cocrystals 10 and cocrystal alloys. 11 Regarding NTZ cocrystals, it was found that it cocrystallized with five organic acids [succinic, 10 glutaric, 10 2,5dihydroxybenzoic, 10 p-aminobenzoic and p-aminosalicylic 11 , showing a common heterodimeric synthon formed between the carboxyl group of the acid coformer and the carboxamidine group of NTZ (Figure 1), namely the carboxyl-carboxamidine synthon.…”

Section: Introductionmentioning

confidence: 99%

Mechanochemical synthesis of a novel eutectic of the antimicrobial nitazoxanide with improved dissolution performance

Fandiño¹,

Bruno²,

Monti³

et al. 2021

Pharm Sci

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Background: Nitazoxanide (NTZ) is a broad spectrum antimicrobial agent with poor aqueous solubility and low bioavailability. Thus, the generation of new solid forms of NTZ is relevant to improve its unfavorable properties. The present study deals with the application of mechanochemistry for the preparation of alternate solid forms of NTZ, using saccharine (SAC) as coformer. Methods: NTZ-SAC mixtures were prepared by neat and liquid-assisted grinding (LAG) and characterized using differential scanning calorimetry (DSC), hot stage microscopy (HSM), X-ray Powder Diffraction (XRPD), 13C Solid-state Nuclear Magnetic Resonance (SSNMR) and Diffuse Reflectance Infrared Fourier Transform (DRIFT) spectroscopy. Powder dissolution (PD) profiles were obtained with USP apparatus 2 in buffer phosphate pH 6.5 with 0.25% Tween 80 - 0.25% triethanolamine and in 0.25% sodium lauryl sulfate, at 37 ºC ± 0.5 ºC and 75 rpm. Drug release was characterized in terms of dissolution efficiency (DE). Results: XRPD, SSNMR and DRIFT indicated that NTZ and SAC did not cocrystallize but DSC and HSM revealed that they formed a binary eutectic mixture which melted near 176 °C, a melting temperature lower than those of NTZ and SAC. PD data indicated that the 1:1 NTZ-SAC sample obtained by LAG exhibited a slightly higher DE than pure NTZ in the two assayed media. Conclusion: NTZ and SAC formed a eutectic, the first reported for this drug, which improved its dissolution rate and opened the pathway for studies searching for new eutectics with better biopharmaceutical attributes than NTZ and the NTZ-SAC eutectic reported herein.

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“…The importance of pharmaceutical application of cyclodextrins as drug carriers has been recognized for a long time [15]. Cyclodextrins, acting as hosts, are able to increase the solubility of the sparingly soluble compounds and thus, in the case of drugs, to enhance their bioavailability [16,17]. Also, some other properties can be improved, such as resistance to light [18], organoleptic properties [19], as well as enhanced drug permeation [20].…”

Section: Introductionmentioning

confidence: 99%

Electrochemical determination of sertraline in pharmaceutical formulation and serum using a gold electrode in a pH 8.4 bicarbonate solution

et al. 2021

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The electrochemical characterization of sertraline at gold electrode was examined by cyclic voltammetry measurements (CV) in pH 8.4 bicarbonate buffer. Then Au electrode was evaluated for the quantitative determination of sertraline using square wave voltammetry (SWV). To enhance the sensitivity during the drug determination, (2-hydroxypropyl)-β-cyclodextrin (HPβCD) and β-cyclodextrin (βCD) inclusion complexes were employed. Using the proposed SWV technique, the anodic current peak was linear within a concentration range of 0.1-0.5 µM with a limit of detection (LOD) of 2.0 × 10 -8 M and a limit of quantification (LOQ) of 6.7 × 10 -8 M. In the case of inclusion complex of the sertraline with HPβCD, a good linearity range of 0.1-0.9 µM was obtained with a LOD of 2.6 × 10 -8 M and a LOQ of 8.8 × 10 -8 M. The gold electrode revealed the same linearity range for inclusion complex of the sertraline with βCD with a LOD and a LOQ being 2.6 × 10 -8 and 8.6 × 10 -8 M, respectively. Comparing the regression equations, it can be concluded that the sensitivity in the presence of inclusion complex can be up to 5 times higher. The applicability of the developed method was confirmed by the analysis of this drug in pharmaceutical formulation and in human serum spiked with sertraline standard. The comparison to HPLC method was successfully performed.

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Electrochemical and spectral characterization of the host-guest inclusion complex of the antiparasitic drug nitazoxanide with β-cyclodextrin

Cited by 6 publications

References 34 publications

The Lord of the NanoRings: Cyclodextrins and the battle against SARS-CoV-2

The Lord of the NanoRings: Cyclodextrins and the battle against SARS-CoV-2

Mechanochemical synthesis of a novel eutectic of the antimicrobial nitazoxanide with improved dissolution performance

Electrochemical determination of sertraline in pharmaceutical formulation and serum using a gold electrode in a pH 8.4 bicarbonate solution

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