Simple mix-and-read assays for the determination of baclofen in pharmaceutical formulation

El-Yazbi, Amira F.; Guirguis, Karin M.; Bedair, Mona M.; Belal, Tarek S.

doi:10.1016/j.heliyon.2019.e01854

Cited by 6 publications

(4 citation statements)

References 20 publications

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“…Fluorescence measurement is an important methodology that is widely used for the determination of various damage types that are induced in DNA through interaction with small molecules. Several fluorescent probes that are commonly used for this purpose include terbium chloride, [ 43,44 ] Hoechst 33258 dye, [ 45 ] fluorescent molecular beacons, [ 46–48 ] and EvaGreen (EG). [ 49,50 ] In this study, EG is selected to detect any possible DNA damage that may be induced due to the interaction of DNA with the studied compounds.…”

Section: Resultsmentioning

confidence: 99%

Discovery of novel benzimidazole acyclic C‐nucleoside DNA intercalators halting breast cancer growth

Abd Al Moaty,

El Kilany,

Awad

et al. 2023

Archiv der Pharmazie

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Breast cancer continues to be the most frequent cancer worldwide. In practice, successful clinical outcomes were achieved via targeting DNA. Along with the advances in introducing new DNA‐targeting agents, the “sugar approach” design was employed herein to develop new intercalators bearing pharmacophoric motifs tethered to carbohydrate appendages. Accordingly, new benzimidazole acyclic C‐nucleosides were rationally designed, synthesized and assayed via MTT (3‐[4,5‐dimethylthiazol‐2‐yl]‐2,5 diphenyl tetrazolium bromide) assay to evaluate their cytotoxicity against MCF‐7 and MDA‐MB‐231 breast cancer cells compared to normal fibroblasts (Wi‐38), compared to doxorubicin. (1S,2R,3S,4R)‐2‐(1,2,3,4,5‐Pentahydroxy)pentyl‐1H‐5,6‐dichlorobenzimidazole 7 and (1S,2R,3S,4R)‐2‐(1,2,3,4,5‐pentahydroxy)pentyl‐1H‐naphthimidazole 13 were the most potent and selective derivatives against MCF‐7 (half‐maximal inhibitory concentration [IC50] = 0.060 and 0.080 µM, selectivity index [SI] = 9.68 and 8.27, respectively) and MDA‐MB‐231 cells (IC50 = 0.299 and 0.166 µM, SI = 1.94 and 3.98, respectively). Thus, they were identified as the study hits for mechanistic studies. Both derivatives induced DNA damage at 0.24 and 0.29 μM, respectively. The DNA damage kinetics were studied compared to doxorubicin, where they both induced faster damage than doxorubicin. This indicated that 7 and 13 showed a more potent DNA‐damaging effect than doxorubicin. Docking simulations within the DNA double strands highlighted the role of both the heterocyclic core and the sugar side chain in exhibiting key H‐bond interactions with DNA bases.

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Section: Resultsmentioning

confidence: 99%

Discovery of novel benzimidazole acyclic C‐nucleoside DNA intercalators halting breast cancer growth

Abd Al Moaty,

El Kilany,

Awad

et al. 2023

Archiv der Pharmazie

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“…A thorough literature survey reveals plenty of adopted methods for BAC determination in pharmaceutical formulations and biological fluids [ 13 ]. Among of them are; UV spectroscopy [ 14 – 18 ], spectrofluorimetry [ 19 – 21 ], capillary electrophoresis [ 20 ], RP-HPLC [ 22 ], HPTLC [ 7 , 23 ], LC–MS/MS [ 24 , 25 ], and potentiometry [ 26 ]. However, only one method that depended on microfluidics-based fluorimetric technology was reported for BAC [ 27 ].…”

Section: Introductionmentioning

confidence: 99%

Smartphone based colorimetric point-of-care sensor for abused drugs: case of baclofen determination in urine

Abd el-Aziz,

Nadim,

Monir

et al. 2023

BMC Chemistry

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As a GABA-β receptor agonist, the central muscle relaxant Baclofen (BAC) has a potential of abuse. Unfortunately, the sense of wellbeing and pleasure is obtained at very high BAC doses. This is associated with many life-threating or even fatal cases due to neurological and respiratory failures. Moreover, having narrow therapeutic index makes BAC a high-risk drug. This is potentiated in case of long-treatment regimen or off-label use in smoking and alcohol cessation protocols. Until now, there is no rapid diagnostic test available for BAC screening. Therefore; It is quite difficult to routinely monitor cases on BAC regimen. On the other hand, smartphone-based colorimetric point of care testing (POCT) is displacing conventional analytical approaches in the detection and assay of abused drugs as well as therapeutic drug monitoring. It offers on-site, rapid, easy, affordable and interpretable analysis. Incorporating smartphone as a portable device facilitates its application, especially in remote areas and low-income countries. For the first time, the current work presents a smartphone-based colorimetric POCT for BAC analysis in urine without interference from urine matrix. It depends on BAC reaction with naphthoquinone sulfonate (NQS) in highly alkaline aqueous medium. The developed color was captured in a customized photo box using smartphone camera. Then, intensity of the blue channel was measured by a software application “Color Analyzer”. All parameters were optimized with respect to the colorimetric reaction, photographing and smartphone-based analysis. All parameters were successfully investigated according to FDA guidelines for bioanalytical method validation. Also, all POCT criteria were considered as per WHO requirements. This method could determine BAC, linearly, from 0.02 to 0.21 mmol L−1 in urine. Moreover, LLOQ was lower than the expected BAC therapeutic concentrations in urine. The proposed method proved high reliability and suitability to analyze BAC in urine. This strongly recommends its routine application in screening BAC abusers and BAC therapeutic monitoring. Graphical Abstract

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“…These methods include derivative ratio ( 2 DD), delta absorbance (ΔA, ΔD 1 ), and derivative compensation. Moreover, colorimetric methods (ElKimary & El-Yazbi, 2016;El-Yazbi, 2017;Ibrahim et al, 2017;El-Yazbi et al, 2019) can be used for the specific analysis of VP. In this study, two specific methods were proposed for the detection of VP by its specific reaction with NBD-Cl and MBTH reagents without interference from SF.…”

Section: Introductionmentioning

confidence: 99%

Eco-friendly analytical methods for the determination of compounds with disparate spectral overlapping: application to antiviral formulation of sofosbuvir and velpatasvir

et al. 2021

Self Cite

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Green analytical chemistry is one of the newest trends in analytical chemistry nowadays targeting the concept of green laboratory practices on chemists and environment. In this text, green practices are proposed in this work for the determination of sofosbuvir (SF) and velpatasvir (VP) in their pharmaceutical formulation. The analysis of SF in a binary mixture with VP represents an analytical challenge due to the complete overlapping of the UV spectrum of SF by that of VP. Therefore, the direct absorbance and derivative measurements cannot resolve such interference and failed to determine SF. In this paper, three direct and simple methods were developed for the analysis of SF without any interference from VP without sample pre-treatment. The proposed methods include measuring the second derivative amplitude of the ratio spectrum of the mixture using VP as a divisor, measuring the absorbance difference of the mixture in NaOH solution against its HCl solution, and using the derivative compensation technique. On the other hand, VP was determined specifically in presence of SF by two methods. Firstly, by its reaction with 4-chloro-7-nitrobenzofurazan (NBD-Cl) where the reaction product was measured spectrophotometrically and spectrofluorometrically and secondly through the reaction of VP with 3-methyl-2-benzothiazolinone hydrazone hydrochloride (MBTH). The calibration curves showed good correlation coefficient (r2 > 0.999). The developed methods were highly precise with RSD% values less than 2%. The method greenness profile was compared with other published methods by applying the eco-scale protocol. Assessment results proved that our analytical procedure is greener than other reported methods. Moreover, upon comparison with other methods, the proposed methods showed better or comparable sensitivity in addition to being inexpensive and ecofriendly. Accordingly, these methods could be readily applied for quality control purposes as an eco-friendly, simple and efficient analytical tool.

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Simple mix-and-read assays for the determination of baclofen in pharmaceutical formulation

Cited by 6 publications

References 20 publications

Discovery of novel benzimidazole acyclic C‐nucleoside DNA intercalators halting breast cancer growth

Discovery of novel benzimidazole acyclic C‐nucleoside DNA intercalators halting breast cancer growth

Smartphone based colorimetric point-of-care sensor for abused drugs: case of baclofen determination in urine

Eco-friendly analytical methods for the determination of compounds with disparate spectral overlapping: application to antiviral formulation of sofosbuvir and velpatasvir

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