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Studying the Complex Formation of Sulfonatocalix[4]naphthalene and Meloxicam towards Enhancing Its Solubility and Dissolution Performance

Research Abstract

The interaction between meloxicam and sulfonatocalix [4] naphthalene was investigated
to improve the meloxicam solubility and its dissolution performance. Solubility behavior was investigated
in distilled water (DW) and at different pH conditions. Besides, solid systems were prepared
in a 1:1 molar ratio using coevaporate, kneading, and simple physical mixture techniques.
Further, they were characterized by PXRD, FT-IR, DCS, and TGA. In vitro dissolution rate for coevaporate,
kneaded, and physical mixture powders were also investigated. Solubility study revealed
that meloxicam solubility significantly increased about 23.99 folds at phosphate buffer of pH
7.4 in the presence of sulfonatocalix [4] naphthalene. The solubility phase diagram was classified as
AL type, indicating the formation of 1:1 stoichiometric inclusion complex. PXRD, FT-IR, DCS, and
TGA pointed out the formation of an inclusion complex between meloxicam and sulfonatocalix [4]
naphthalene solid powders prepared using coevaporate technique. In addition, in vitro meloxicam
dissolution studies revealed an improvement of the drug dissolution rate. Furthermore, a significantly
higher drug release (p ≤ 0.05) and a complete dissolution was achieved during the first 10
min compared with the other solid powders and commercial meloxicam product. The coevaporate
product has the highest increasing dissolution fold and RDR10 in the investigated media, with average
values ranging from 5.4–65.28 folds and 7.3–90.7, respectively. In conclusion, sulfonatocalix [4]
naphthalene is a promising host carrier for enhancing the solubility and dissolution performance of
meloxicam with an anticipated enhanced bioavailability and fast action for acute and chronic pain
.disorders

Research Authors
Tayel A. Al Hujran, Mousa K. Magharbeh, Samer Al-Gharabli, Rula R. Haddadin, Manal N. Al Soub and Hesham M. Tawfeek
Research Date
Research Department
Research Journal
Pharmaceutics
Research Publisher
MDPI
Research Vol
13
Research Website
https://doi.org/10.3390/pharmaceutics13070994
Research Year
2021

The first seminar of the master's thesis for the pharmacist: Mina Fayez Saad - the registrar (from abroad) to obtain a master's degree in pharmaceutical sciences (pharmaceutics) - on Wednesday, 30-6-2021 AM.

The first seminar of the doctoral thesis for the master's lady: Heba Yousry Abdel Hamid Raslan - registered in the department (from abroad) to obtain a doctorate degree in pharmaceutical sciences (pharmaceutics) - on Wednesday 30-6-2021 AM

The inhibition of inducible nitric oxide production in lipopolysaccharide-stimulated rat macrophages and in silico studies by flavonoids from Iris spuria L. rhizomes

Research Abstract

Ethnopharmacological relevance: Iris is the largest genus in the family Iridaceae. Iris plants are distributed in
tropical regions of the world. They are used as ornamentals and traditionally used to treat a variety of ailments.
Aim: This study aimed to evaluate the anti-inflammatory effect of flavonoids isolated from Iris spuria L.
Materials and methods: The isolated flavonoids (1-4) were identified on the basis of different spectroscopic
methods (1D- and 2D-NMR) and co-TLC with authentic samples. The anti-inflammatory effect was tested on
lipopolysaccharide (LPS)-induced nitric oxide (NO) production from rat-isolated peritoneal macrophages.
Modeling and docking simulations of the compounds were performed using Molecular Operating Environment
software and the crystal structure of the murine inducible nitric oxide synthase (iNOS).
Results: Four flavonoids (1-4) had been isolated from the rhizomes of Iris spuria L. (Hocka Hoona) for the first
time. They were characterized as 5,7,2’-trihydroxy-6-methoxyflavanone (1), tectorigenin 7-O-β-D-glucopyranoside
(2), tectorigenin 4’-O-β-D-glucopyranoside (3), and tectorigenin 4’-O-[β-D-glucopyranosyl(1 → 6)-β-Dglucopyranoside]
(4). The selective inducible NO synthase inhibitor; aminoguanidine was used as a positive
control. The production of nitric oxide (NO) was inhibited in a dose-dependent manner of the isolated compounds
along with isoflavonoids (5-9) previously isolated from Iris spuria L. (Calizona). A concentration of 60 μg/
ml of all tested compounds showed a significant inhibitory effect compared to media with LPS. Molecular
modeling experiments supported the obtained biological data.
Conclusion: Our results reveal that flavonoids isolated from I. spuria L. (Hocka Hoona) and I. spuria L. (Calizona)
appear to have a potential anti-inflammatory effect via inhibition of iNOS

Research Authors
Iman S.A. Khallaf, Soad A.L. Bayoumi, Lourin G. Malak , Abeer M.R. Hussein, Anber F. Mohammed, Mohamed A. El-Mokhtar, Salwa F. Faragg
Research Date
Research Department
Research Journal
Journal of Ethnopharmacology
Research Publisher
Elsevier
Research Vol
278
Research Website
https://doi.org/10.1016/j.jep.2021.114311
Research Year
2021

Natural coumarins as potential anti-SARS-CoV-2 agents supported by docking analysis

Research Abstract

COVID-19 is a global pandemic first identified in China, causing severe acute respiratory syndrome. One of the therapeutic strategies for combating viral infections is the search for viral spike proteins as attachment inhibitors among natural compounds using molecular docking. This review aims at shedding light on the antiviral potential of natural products belonging to the natural-products class of coumarins up to 2020. Moreover, all these compounds were filtered based on ADME analysis to determine their physicochemical properties, and the best 74 compounds were selected. Using virtual-screening methods, the selected compounds were investigated for potential inhibition of viral main protease (Mpro), viral methyltransferase (nsp16/10 complex), viral recognition binding domain (RBD) of S-protein, and human angiotensin-converting enzyme 2 (ACE2), which is the human receptor for viral S-protein targets, using molecular-docking studies. Promising potential results against SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) and methyltransferase (nsp16) are presented

Research Authors
Usama Ramadan Abdelmohsen, Amgad Albohy, Basma S. Abdulrazik, Soad A. L. Bayoumi, Lourin G. Malak, Iman S. A. Khallaf, Gerhard Bringmann and Salwa F. Farag
Research Date
Research Department
Research Journal
.RSC Adv
Research Publisher
Royal society of chemistry
Research Vol
11
Research Website
DOI: 10.1039/d1ra01989a
Research Year
2021

Vortex-assisted dispersive solid phase microextraction using Fe3O4/FeOOH magnetic nanocomposites for high-performance thin-layer chromatographic determination of zolmitriptan in rabbit plasma samples

Research Abstract

In this work, a fast, versatile, and convenient dispersive solid-phase micro-extraction (DSPME) method is combined with a spectro-densitometric technique for the analysis of zolmitriptan (ZOLM) in biologi- cal fluids. Fe 3 O 4 /FeOOH magnetic nanocomposites (MNCs) were prepared by a co-precipitation method in aqueous solutions and utilized subsequently as a sorbent in DSPME. By coupling DSPME with high- performance thin-layer chromatography (HPTLC) with fluorescence detection, the preconcentration and determination of (ZOLM) in presence of metoclopramide (MET) and paracetamol (PARA), which are pre- scribed as an adjuvant therapy with ZOLM, was accomplished. Adsorption capability was assessed using both Langmuir and Freundlich adsorption isotherm models. The adsorption data was fitted to Langmuir adsorption isotherm model as reflected by high determination coefficient (R 2 = 0.9944). Moreover, ad- sorption kinetics was assessed by pseudo-first and pseudo-second order kinetic models. The data was fitted to pseudo-second order kinetics, which proves that ZOLM interaction with the adsorbent is a chemisorption process. Surface complexation with MNCs was suggested to explain the pH dependence of ZOLM sorption. The key parameters of extraction and desorption steps (including pH, extraction time, sample volume, magnetic adsorbent amount, and desorption circumstances) were evaluated. Optimized conditions for solid phase microextraction of ZOLM were pH 2.9, 5.0 mg Fe 3 O 4 /FeOOH MNCs, 15 min vortex-assisted extraction time and 3 ×200 μL of methanol: 33% ammonia; 4:1 as eluent. The analysis was achieved using ACN: dichloromethane: 33% ammonia (22.5: 6.0: 1.5, v/v/v) as a mobile phase and the fluorescence detection was carried out at 223 nm. The proposed DSPME method was successfully ap- plied for trace quantification of ZOLM in rabbits’ plasma ( n = 6) after oral administration with a linearity range of 50.0 –400.0 ng mL −1 (R 2 = 0.9931), a detection limit of 12.0 ng mL −1 and extraction recovery of 97.27–99.89% with an RSD < 2% ( n = 9). Moreover, the selectivity of the proposed approach for analysis of ZOLM in the presence of MET and PARA is demonstrated

Research Authors
Pakinaz Y. Khashaba, Azza H. Rageh, Noha N. Atia, Sally A. El Zohny
Research Date
Research Journal
Journal of Chromatography A
Research Publisher
Elsevier
Research Vol
1651
Research Website
https://doi.org/10.1016/j.chroma.2021.462276
Research Year
2021
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