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   2021| April-June  | Volume 20 | Issue 2  
    Online since June 30, 2021

 
 
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REVIEW ARTICLE
Oral disintegrating tablets: best approach for faster therapeutic action of poorly soluble drugs
Kusuma Anusha, Santosh K Rada
April-June 2021, 20(2):105-114
DOI:10.4103/epj.epj_63_20  
Drug carrier networks are sophisticated because pharmaceutical scientists gain a greater understanding of the performance of biochemical as well as physicochemical parameters. Oral disintegrating tablets (ODTs) are now more commonly available for the treatment of various diseases than other products. Due to its convenience in terms of manufacture and administration, the oral administration route is being studied as the most utilized route. ODTs, particularly for pediatric patients, are considered to be effective drug-delivery systems due to their quick disintegration properties, water-free usage, and ease of swallowing. ‘Orally disintegrating tablets’ are present in solid dosage forms that dissolve in the mouth in less than 60 s without the need for water. Rapid tablet disintegration leads to rapid dissolution and therefore rapid action. ODTs are an ideal treatment for specific populations such as unconscious patients, bedridden patients, dysphagic patients, psychotic patients, geriatric patients, pediatric patients, and young patients with underdeveloped nervous and muscular systems. The main aim of this research paper is to discuss the advantages, drawbacks, formulation problems, manufacturing methods, patented technology, evaluation tests, and marketed formulations of ODTs, their value, different technologies, ideal characteristics, and aspects of formulation and design, future perspectives, and marketed preparations, particularly for pediatric patients.
  2,233 285 -
ORIGINAL ARTICLES
Influence of Melissa officinalis methanolic extract on hyperthyroidism in a rat model
Fathia A Mannaa, Khaled G Abdel-Wahhab, Laila K Hassan, Rehab F Taher, Fatma A Morsy, Nevein N Fadl
April-June 2021, 20(2):134-144
DOI:10.4103/epj.epj_60_20  
Background and objective Thyroid disease represents the most common endocrine abnormality in recent years. This study was conducted to evaluate the effect of Melissa officinalis methanolic extract (MME) on hyperthyroidism in a rat model. Materials and methods Hyperthyroidism was induced by daily subcutaneous injection of L-thyroxine (250 μm/kg body weight) for 14 days. Total phenolic compounds in extract and the in-vitro antioxidant activity of extract were determined. Moreover, identification of methanolic extract component of Melissa officinalis leaves (MME) was done using liquid chromatography–mass spectrometry. After 30 days of MME treatments, blood samples were collected for further biochemical determinations. Liver and kidney were excised for the determination of oxidative stress markers. Thyroid gland was also removed for histopathological examination. Results Various thyroid hormones (total and free triiodothyronine, as well as total and free thyroxine) were seriously affected and increased significantly with hyperthyroidism induction. Significant increases in serum glucose, interleukin-6, and interleukin-8 were detected in hyperthyroid group compared with control values, whereas hemoglobin level has not changed. Compared with control group, hyperthyroidism-induced glutathione depletion and reduction in glutathione peroxidase activity in the liver and kidney tissues, with significant increase in the lipid peroxidation and nitric oxide levels. Upon treatment with MME, significant improvements in thyroid hormones and the other aforementioned parameters were achieved. MME succeeded also in ameliorating the histological picture of the thyroid gland. Conclusions Current results indicate that MME treatment counteracts the oxidative stress induced by L-thyroxine and protects the liver and kidney and regulates blood glucose in hyperthyroidism state. We suggest that MME treatment may be considered for therapeutic use for hyperthyroidism.
  2,191 219 -
Hepatoprotective activity of hydroalcoholic extract of Cissampelos pareira linn. leaves against CCl4-induced acute and chronic hepatotoxicity
Mohammad Asif, Jayesh Dwivedi, Sandeep Yadav, Chandra Kala
April-June 2021, 20(2):126-133
DOI:10.4103/epj.epj_57_20  
Background and objective Cissampelos pareira L. is a medicinal plant distributed across the tropics and used across the world traditionally for curing various pathological conditions. Hence, the present study has been carried out to evaluate the hepatoprotective effect of hydroalcoholic extract of C. pareira L. Materials and methods C. pareira L. leaves were extracted with a hydroalcoholic solvent. The resulting extract was subjected to an acute oral toxicity test on the basis of the OECD 423 guideline. Afterward, the selected dose of C. pareira hydroalcoholic extract (CPHE) was checked for hepatoprotective activity against CCl4-induced acute and chronic hepatotoxicity. Measurements of serum glutamic oxaloacetic transaminase, serum glutamic pyruvic transaminase, total bilirubin, and direct bilirubin were performed. At the end of the study, histopathological analysis of livers of the animals of various treatment groups was carried out. Result and conclusion Based on the acute oral toxicity study, three doses of CPHE were selected, namely, 100, 200, and 400 mg/kg. Administration of CPHE at 200 and 400 mg/kg prevented an increase in serum glutamic oxaloacetic transaminase, serum glutamic pyruvic transaminase, and bilirubin levels against CCl4-induced hepatotoxicity. The histopathological investigation of the portal triad structure of the liver clearly indicated that CPHE at 400 mg/kg showed significantly greater reduction in the necrotized area and normal appearance of the central vein, Kupffer cells and hepatocyte cells with no inflammatory cells. The results indicated that CPHE at 400 mg/kg protected the hepatic cells’ membrane integrity against CCl4-induced hepatotoxicity.
  1,354 192 -
Biological activity and investigation of some active constituents with molecular docking from two Cleome species
Wael Abdullah, Wael M Elsayed, Khaled A Abdelshafeek, Naglaa M Nazif, Nasser S.M Ismail, Shams I Ismail, Abdel N.B Singab, Somaia A Nada
April-June 2021, 20(2):115-125
DOI:10.4103/epj.epj_47_18  
Objective Cleome genus belonging to Cleomeaceae family is used as an antidiabetic agent in Egyptian folk medicine. The current study aimed to isolated and identify the active constitutes of two species, Cleome africana and Cleome droserifolia, and to study the biological activities, such as antidiabetic, anti-inflammatory, and hepatoprotective. Materials and methods The lipid constituents of two plant species, C. africana and C. droserifolia, were extracted with petroleum ether and fractionated to acetone-insoluble fraction and acetone-soluble fraction. Molecular docking studies were carried out in isolated compounds. Antidiabetic, anti-inflammatory, and hepatoprotective activities of the promising compounds were investigated. Results and conclusion The fatty alcohols and hydrocarbons were identified from the acetone-insoluble fraction. C. africana comprises four fatty alcohols, in which tetratetracontanol is the main one, whereas C. droserifolia consists of two fatty alcohols, in which dotriacontanol is the main one. The hydrocarbons include seven compounds, with tritriacontane as the main one in both species. The acetone-soluble fraction was saponified to afford the unsaponifiable fraction, which contains in C. africana a series of n-alkanes from n-C14 to n-C31, representing 93.66%, with n-C22 as the main one, in addition to a sterol fraction, forming 5.13%, in which β-sitosterol is the main compound, and the fraction of C. droserifolia was found to contain a series of n-alkanes from n-C18 to n-C30, representing 60.46%, in which n-C30 is the main compound, besides sterols, representing about 39.54%, with campesterol as a major compound (12.46%), and finally, a triterpene fraction consisting of α-amyrin and β-amyrin. In addition, fatty acids as a mixture of eight acids (saturated and unsaturated) were found in both species; the major two acids are linoleic acid (38.99%) and palmitic acid (33.05%). Extraction of the glucosinolate (GL) constituents from the methanolic extract of C. africana led to isolation and identification of one compound (G), identified as 3-ethylsulfonyl-2,3-dimethoxypropyl GLs. Enzymatic hydrolysis of the total GLs allowed us to identify eight isothiocyanate and two thione compounds. Molecular docking of compound G with glucosidase enzyme using C-DOCKER protocol resulted in having higher docking scores relative to the lead molecule and the ligand (Glimepiride). Accordingly, molecular docking studies proved that the molecule of G compound has a promising active hits and can be used as antidiabetic through glucosidase inhibitor and also different extracts exhibited an anti-inflammatory and hepatoprotective activity.
  1,354 190 -
Synthesis, characterization, and functional properties of a novel sodium carboxymethyl starch obtained from matured seeds of Brachystegia eurycoma
Elizabeth Atuchukwu, Musiliu Adedokun, Martins Emeje
April-June 2021, 20(2):145-156
DOI:10.4103/epj.epj_61_20  
Background and objective Brachystegia eurycoma is an indigenous but underutilized legume crop in Nigeria. The aim of this study was to extract, purify, chemically modify, and characterize for its material and functional properties the starch from matured seeds of B. eurycoma and determine its suitability as an excipient in solid oral dosage formulations. Materials and methods Starch was extracted, purified, and subjected to carboxymethylation using modified methods. Micromeritic and rheological properties of the starch products were evaluated using differential scanning calorimetry, powder radiograph diffraction (XRD), Fourier-transform infrared spectroscopy, scanning electron microscopy, and thermogravimetric analysis techniques, which were used to characterize the preparations. Granules were prepared using the method of wetting and massing. The bulk properties, solubility, and the disintegrant properties were evaluated in isoniazid capsules and tablets. Results and discussion The results show good compressibility and excellent flow of the modified starch. The solubility of the modified starch was increased by 2–10 folds, whereas the swelling capacity of the native starch was increased up to 9.0–16 times. Both differential scanning calorimetry and XRD results have shown a reduction of crystallinity, whereas the Fourier-transform infrared spectroscopy indicated formation of carbonyl functional group and absence of interactions. Scanning electron microscopy revealed eruption and coalescence of starch granules after modification. XRD showed decreased thermal stability, and thermogravimetric analysis showed product decomposition at lower temperatures than the native starch. Disintegration was found to be faster with lower concentration of carboxymethylated starches. Conclusion The study concludes that derivatization of carboxymethylated starch from B. eurycoma seed yielded starch products with unique functional properties that could be explored for the formulation of controlled-release systems.
  1,333 175 -
Ameliorating and anti-inflammatory role of Balanites aegyptiaca aqueous extract on Doxorubicin-induced hepatotoxicity in male Wistar rats
Hanaa F.A Elkareem, Abd El-Naby I Essawy, Mahmoud Ashry, Manal A Badawi, Khaled G Abdel-Wahhab
April-June 2021, 20(2):157-165
DOI:10.4103/epj.epj_2_21  
Background and objective Doxorubicin (Doxo) is an antibiotic that used in cancer treatment, with many complications like hepatotoxicity. The objective of this study was to explore the ameliorative effect of Balanites aegyptiaca aqueous extract (BAE) against Doxo-induced hepatotoxicity in male rats. Materials and methods Adult male Wistar rats (140–160 g) were randomly divided into six groups (10 animals each) as follows: group I, normal rats act as a control group; group II, rats ingested with BAE (200 mg/kg) for 4 weeks; group III, rats intoxicated (intraperitoneal) with Doxo (0.5 mg/kg) for 4 weeks; group IV, rats ingested with BAE in combination with Doxo injection for 4 weeks; group V, rats ingested with BAE for 4 weeks before Doxo injection for another 4 weeks; and group VI, rats ingested with BAE for 4 weeks after Doxo injection. Results The results revealed all BAE regimens succeeded to decrease the hepatotoxicity induced by Doxo. This was evidenced by the significant reduction of serum alanine aminotransferase, aspartate aminotransferase, alkaline phosphatase, bilirubin, urea, creatinine, tumor necrosis factor alpha, and interleukin-1beta levels, as well as hepatic malondialdehyde and nitric oxide levels. Moreover, a marked increase was observed in serum protein and albumin levels, as well as hepatic-reduced glutathione, superoxide dismutase, and catalase values. The obvious histopathological regenerations came in line with both serum and tissue biochemical findings. The Doxo-BAE combined regimen exhibited the highest potential of amelioration. Conclusion As a promising supplement, BAE exhibited hepatoprotective potential against Doxo-induced hepatic injuries; this could be mechanized through its antioxidant and radical scavenging exhibition of its bioactive constituents.
  1,053 161 1
FTIR spectroscopy used for study the thermal degradation of lard
Andrei A Bunaciu, Serban Fleschin, Hassan Y Aboul-Enein
April-June 2021, 20(2):166-172
DOI:10.4103/0003-2778.320252  
Aim Recent developments in Fourier transform infrared (FTIR) spectroscopy instrumentation extend the application of this technique to the field of food research, in particular facilitating studies on edible oils and fats. Materials and methods In this work, an attenuated total reflection-FTIR spectroscopy method was used as an effective analytical tool to monitor the oxidation process of lard samples during heating. The process was interpreted according to the peaks data. Results and discussion FTIR spectroscopy has been found to be a versatile technique for evaluating the oxidative stability of lard and for providing information on the oxidation degree of a sample in a simple, fast and accurate way. To follow the oxidation process during the period of frying, about 40 min, the samples were subjected to increasing heat up to a temperature of 300°C, and samples were withdrawn every 10 min. Attenuated total reflection spectra were obtained and the process was interpreted according to the peaks data modifications. Conclusion FTIR spectroscopy has been found to be a versatile technique for evaluating the oxidative stability of lard and for providing information on the oxidation degree of a sample in a simple, fast, and accurate way. A slight decrease in the intensity was observed for the band at 721 cm−1, which implies the loss of cis double bonds during oxidation, a fact also confirmed by the decrease in intensity at 3006 cm−1, assigned to the same cis-double bonds in C=CH.
  584 118 -
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