Characterization and evaluation of the performance of starch and cellulose as excipients for direct compression technique

Purpose: To investigate the influence of two often-used excipients (starch and microcrystalline cellulose) on the physical properties of powder blends and tablets that contain mannitol as diluent.Methods: Powder and powder mixtures of three commonly used excipients (starch, mannitol and microcrystalline cellulose) were thoroughly examined using the angle of repose for flowability, particle size analyzer to determine the diameter of the particles, scanning electron microscopy (SEM) for morphological assessment, and x-ray diffraction to determine crystalline/amorphous characteristics. Tablets were prepared by direct compression technique and were evaluated for mechanical strength and disintegration behavior as part of quality control test.Results: The results showed that increase in MCC concentration of the mixture leads to significantly enhanced flowability (p < 0.05) when compared to starch. The angle of repose for mannitol/MCC powder mixture with 70 % w/w MCC was approximately 29°, indicating good flow properties of thepowder mix. Moreover, starch tablets containing MCC exhibited better mechanical strength and longer disintegration time, while, at 1:1 ratio of MCC and mannitol, tablet disintegration was faster (33.0 ± 5.2s)Conclusion: MCC (at 30 %w/w in the blend) produces optimal flow of the powder blend and superior mechanical strength, Keywords: Tablet disintegration, Flowability, Starch, Hardness, Mechanical strengt

Investigation of the cardiac depressant effect of Caralluma tuberculate N.E.Br on isolated rabbit heart

Purpose: To investigate the histopathological and cardiac depressant effect of the aqueous methanol extract of Caralluma tuberculata N.E. Br (AMECT) (family: Asclepiadaceae)’ and to determine if there is a scientific basis for its cardiovascular diseases-related folkloric use. Methods: The effect of AMECT in different concentrations ranging from 0.00001 to 1.0 mg/mL were evaluated in isolated perfused rabbit heart to assess their effect on the force of contraction and heart rate using Langendorff’s apparatus. Atropine and adrenaline were used to identify the underlying mechanism of response produced by AMECT. The extract was studied for its possible mechanism in the absence and presence of atropine and adrenaline. In addition, sub-chronic toxicity and histopathological study of heart tissues in rats were assessed by administering 500 mg/kg of extract. Results: At all concentrations, AMECT produced significant (p < 0.001) negative ionotropic and negative chronotropic effects. The most significant effect was observed at 0.001 mg/mL and higher concentrations hence 0.001 mg/mL was selected for further studies. Pre-incubation with atropine did not significantly inhibit the effects of AMECT. However, AMECT significantly (p < 0.01) blocked the cardiac stimulant effect of adrenaline. In the histopathological studies, AMECT did not produce any significant cellular changes or signs of toxicity in the sub-chronic toxicity study. Conclusion: The cardiac-depressant responses of AMECT may involve the β-adrenergic receptors in the myocardium of isolated rabbit heart thus confirming the rationale for its use in ethnomedicine for cardiac diseases

Investigation of anti-nociceptive, anti-inflammatory potential and ADMET studies of pure compounds isolated from Isodon rugosus Wall. ex Benth

The strong ethnopharmacological utilization of Isodon rugosus Wall. Ex. Benth is evident in the treatment of several types of pain and inflammation, including toothache, earache, abdominal pain, gastric pain, and generalized body pain and inflammation. Based on this background, the antinociceptive effects of the crude extract, various fractions, and essential oil have been reported previously. In this research work, we isolate and characterize pure bioactive compounds from I. rugosus and evaluate possible mechanisms using various in vivo and in vitro models. The pure compounds were analyzed for analgesic and anti-inflammatory activities through various assays. The column chromatography of the chloroform fraction of I. rugosus led to the identification of two pure compounds, i.e., 1 and 2. Compound 1 demonstrated notable inhibition (62% writhing inhibition, 72.77% COX-2 inhibition, and 76.97% 5-LOX inhibition) and anti-inflammatory potential (>50% paw edema inhibition at various intervals). The possible mechanism involved in antinociception was considered primarily, a concept that has already been elucidated through the application of naloxone (an antagonist of opioid receptors). The involvement of adrenergic receptors was investigated using a hot plate model (an adrenergic receptor antagonist). The strong ethnomedicinal analgesic background of I. rugosus, supported by previous reports and current observations, leads to the conclusion that I. rugosus is a potential source of antinociceptive and anti-inflammatory bioactive compounds. It may be concluded from the results that the isolated analgesic compounds of I. rugosus may be a possible alternative remedy for pain and inflammation management with admirable efficacy and safety profiles

Psychological factors behind taking the coronavirus COVID-19 vaccine and associated symptoms for a sample of people in Saudi Arabia

The study aimed to examine the psychological factors behind taking the COVID-19 vaccine and the associated symptoms for a sample of people in Saudi Arabia. The descriptive approach was used. The questionnaire was applied to collect data from a sample of (520) members of the Saudi community who received the COVID-19 vaccine (three doses) in Najran, Saudi Arabia in the year 2022. Their ages ranged between (20-50) years. The sample was selected following the convenience method from different classes of society (students, employees). The results showed statistically significant differences between the distribution of the observed and expected values of the study sample’s responses about the psychological factors behind taking the coronavirus COVID -19 vaccine, and in favor of the observed values (yes). The most important psychological factors were as follows: collective responsibility, restrictions, trust, conviction, and credit. Also, it was shown that the most common and frequent symptoms in the first, second, and third doses, respectively: pain, swelling and redness at the vaccination site, high fever, body pain and fatigue, However, symptoms such as vomiting, diarrhea and headach

Incorrect beliefs about traditional medicine for malignant and chronic diseases and disabilities among members of saudi society

The study aimed to explore incorrect beliefs about traditional medicine for malignant and chronic diseases and disabilities among members of the Saudi society and their relationship to some demographic variables. The study used the descriptive approach. The study sample consisted of (560) persons who were chosen following purposefully from members of the Saudi society in Najran region in the Kingdom of Saudi Arabia in February of the year 2022. A questionnaire was used to collect the data. The results showed that 65.5% of the study sample did not resort to traditional medicine in treating malignant and chronic diseases and disabilities, while 34.5% of the study sample turned to traditional medicine. Also, it was shown that the total degree of wrong beliefs about traditional medicine for malignant and chronic diseases and disabilities among members of the Saudi society came with a mean of (1.14) rating low level. In addition, the results revealed statistically significant differences in the incorrect beliefs about the traditional medical treatment of malignant and chronic diseases and disabilities among members of the Saudi society due to the variables of gender in favor of females

Kinetics and thermodynamics of enhanced adsorption of E120 dye using activated carbon

Purpose: To study the adsorption of dye (E120) from aqueous solution onto activated carbon. Method: Factors influencing adsorption were examined and optimized. Three adsorption isotherm models (Langmuir, Freundlich and Temkin) were investigated. Agitation time was set at 72 hours, E120 dye concentration at 10 – 80 mg/L, pH at 7, temperature at 25°C and mass at 125 mg. Results: Adsorption of E120 dye onto activated carbon was enhanced by decreasing the mass of activated carbon, pH and ionic strength of the solution and by increasing the temperature. Under optimal conditions, the maximum adsorption capacity of activated carbon for E120 dye was 10.1 mg/g at 30°C. The model parameters were 0.307 L/mg (KL), 10.1 mg/g (qm), 0.9491 (R2) for the Langmuir isotherm; 2.98 (n), 0.445 mg/g (Kf), and 0.6592 (R2) for Freundlich isotherm; and 4.59 mg/L (A), 2.23 J/mol (B), and 0.5914 (R2) for Temkin isotherm. Thermodynamic studies indicate that the adsorption of E120 dye onto activated carbon is an endothermic process with an adsorption enthalpy (ΔH) of 8.7 KJ/mol. The positive values for ΔG indicate that adsorption was non-spontaneous. The kinetic study of E120 dye adsorption showed that the adsorption process obeyed pseudo-second order kinetics. Conclusion: Commercially available activated carbon, in terms of its physical and chemical characteristics, is a superior adsorbent to other adsorbents mentioned in the literature for removal of toxic dye E120 from aqueous solutions at a high removal capacity

Design, Synthesis, and Biological Evaluation of a Novel VEGFR-2 Inhibitor Based on a 1,2,5-Oxadiazole-2-Oxide Scaffold with MAPK Signaling Pathway Inhibition

Over the past few decades, the development of broad-spectrum anticancer agents with anti-angiogenic activity has witnessed considerable progress. In this study, a new series of pyrazolo[3,4-d]pyrimidines based on a phenylfuroxan scaffold were designed, synthesized, and evaluated, in terms of their anticancer activities. NCI-60 cell one-dose screening revealed that compounds 12a–c and 14a had the best MGI%, among the tested compounds. The target fluorinated compound 12b, as the most active one, showed better anticancer activity compared to the reference drug sorafenib, with IC50 values of 11.5, 11.6, and 13 µM against the HepG-2, A2780CP, and MDA-MB-231 cell lines, respectively. Furthermore, compound 12b (IC50 = 0.092 µM) had VEGFR-2-inhibitory activity comparable to that of the standard inhibitor sorafenib (IC50 = 0.049 µM). Furthermore, the ability of compound 12b in modulating MAPK signaling pathways was investigated. It was found to decrease the level of total ERK and its phosphorylated form, as well as leading to the down-regulation of metalloproteinase MMP-9 and the over-expression of p21 and p27, thus leading to subG1 cell-cycle arrest and, thus, the induction of apoptosis. Additionally, compound 12b decreased the rate of wound healing in the absence of serum, in comparison to DMSO-treated cells, providing a significant impact on metastasis inhibition. The quantitative RT-PCR results for E-cadherin and N-cadherin showed lower expression of the neuronal N-cadherin and increased expression of epithelial E-cadherin, indicating the ability of 12b to suppress metastasis. Furthermore, 12b-treated HepG2 cells expressed a low level of anti-apoptotic BCL-2 and over-expressed proapoptotic Bax genes, respectively. Using the DAF-FM DA fluorescence probe, compound 12b produced NO intracellularly as efficiently as the reference drug JS-K. In silico molecular docking studies showed a structural similarity through an overlay of 12b with sorafenib. Interestingly, the drug-likeness properties of compound 12b met the expectations of Pfizer’s rule for the design of new drug candidates. Therefore, this study presents a novel anticancer lead compound that is worthy of further investigation and activity improvement

Fabrication and Characterization of Acute Myocardial Infarction Myoglobin Biomarker Based on Chromium-Doped Zinc Oxide Nanoparticles

In this article, we describe the fabrication and characterization of a sensor for acute myocardial infarction that detects myoglobin biomarkers using chromium (Cr)-doped zinc oxide (ZnO) nanoparticles (NPs). Pure and Cr-doped ZnO NPs (13 × 1017, 20 × 1017, and 32 × 1017 atoms/cm3 in the solid phase) were synthesized by a facile low-temperature sol-gel method. Synthesized NPs were examined for structure and morphological analysis using various techniques to confirm the successful formation of ZnO NPs. Zeta potential was measured in LB media at a negative value and increased with doping. XPS spectra confirmed the presence of oxygen deficiency in the synthesized material. To fabricate the sensor, synthesized NPs were screen-printed over a pre-fabricated gold-coated working electrode for electrochemical detection of myoglobin (Mb). Cr-doped ZnO NPs doped with 13 × 1017 Cr atomic/cm3 revealed the highest sensitivity of ~37.97 μA.cm−2nM−1 and limit of detection (LOD) of 0.15 nM for Mb with a response time of ≤10 ms. The interference study was carried out with cytochrome c (Cyt-c) due to its resemblance with Mb and human serum albumin (HSA) abundance in the blood and displayed distinct oxidation potential and current values for Mb. Cr-doped ZnO NP-based Mb biosensors showed 3 times higher sensitivity as compared to pure ZnO NP-based sensors

Green Synthesis and Characterization of Iron Nanoparticles Synthesized from Aqueous Leaf Extract of Vitex leucoxylon and Its Biomedical Applications

The cold extraction method was used to obtain the aqueous extract of Vitex leucoxylon leaves in a ratio of 1:10. Iron nanoparticles (FeNPs) were synthesized using aqueous leaf extract of V. leucoxylon as a reducing agent. The phytoreducing approach was used to make FeNPs by mixing 1 mL of plant extract with 1 mM of ferric sulfate. Scanning electron microscopy (SEM), Fourier-transform infrared spectroscopy (FTIR), Ultraviolet–visible spectroscopy (UV-Vis), and energy-dispersive X-ray spectroscopy were used to examine the synthesized FeNPs. The reducing reaction was shown by a change in the color of the solution, and the formation of black color confirms that FeNPs have been formed. The greatest absorption peak (max) was found at 395 nm in UV-Vis spectral analysis. The FTIR spectra of V. leucoxylon aqueous leaf extract showed shifts in some peaks, namely 923.96 cm−1 and 1709.89 cm−1, with functional groups carboxylic acids, unsaturated aldehydes, and ketones, which were lacking in the FTIR spectra of FeNPs and are responsible for FeNPs formation. FeNPs with diameters between 45 and 100 nm were observed in SEM images. The creation of FeNPs was confirmed by EDX, which shows a strong signal in the metallic iron region at 6–8 Kev. XRD revealed a crystalline nature and an average diameter of 136.43 nm. Antioxidant, anti-inflammatory, cytotoxic, and wound healing in vitro tests reported significant activity of the FeNPs. The cumulative findings of the present study indicate that the green synthesis of FeNPs boosts its biological activity and may serve as a possible dermal wound-healing agent and cytotoxic agent against cancer. Future study is needed on the identification of mechanisms involved in the synthesis of FeNPs by V. leucoxylon and its biomedical applications

A Reliable Auto-Robust Analysis of Blood Smear Images for Classification of Microcytic Hypochromic Anemia Using Gray Level Matrices and Gabor Feature Bank

Accurate blood smear quantification with various blood cell samples is of great clinical importance. The conventional manual process of blood smear quantification is quite time consuming and is prone to errors. Therefore, this paper presents automatic detection of the most frequently occurring condition in human blood—microcytic hyperchromic anemia—which is the cause of various life-threatening diseases. This task has been done with segmentation of blood contents, i.e., Red Blood Cells (RBCs), White Blood Cells (WBCs), and platelets, in the first step. Then, the most influential features like geometric shape descriptors, Gray Level Co-occurrence Matrix (GLCM), Gray Level Run Length Matrix (GLRLM), and Gabor features (mean squared energy and mean amplitude) are extracted from each of the RBCs. To discriminate the cells as hypochromic microcytes among other RBC classes, scanning is done at angles (0∘, 45∘, 90∘, and 135∘). To achieve high-level accuracy, Adaptive Synthetic (AdaSyn) sampling for imbalance learning is used to balance the datasets and locality sensitive discriminant analysis (LSDA) technique is used for feature reduction. Finally, upon using these features, classification of blood cells is done using the multilayer perceptual model and random forest learning algorithms. Performance in terms of accuracy was 96%, which is better than the performance of existing techniques. The final outcome of this work may be useful in the efforts to produce a cost-effective screening scheme that could make inexpensive screening for blood smear analysis available globally, thus providing early detection of these diseases