Coronavirus disease-2019 is a serious health threat around the globe. Across the world, approximately 142 million people were infected, and three million deaths happened. The fast propagation is also associated with constant anxiety, mental stress, and discomfort in public and health-care professionals. Lack of approved drugs regimen to combat the pandemic challenge concretely is a challenging project for all who are committed to developing remedial assistance. However, the successful development of three vaccines gives a solid roadmap to combat this disease. In this review, we highlighted the current development and challenges of this pandemic.

Pyrazoline plays an important role in the development of heterocyclic chemistry theory and is widely used as a synthesis useful in organic synthesis. The structure of the pyrazoline derivative compound contains a 5-membered heterocyclic framework with two nitrogen atoms and one endocyclic double bond. The function of pyrazoline as a fragment was stable enough in the bioactive group to synthesize new compounds with various biological activities. Various methods that could be used for the synthesis of pyrazole derivatives were ultrasonic irradiation, microwave assistance, ionic liquids, grinding techniques, and conventional methods. However, the synthesis of pyrazoline derivatives using conventional methods had many problems, one of which is the product yield, which was <70%. Therefore, this article will discuss the importance of optimizing the synthesis reaction conditions by taking into account several synthesis parameters to get the best organic product results based on conventional methods. A literature search was conducted by employing PubChem, Chemspider Google Scholar, Research Gate, Science Direct, and Elsevier by selecting pyrazoline synthesis based on physicochemical profile, reaction mechanism, and synthesis method.

Plants have been used as traditional medicine since ancient times for treating the diseases, metabolite active compounds from plants have excellent bioactivity, and pharmacological properties from plants are used as skin whitening agent and antioxidant in multiple mechanisms of action. However, these compounds have physicochemical limitations in terms of its poor solubility and penetration into the cells membrane. Phytosome drug delivery system can be the primary choice to improve the physicochemical properties, which allows increasing the effectiveness. This review aimed to summarize and discuss the phytosome formulations of potential active compounds as skin whitening agent and skin antioxidant, which obtained from Scopus, PubMed, and Google Scholar databases. We assessed that the main purpose of these phytosome formulations was to improve penetration, stability, and solubility of the active compounds. These studies proved that phytosome formulations can improve the physicochemical characteristics and effectiveness of compounds. The phytosome drug delivery system becomes a promising modification technique for natural compounds due to the ability to improve the physicochemical properties and increase the effectiveness. Phytosome formulation could be the excellent approach for cosmeceutical product with good effectivity in the future.

Fermented foods and drinks derived from animals as well as plants play an important role in diets. These foods usually contain lactic acid bacteria (LAB) grown during fermentation, and these naturally contain compounds, including organic acids, ethanol, or antimicrobial compounds with the ability to inhibit spoilage organisms and pathogenic bacteria in fermented foods. Furthermore, these bacteria are able to adapt well to the spontaneous fermentation process and play a role in human as well as animal health, especially in digestive tract, commonly known as probiotics. This study therefore aims to describe the microorganisms produced by fermented foods suitable for development as probiotics to improve human health, as these generally have the ability to improve the immune system against pathogenic bacteria. Several genera are used as probiotics, including Lactobacillus, Bifidobacterium, Bacillus, Pediococcus, and several yeasts. Therefore, LAB produced from fermented foods were concluded to be suitable potential candidates for probiotics, to replace antibiotics in overcoming pathogenic bacteria, and to possess the ability to improve the immune system and strengthen the body against pathogenic bacteria.

Origanum syriacum (O. syriacum) (L.) belongs to Group B of the genus Origanum from (Lamiaceae), which is rich in essential oils that exhibit antimicrobial efficacy, anti-inflammatory efficacy, antioxidant activity, and antitumor efficacy. These processing activities are because of its richness in carvacrol and Thymol. In this article, we will focus on O. syriacum, discussing the antimicrobial efficacy for its essential oil and extracts, in addition, cast light on mechanism of essential oil antimicrobial action. This study was conducted from March 2019 to February 2021. We have analyzed the results of studies on antimicrobial efficacy of a plant O. syriacum in the PubMed, Google Scholar, Elsevier over the past 15 years using keywords. O. syriacum essential oil and its extracts have an extensive antimicrobial efficacy give it a great importance in pharmaceutical and medical purposes.

Skin permeation is an integral part of penetration of topical therapeutics. Zero order in addition to Higuchi permeation kinetic is usually preferred in topical drug delivery cargo. Penetration of therapeutic entities through epidermal barrier is a major challenge for scientific fraternity. Furthermore, penetration of therapeutic entities determines the transportation and ultimately therapeutic efficacy of topical dermal dosage forms. Apart from experimentation models, mathematical equations, in silico docking, molecular dynamics (MDs), and artificial neural network (Neural) techniques are being used to assess free energies and prediction of electrostatic attractions in order to predict the permeation phenomena of therapeutic entities. Therefore, in the present review, we have summarized the significance of kinetic equations, in silico docking, MDs, and ANN in assessing and predicting the penetration behavior of topical therapeutics through dermal dosage form. In addition, the role of chitosan biomacromolecule in modulating permeation of topical therapeutics in skin has also been illustrated using computational techniques.

Tobramycin remains the anchor drug for bacterial keratitis treatment and management; however, unlike other aminoglycosides, it does not pass through the gastrointestinal tract. The aim of the current investigation was to formulate tobramycin-loaded nanostructured liquid crystalline particles as an ophthalmic drug delivery system to ameliorate its preocular residence duration and ophthalmic bioavailability. Tobramycin cubosomes were fabricated by liquid–lipid monoolein, water, and poloxamer 407 as a stabilizer. Corneal penetration studies exhibited that the apparent permeation coefficient of tobramycin cubosomes was nearly 3.6-fold greater than marketed tobramycin eye drops. Ocular in vivo analysis performed in rabbits' eyes manifested that the intensity of bacterial keratitis was reduced on day 3, and on day 5, the manifestations were considerably mitigated with tobramycin cubosomes as compared to marked eye drops. Pharmacokinetic study of rabbit aqueous humor demonstrated that the area under curve and the peak concentration of optimized cubosomes were 3.1-fold and 3.3-fold, respectively, which was significantly higher than marketed eye drops. Moreover, histopathological studies illustrated the existence of normal ocular structures, thus indicating that there was no damage to the corneal epithelium or stromal layer. Consequently, the results acquired demonstrated that tobramycin-loaded cubosomal formulation could be a propitious lipid-based nanodelivery system that would enhance retention time and corneal permeability contrast to commercial eye drops.

Herbal active compound with immunoregulator ability is considered a potential therapy for COVID-19 oral manifestation by downregulating pro-inflammatory cytokine storm. Meanwhile, anthocyanin and ternatin are the active compounds in Clitoria ternatea, which may act as a potential immunoregulator for COVID-19 therapy. The intention of this investigation was to investigate anthocyanin and ternatin as active compounds in C. ternatea that may be able to increase anti-inflammatory cytokine and inhibit pro-inflammatory cytokine and key proteins of severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2). This study implemented bioinformatic approach to analyze anthocyanin and ternatin as active compounds in C. ternatea with anti- and pro-inflammatory cytokines and antiviral examination history through blind molecular docking study (in silico). Moreover, anthocyanins and ternatin were obtained from PubChem database by minimizing ligand structure in PyRx software to increase the flexibility. RCSB database was employed for preparing the protein samples consisting of interleukin (IL)-6, SARS-CoV-2-ACE2 glycoprotein complex, tumor necrosis factor-α receptor (TNF-αR), matrix metalloproteinase-9 (MMP-9), IL-6, IL-10, and human beta defensin-2 (HBD-2). In addition, The PyMol sofware was used to sterilize the protein samples to obtain the molecular docking optimization. This investigation found that, in the molecular docking simulation, the anthocyanin and ternatin showed producing the negative binding affinity to the ACE2 domain which interacted with RBD glycoprotein SARS-CoV-2. Anthocyanin and ternatin were then predicted to be able to influence any inhibitory activity of TNF-αR, MMP-9, and IL-6; increase IL-10; and increase HBD2 binding affinity values negatively. It can be predicted through molecular docking that anthocyanin and ternatin as the active compounds in C. ternatea contribute as a potential agent for COVID-19 oral manifestation therapy.

Continuing education (CE) is a structured educational activity. Pharmacists must actively participate in CE and is an important part of developing the professional competency of pharmacists. This research focuses on measuring Saudi pharmacists' perception in CE, its impact on professional performance, and the barriers in CE. This was a cross-sectional study, conducted in 2020, using random sample of Saudi pharmacists working in all workplaces from different cities in Saudi Arabia using a questionnaire. The questionnaire consists of 15 questions that assess the perception of Saudi pharmacists toward CE and barriers that prevent them from CE. A total of 409 pharmacists participated in the study. Majority of pharmacists were working in government hospitals (48.4%) and have <2 years of practice experience (44.5%). More than 70% of respondents acknowledged that CE helps to increase their knowledge. The pharmacists mentioned that getting a certificate (23.37%) was the major reason for attending a CE event. The reasons that prevent respondents from attending live CE were cost and work responsibilities (23.59% and 24.57%, respectively). This study reported a subjective assessment of pharmacists' perception toward CE, their lifelong learning experience. Saudi pharmacists showed a great desire for CE because they believed that it greatly affects their professional performance.

The present study evaluated the physicochemical characterization and cytotoxicity activity of chitosan and chito-oligosaccharides (COSs). The extraction of chitosan and COSs was executed by chemical hydrolysis. The physicochemical characterization and deacetylation (DA) value were determined using an FTIR. The molecular weight was determined by using the Mark–Houwink equation. The physical parameters such as solubility, water-binding capacity (WBC), and fat-binding capacity (FBC) were determination as per equation (i), (ii), and (iii) respectively. The cytotoxic activities of chitosan and COS against MCF-7, HepG2, HeLa-6, and 3T3 were performed by MTS assay. The COS induced enhance cytotoxicity with IC₅₀ 0.87 and 2.21 mg/ml against MCF-7 and HepG2 respectively. However, COSs seem to be more sensitive toward the cell lines with the relative potential of MCF-7 > HepG2 > HeLa. Hence, the results showed promising future perspectives of chitosan and COS to develop biodegradable, antibacterial, cytotoxic naturally derived polysaccharides for cancer drug delivery and smart wound dressings.

Dexamethasone sodium phosphate (DSP) is an ester of dexamethasone with anti-inflammatory action. This study provides new insights to develop a simple, precise, and accurate spectrophotometric method for the quantitative determination of DSP in bulk and pharmaceuticals. The method was validated before being applied to determine the DSP in six pharmaceutical injection forms from different companies. DSP is soluble in phosphate buffer, so it was used as a solvent, and a pH of 6 was found to be suitable for determination purposes. The DSP solution was scanned in the ultraviolet range (200–400 nm) using a double-beam spectrophotometer with a 1-cm quartz cell. The wavelength (λ max) of DSP was set at 242.5 nm, following the Beer–Lambert law for concentrations from 2 to 50 μg/ml. Dexa AIWA (Germany) showed the best results, being very close to the bulk value with no significant variation. Similarly, Dexamed (Cyprus) and HEMAZON (Syria) showed no significant differences from the bulk; however, the three remaining injections, DEXAKAL (India), DEXABRU (India), and DEXARON (China), showed significant variations from the bulk. Estimated limit of detection and limit of quantitation values for DSP were 0.83 and 2.5 μg/ml, respectively, with a regression coefficient of 0.999. Recovery studies were then used to determine the accuracy of the suggested method. The percentage of recovery was found to be 98.58%–102.52%. All results are suggesting a pivotal method for the routine analysis of DSP both in pure form and the commercially pharmaceutical forms.

In Indonesia, hypertension is a condition that can lead to death through stroke and TB. Herbs have traditionally been used in Indonesia as an alternative medicine for lowering blood pressure. The leaves of Anredera cordifolia and Sonchus arvensis have been investigated for their antihypertensive potential. Based on the number of treatments, rats were randomized into groups. Each group consists of five rats. The test animals were grouping as follows: the positive control group (hypertension induction without treatment), A. cordifolia 50 mg/kg b.w. group, A. cordifolia 100 mg/kg b.w., S. arvensis 50 mg/kg b.w, S. arvensis 100 mg/kg b.w., A. cordifolia 25 mg/kg b.w + S. arvensis 25 mg/kg b.w, A. cordifolia 50 mg/kg b.w + S. arvensis 50 mg/kg b.w, and atenolol 4.5 mg/kg b.w. The rats were given 0.25 mg/kg b.w. of epinephrine intraperitoneally. The initial, after induction, and final blood pressure of the animals were measured using the CODA^® noninvasive blood pressure device. All animal test groups at T60 showed a significant difference in systolic and diastolic blood pressures to initial blood pressure (T0), P < 0.05. The combination of A. cordifolia 50 mg/kg b.w and S. arvensis 50 mg/kg b.w showed the highest percent inhibition of systolic and diastolic blood pressure. The combination of A. cordifolia and S. arvensis 50–50 mg/kg b.w showed the best effect of lowering systolic and diastolic blood pressure on the pathway of inhibiting adrenergic receptors.

Recently, the antioxidant is applied for the teeth bleaching treatment as an alternative of toxic material of hydrogen peroxide that is used in teeth bleaching. One of natural sources antioxidant is Uncaria gambir those containing active antioxidant agents. To be applied as a new bioactive constituent in teeth bleaching treatment, a preexperimental study is performed. The aim of the study is to identify the antioxidant constituent of U. gambir and predict their activity including action mode as an inhibitor of enzyme superoxide dismutase (SOD) through in vitro and in silico method. Combination of chromatography methods and spectroscopic analysis is used for isolated bioactive antioxidant constituent. The antioxidant activity was evaluated by in vitro assay against diphenylpicrylhydrazyl (DPPH) and SOD, respectively, while prediction of action mode of the active compounds as SOD-mutant enzyme inhibitor was conducted by in silico study using AutoDock 4.2 program. Antioxidant of ursolic acid was isolated from U. gambir with inhibitory concentration₅₀ values 1721 ± 30.6 and 392 ± 53.57 μg/mL, respectively, against DPPH and SOD. By in silico study presented that ursolic acid inhibited SOD enzyme with a binding affinity of − 5.4 kcal/mol those higher than a quercetin as a positive control. The ursolic acid was identified as a potential natural antioxidant with potentially activity to inhibit SOD mutant.

The link between chronic obstructive pulmonary disease (COPD) and osteoporosis is unclear and yet to be understood. The study goals were to detect the prevalence of osteoporosis and investigate its predictors among COPD patients. This is a longitudinal study conducted in a tertiary care setting. During the study, patients' bone mineral density was checked, pulmonary parameters were recorded, and a risk assessment tool was validated. Based on T-score, more than 50% of subjects were osteoporotic. Spirometric parameters were significantly lower among osteoporotic patients. For the risk assessment tool, a cutoff point of 34 made the optimum balance between sensitivity and specificity (0.867 and 0.087, respectively) with a generated area under the curve of 0.934. Severe COPD patients were four times at higher risk of getting osteoporosis, forced expiratory volume (FEV) % predicted, and FEV/forced vital capacity was inversely related to the risk of osteoporosis. Patients with severe dyspnea had twice the risk of getting osteoporosis. Osteoporosis was prevalent among COPD patients, and severe COPD patients were at higher risk of getting osteoporosis.

Herein, chitosan nanoparticles (CS-NPs) were prepared and functionalized chemically with titanium dioxide nanoparticles (TiO₂-NPs) to allow on-demand degradation of CS-NPs, using ultraviolet (UV) irradiation as a trigger. This is expected to allow drug release depending on patients' needs or physiological circumstances. Eleven formulations were arranged and their particle size, charge, and polydispersity were determined. The effect of CS-NPs size and the amount of TiO₂-NPs, on the system collapse, was studied accordingly. Moreover, the collapse of these systems was examined using a fluorescence microscope after loading CS-NPs with Rhodamine. The formulations showed high monodispersity and had sizes ranged between 170 and 440 nm and charges ranged between +5 and +34 mV. Scanning electron microscope, Fourier-transform infrared spectroscopy, and X-ray diffraction proved the chemical deposition of TiO₂-NPs on CS-NPs. The dye test showed that there are two factors that oppose each other and affected the deposition of TiO₂-NPs on CS-NPs, the size of CS-NPs, and the amount of TiO₂-NPs used. In addition, the dye test showed that the deposition of TiO₂-NPs is a saturated process that relies on the amount of TiO₂-NPs used initially. Finally, the intensity of Rhodamine released from these systems after illumination with UV light was related to the amount of TiO₂-NPs deposited on CS-NPs. In conclusion, functionalization of CS-NPs with TiO₂-NPs can be controlled and used to rupture CS-NPs on demand by illumination with UV light.

Sildenafil is a specific inhibitor of the phosphodiesterase type 5 (PDE-5) enzyme that protects cyclic guanosine monophosphate from breakdown by PDE-5. It is a biopharmaceutical categorization system Class II medication with low bioavailability because it is almost insoluble in water. The objectives of this study were to prepare sildenafil cocrystals with co-former molecules including aspirin (acetylsalicylic acid [ASA]), fumaric acid (FMA), and benzoic acid (BZA) to improve the water solubility of sildenafil. The cocrystals were prepared by antisolvent addition (AA) and slow solvent evaporation (SE) methods. The stoichiometric ratios of sildenafil and co-former molecules were varied. The obtained crystals were characterized by stereomicroscope, Fourier transformed infrared spectroscopy (FT-IR), nuclear magnetic resonance (NMR), and powder X-ray diffraction (PXRD). The water solubility of sildenafil cocrystals was compared with sildenafil base. In the AA method, the crystals only form in sildenafil-ASA reaction. These crystals were not cocrystals between sildenafil and ASA because they were formed to new substances that were confirmed by single-crystal X-ray diffraction. In the SE method, the cocrystals were successfully prepared in the reaction of sildenafil with ASA, FMA, and BZA which use acetone or ethyl acetate as a solvent. The obtained crystals are irregular shapes and their FT-IR, NMR, and PXRD results exhibited the characteristics of sildenafil and its co-former. The stoichiometric ratios of sildenafil and co-formers after cocrystallization were different from an initial of crystallization. The sildenafil cocrystals with ASA, FMA, and BZA by SE method had higher water solubility than sildenafil base. The sildenafil-FMA cocrystals had the highest water solubility and increased up to five times when compared with sildenafil base.

Platelets form a plug to prevent blood loss and contribute to wound healing. Kradonbok, Careya sphaerica Roxb., is a Thai plant with medicinal properties. Conventionally, leaves of C. sphaerica are being used to help wound healing in Thailand. The present study was aimed to investigate the effect of C. sphaerica on the function of platelet. Four different extracts of leaves of C. sphaerica (distilled water, methanol, ethanol, and chloroform extracts) were prepared. The extracts at 5.0 mg/ml per dose were tested for the effect of C. sphaerica on platelet adhesion and aggregation properties, by employing a microtiter plate approach. The phytochemical identification was done by using gas chromatography–mass spectrometry (GC-MS). Our data revealed that chloroform extract significantly activated thrombin-induced platelet adhesion (105.27 ± 0.11%, P < 0.05). None of the extracts exhibited an improvement in platelet aggregation. Further GC-MS analysis of the chloroform extract revealed five key phytochemical constituents with potential platelet activation properties. In conclusion, our study evaluated platelet activation and potentially wound healing property of C. sphaerica. GC-MS analysis identified potential bioactive phytochemical compounds in C. sphaerica which warrant further investigation to characterize these compounds.

Eriocaulon cinereum R. Br is used as traditional medicine by the local community in Bangka Belitung Island, Indonesia. The plant is processed as an infusion for fever, boosts the immune system, and treats tumor cells. However, scientific research on this species is still limited. The aims of this study were to determine the cytotoxic of E. cinereum against MCF-7 cells. The results suggested that one of the compounds has a good cytotoxic activity. Therefore, it is quite promising in the effort of cancer drug discovery. The active compound has a flavonoid, which plays a role in several anticancer mechanisms. This study provided scientific evidence regarding the utilization of E. cinereum by the local community for cancer therapy. The plant can be further developed as an alternative agent to treat cancer or as cancer adjuvant therapy.

Heavy metal impurities in cosmetics are common due to their natural abundance. However, they should be kept to a minimum wherever technically feasible. Although human external contact with a substance rarely results in a significant systemic exposure, local exposure to cosmetics may pose a risk of heavy metal contamination. In this study, we sought to investigate the heavy metal concentration present in various cosmetic products from different brands and qualities that are available in the Saudi Market, also to analyze and compare the determined values relative to the reported permissible levels according to international standards. In this study, we have selected several facial cosmetics from the Saudi market and classified their quality into three main classifications based on their price. This was followed by an analysis and reporting of heavy metal content using an inductively coupled plasma–mass spectrometer. We found that three metals were below the permissible limits (Pb, As, and Cd) for cosmetics according to the Saudi Food and Drug Administration and Canadian Standards, besides (Cr) which was also below the limit of the United States Food and Drug Administration. The level of (Ni) exceeded the recommended range in the three-class classifications. On contrary, Pb, Cr, As, and Cd have all exceeded the acceptable levels based on European standards. Further assessment and careful selection of heavy metals content in cosmetics are urgently needed, as there are fluctuations in values between different international standards which might pose a potential harmful effect to human health from the daily use of cosmetics containing heavy metals impurities.