Journal of Advanced Pharmaceutical Technology & Research最新文献

β-estradiol is an estrogen steroid hormone and acts as an estrogen receptor agonist. Radiolabeled β-estradiol is widely used as a radioligand for binding assays. In this present study, the synthesis of [¹³¹I]β-estradiol has been successfully carried out. Accordingly, the measurement of the radiochemical purity (RCP) value and the presence of chemical impurities are needed. To validate the method for identifying the RCP and chemical impurities from [¹³¹I]β-estradiol using high-performance liquid chromatography (HPLC). The synthesis of [¹³¹I]β-estradiol was accomplished by a radioiodination reaction, and the RCP was determined by radio-HPLC. The method for β-estradiol measurement was validated by reversed-phase HPLC radio-analytical employing ultraviolet-visible (UV-Vis) and radioactive detector. The method for radio-HPLC analysis was validated and established using a C-18 column and MeCN: H₂O (55:45 v/v) as the mobile phase. The following conditions were applied: a flow rate of 1.2 mL/min, isocratic, and a UV-Vis detector at 280 nm. The RCP of [¹³¹I]β-estradiol measured by thin-layer chromatography and radio-HPLC was 99.27% ± 1.25% and 95.75% ± 2.41%, respectively. The validation parameters were appropriate and met the requirements for acceptance. HPLC analysis was able to identify the presence of unlabeled estradiol (24.51%-27.29%) in the mixture of [¹³¹I]β-estradiol. As a result, purification using preparative HPLC or other methods will be required in future studies.

Eleutherine bulbosa bulbs, an endemic plant in Indonesia, have enormous potential as raw materials for pharmaceutical products. Therefore, it is necessary to strengthen and develop extraction methods that are easy, rapid, and efficient to enrich targeted secondary metabolites. This study aims to optimize the microwave-assisted extraction (MAE) method conditions for polyphenol metabolite from E. bulbosa bulbs. The MAE method (with different conditions) was applied to extract total polyphenol content (TPC) from E. bulbosa bulbs. TPC values were determined using a 96-well microplate reader spectrophotometry method and Folin-Ciocalteu reagent. The variables of MAE, as an experimental design-independent variable, were involved. The MAE method condition was optimized using response surface methodology (RSM) and Box-Behnken design based on the TPC value. The MAE condition was optimized with 60% ethanol, sample-solvent ratio of 1:10 g/mL, and 50% Watts of microwave power for 10 min. The quadratic regression analysis was achieved to predict the TPC value using the equation: TPC value = 28.63-5.545A +2.211B -0.741C +1.995D - 4.045AB +0.856AC -7.541BC +1.961CD -8.342A²-0.071B² +1.840C²-1.535D². For the scale-up confirmation test, a 50-g sample was used to prove the validity of the equation to predict the TPC value, yielding 35.33 ± 2.13 mg gallic acid equivalent/g samples. The optimum of the MAE condition recommended based on the results of RSM analysis can be applied directly to the enrichment of polyphenols metabolite constituent of E. bulbosa easily, cheaply, quickly, and efficiently.

Vanillin, an extract from the Vanilla planifolia plant, is reported to possess potent antioxidant properties. The ability of vanillin to protect skin cells from reactive oxygen species (ROS)-induced damage and its potential use in the treatment of wounds were studied. Cytocompatibility and cytoprotective properties against ROS-induced damage were examined using keratinocyte and fibroblast cell models. Vanillin's effect on cell migration was studied using the scratch wound healing assay. Vanillin exhibited cytocompatibility and cytoprotective properties against cell damage induced by ROS. Human keratinocytes and fibroblast cells showed >80% survival when exposed to vanillin (10-500 μM). Both cells showed no evidence of necrosis or apoptosis, which was confirmed by acridine orange/propidium iodide staining. Both examined cells were exposed to 750 μM hydrogen peroxide to cause oxidative stress, and vanillin demonstrated the ability to inhibit ROS-induced cell death. In addition, a considerable increase in cell migration suggested that vanillin had the ability to heal wounds in vitro. Vanillin is safe and potentially useful in wound healing treatments.

Cinnamon is one of the world's oldest spices that is also widely used as medicine for antimicrobe, anti-inflammation, and immune stimulant to now developed as an antidiabetic herbal medicine. Among its bioactive contents, the coumarin must have been controlled; since of its toxicities. Therefore, in this study aimed to reduce the amount of coumarin in the extracts by chloroform preextraction to dried powdered cinnamons and determine their glucose binding capacity. The extractions were used two methods by water infusion and ethanol soxhletation. To measure the coumarin's was used validated thin-layer chromatography (TLC)-densitometry, while for the chemical profiling of the extract was examined with liquid chromatography-mass spectrometry. The activity antidiabetic of the extracts was obtained by glucose binding. The TLC-densitometry method has been validated with silica gel 60F₂₅₄ and n-hexane: ethyl acetate (8:2, v/v) systems. The coumarin's spot was observed at a wavelength of 285 nm on retention factor (Rf) 0.33, with tailings factor 1. The intraday and interday linearities tests showed a linear response result. The recovery value, coefficient of variation, and detection and a quantitation limit were met the standard requirements, respectively. Moreover, the results were observed (1) the solvent preextraction may reduce the coumarin content, (2) the coumarin content in the ethanol extract was higher than in the infusion, and (3) the preextraction solvents would reduce the glucose-binding capacity in ethanol and water cinnamomi's extract. These results may be developed further and applied for producing cinnamon's free coumarin extracts.

The study's goal was to create an in situ intrarectal mucoadhesive gel of sumatriptan (SMT) combining mucoadhesive polymer (xyloglucan) and thermosensitive polymers (poloxamer 407 and poloxamer 188) to prolong rectal residence time for treatment of migraines. Nine SMT mucoadhesive rectal in situ gel (RIG) formulas were created by mixing poloxamer 407 (18%, 19%, or 20%) with poloxamer 188 (5%), a mucoadhesive polymer at various doses (0.1, 0.2, and 0.3) as well as SMT (25 mg/ml). The prepared suppositories underwent for mucoadhesive force, gelation temperature, and gelation time. When SMT and mucoadhesive polymer were added to the poloxamer mixture, the gelation temperature dropped; however, poloxamer 188 had the opposite effect. These polymers supported the prepared liquids' ability to adhere to mucous membranes and form a strong gel. The transition gelation temperature of the poloxamer solution rose as a result of the addition of poloxamer 188. The findings showed that the formula RIG5 which is composed of poloxamer 407 (19%), poloxamer 188 (5%), and xyloglucan (0.2%) had an ideal transition temperature of 36.33°C, gel strength of 44.66°C, mucoadhesive force of 6409°C, and in vitro drug release of 93.98% over an 8-hour period. In light of this, it can be said that SMT was successfully manufactured as RIG without causing any chemical reaction with its additives.

Hyaluronic acid (HA) has the capability to influence dentin niche which is important in regenerative process. The CD44 as a specific receptor of HA was found to be related to dentin mineralization process. Meanwhile, transforming growth factor β1 (TGF-β1) has a vital role in the transition from proliferation into the differentiation of human dental pulp stem cell human dental pulp stem cells (hDPSCs) to become odontoblast cells and dentin mineralization. This study aims to analyzed HA's effect on dentin mineralization through CD44 and TGF-β1 expressions. Stem cells were cultured in four different supplemented conditioned media (control, +10 μg/mL, +20 μg/mL, and + 30 μg/mL of HA). Evaluation of CD44 expression was analyzed using flow cytometry and TGF-β1 was analyzed using enzyme-linked immunosorbent assay reader. Qualitative result using Alizarin red test after 21 days was done to confirm the formation of mineralization nodules. It was shown that HA expression of CD44 and TGF-β1 on hDPSCs were higher in AH groups compared to the control group and 30 μg/mL HA induced the highest TGF-β1 expression on hDPSCs. Alizarin red test also showed the highest mineralization nodules in the same group. Therefore, from this study, we found that supplemented 30 μg/mL of HA was proved in initiating hDPSCs differentiation process and promote dentin mineralization.

Olfactory dysfunction (OD) is a common feature of COVID-19. The goal of the study was to define the modes of onset of OD in the clinical course of the disease and to follow the cases for 12-18 months in order to estimate the differences in the recovery time from OD over the course of the disease. We managed to follow a total of 325 patients (females: 198, males: 127) in the Babylon governorate in Iraq. All were COVID-19 patients who should have OD during the course of the disease. COVID-19 infection was established in all patients by swab test, i.e. polymerase chain reaction (PCR) and/or chest computed tomography findings of pneumonia compatible with COVID-19. Detailed medical records were obtained directly from the patients or their relatives. The patients were then followed up by telephone and questioned with structured questionnaires concentrating upon general clinical features and the sense of olfaction. Information about the presence of olfactory disorders, their occurrence, and development was recorded. Based on the onset of OD, the patients were categorized into three groups. Olfactory functions were assessed primarily by face-to-face interview and then (if necessary) by a telephone questionnaire assessing self-reported olfactory function and olfactory-related quality of life, which measures the subjective olfactory capability (SOC). In the first 2 weeks, 148 (45.5%) patients reported complete recovery from OD, of which 90 (73.2%) patients joined at the end of the 1^st month. OD persistence was observed in 11 (3.3%) patients toward the end of the 1^st year, in 5 (1.5%) patients at the end of the 15^th month, and only in two (0.6%) patients at the end of the 18^th month. We found no significant correlation between the type of onset of OD and the duration and persistence of OD. Most sufferers of COVID-associated OD recover their sense of smell within the 1^st month.

Quinoline and its derivatives are known to have various biological activities such as antibacterial and antioxidant. Therefore, this study aims to synthesize quinoline moiety from isatin and ethyl acetoacetate by Pfitzinger reaction under acidic conditions. The benzimidazole derivative was synthesized from quinoline and o-phenylenediamine by a solvent-less reaction, while the hydrazone derivative was formed by the reaction with hydrazine hydrate and aromatic aldehyde. In addition, 4-hydroxybenzaldehyde was used as an aromatic aldehyde. The four compounds formed were characterized by thin-layer chromatography (TLC), melting point measurement, Fourier-transform infrared, liquid chromatography-mass spectrometry, and ultraviolet-visible spectrophotometry. They were also evaluated for their antioxidant and antimicrobial activities using the 2,2-diphenyl-1-picrylhydrazyl assay and the disc diffusion method, respectively. All compounds showed weak antioxidant activity compared to ascorbic acid; the quinoline-hydrazone derivative showed the best antioxidant activity with IC₅₀ = 843.52 ppm, while the IC₅₀ value for quinoline-benzimidazole was 4784.66 ppm. All synthesized compounds have not been confirmed to be effective against Staphylococcus aureus and Escherichia coli bacteria in a concentration range of 75-1000 ppm. The bioactive compounds based on the quinoline-hydrazone and benzimidazole structures have been successfully synthesized and tested for their activity as antioxidant and antimicrobial agents.

Drug excipient compatibility studies are considered important in successful formulation of drug products. Suggested methods for this purpose are thermal techniques under isothermal or nonisothermal conditions. In this study, modafinil, a wakefulness-promoting drug, was investigated under nonisothermal conditions using differential scanning calorimetry. Four different heating rates, 5, 10, 15, and 20°C/min, were performed for modafinil pure material and its physical mixtures with magnesium stearate (MgSt) or Gelucire 48/16. Activation energy (Ea) was calculated from the straight line of plotting a function of heating rate versus temperature and found that modafinil-Gelucire physical mixture increased Ea. This indicates drug-excipient interaction, supported by evidence from Fourier transform infrared spectroscopy and nuclear magnetic resonance spectroscopy. No significant interaction was detected with MgSt.

The aim was to analyze the influence of the incorporation of 4% by mass of colloidal dispersion of titanium dioxide (TiO₂) nanoparticles on the long-term water sorption and solubility of two commercial universal bonding agents. In vitro studies. A colloidal dispersion of TiO₂ nanoparticles was formulated and blended into two commercial dental bonding agents, i.e., Ambar Universal (FGM, Brasil) and G-Premio Bond Universal (GC, America) at 4% by mass. Forty bonding agent discs were fabricated and segregated into four bonding agent groups of 10 discs each, i.e., GA: Ambar Universal (control), GB: Ambar Universal (4% TiO₂ incorporated), GC: G-Premio Bond universal (control), and GD: G-Premio Bond (4% TiO₂ incorporated). The bonding agent discs were developed by dispensing the bonding agents into a silicone cast of 5 mm diameter and 1 mm depth. After bonding agent discs were desiccated, the cured discs were weighed and kept in distilled water to be evaluated for water sorption and solubility over 1 year storage period. Statistical analysis was performed by independent variable t-test performed using the IBM SPSS software (Chicago, IL: SPSS Inc). The incorporated bonding agent groups (GA and GB) showed significantly lower (P < 0.05) water sorption and solubility following 1 year of water storage in comparison to the control bonding agents. Both GC and GD demonstrated remarkably lower water sorption and solubility than GA and GB. Incorporation of the colloidal dispersion of TiO₂ nanoparticles at 4% by mass into the universal bonding agents has significantly reduced their water sorption and solubility contrast to their control groups.