Methimazole in the Treatment of Melasma: A Clinical and Dermascopic Study

BACKGROUND: Melasma is a chronic hypermelanotic disorder that is challenging to treat; no single effective therapeutic agent for it has been discovered. Methimazole, an oral antithyroid drug, has a skin depigmenting effect when used topically. OBJECTIVE: We sought to evaluate the efficacy and safety of methimazole, applied during microneedling sessions and additional topical use in between sessions, for the treatment of melasma. METHODS: This split-face study included 30 Egyptian patients with melasma, each of whom received 12 microneedling sessions once per week for 12 weeks followed by topical methimazole on the right side of face and placebo on the left side. In between the sessions, topical methimazole 5% cream was applied twice per day on the right side and placebo on the left side. Assessments were performed using the Hemi-melasma Area and Severity Index (hemi-MASI) percentage of improvement, patient satisfaction, dermoscopy, and thyroid-stimulating hormone (TSH) serum levels. RESULTS: There were significant clinical and dermoscopic improvements; hemi-MASI scores on the methimazole-treated right sides were decreased (p<0.001). The percent of hemi-MASI score improvement was significantly associated with the malar pattern (p=0.031) and epidermal type (p=0.04) of melasma. About 70 percent of our studied patients reported being satisfied with their treatment response (7% excellent, 33% good, 30% fair). No significant local or systemic side effects were observed. Pre- and posttreatment serum TSH levels were within the normal range in all treated cases. CONCLUSIONS: Methimazole has the potential to be a safe and promising therapeutic agent for the treatment of melasma via dermapen-delivered microneedling sessions with topical use in between sessions.     

Photocatalytic activity and antibacterial properties of linen fabric using reduced graphene oxide/silver nanocomposite

Silver nanoparticles were in situ prepared on the surface of linen fabric coated by graphene oxide (GO). In the meantime, the reduction of silver nitrate on the GO-coated fabric led to the synthesis of reduced graphene oxide on the fabric. Two kinds of substrate (cotton and linen) were used. Both RGO/Ag and Ag/GO nanocomposites were added on cotton and linen fabrics through a conventional “pad–dry–cure” method. The chemistry and morphology of the coated surfaces were extensively characterized using Fourier-transformed infrared spectroscopy, energy-dispersive X-ray spectroscopy, and scanning electron microscopy. Resistivity measurements were used for assessing the conductivity. The UV protection properties and the photocatalytic activity of the coated fabrics against methylene blue dye were also investigated. The antibacterial activity was studied against Gram-positive S. aureus and B. subtilis and Gram-negative bacterial strains E. coli and P. aeruginosa by determining the zone of inhibition using the agar diffusion method. Methicillin-resistant Staphylococcus aureus (MRSA) has been responsible for many serious hospital infections worldwide. The fabrics showed superior antibacterial activity and successfully hindered the growth of pathogenic bacterial strains. This outcome suggested that both the RGO/Ag and Ag/GO nanocomposites-coated fabrics could be potentially applied in biomaterials and biomedical fields.

Silver nanoparticles were in situ prepared on the surface of linen fabric coated by graphene oxide (GO).     

Enhanced bioavailability of buspirone hydrochloride via cup and core buccal tablets: Formulation and in vitro/in vivo evaluation

This work aims to prepare sustained release buccal mucoadhesive tablets of buspirone hydrochloride (BH) to improve its systemic bioavailability. The tablets were prepared according to 5 × 3 factorial design where polymer type was set at five levels (carbopol, hydroxypropyl methylcellulose, sodium alginate, sodium carboxymethyl cellulose and guar gum), and polymer to drug ratio at three levels (1:1, 2:1 and 3:1). Mucoadhesion force, ex vivo mucoadhesion time, percent BH released after 8 h (Q8h) and time for release of 50% BH (T_50%) were chosen as dependent variables. Additional BH cup and core buccal tablets were prepared to optimize BH release profile and make it uni-directional along with the tablets mucoadhesion. Tablets were evaluated in terms of content uniformity, weight variation, thickness, diameter, hardness, friability, swelling index, surface pH, mucoadhesion strength and time and in vitro release. Cup and core formula (CA10) was able to adhere to the buccal mucosa for 8 h, showed the highest Q8h (97.91%) and exhibited a zero order drug release profile. Pharmacokinetic study of formula CA10 in human volunteers revealed a 5.6 fold increase in BH bioavailability compared to the oral commercial Buspar^® tablets. Conducting level A in vitro/in vivo correlation showed good correlation (r² = 0.9805) between fractions dissolved in vitro and fractions absorbed in vivo.     

Nanobiotic formulations as promising advances for combating MRSA resistance: susceptibilities and post-antibiotic effects of clindamycin,doxycycline, and linezolid

Antimicrobial activity and post-antibiotic effects (PAEs) are both important parameters in determination of the dosage regimen of antimicrobial agents. In the present study, antimicrobial activity and PAEs of clindamycin, doxycycline, linezolid, and their nanobiotic formulations were evaluated against two methicillin resistant Staphylococcus aureus clinical isolates (MRSA) encoded (MRSA-S1 and MRSA-S2). Nanobiotic formulations increased the susceptibility of MRSA isolates by 4–64 folds as compared to their conventional ones. The PAE values were determined after exposure of MRSA isolates for 1 h to 10× the MICs of the tested antibiotics. The duration of PAEs were recorded after bacterial growth in Mueller Hinton broth (MHB) free from antibiotic has been restored. The PAE values for MRSA-S1 were 2.5 h for the conventional antibiotics. However, the PAEs for nanobiotics were 4 h for both clindamycin and linezolid, while 3 h for doxycycline. For MRSA-S2, linezolid and linezolid nanobiotics PAEs were 3 h. PAEs of clindamycin and clindamycin nanobiotics were 3.75 h and 4 h, respectively. Doxycycline and doxycycline nanobiotics revealed the same PAEs patterns of 3.5 h. The findings of the current study may positively influence the pharmacodynamics of the antibiotics and consequently the dosage regimen of nanobiotics as well as on their clinical outcome.

Novel nanobiotic formulations of clindamycin, doxycycline, and linezolid were evaluated for the post-antibiotic effects against biofilm forming methicillin resistant Staphylococcus aureus (MRSA).     

Characteristics of Conventional and Microwave Sintered Iron Ore Preform

In this study, compacted hematite (Fe₂O₃) preforms were made and sintered at various temperatures, such as 1250 °C and 1300 °C, using both conventional and microwave sintering methods. The density, porosity, microhardness, cold crushing strength, microphotographs, and X-ray diffraction (XRD) analysis of the sintered preforms were used to evaluate the performance of the two sintering methods. It was found that microwave sintered preforms possessed lesser porosity and higher density than conventionally sintered preforms owing to uniform heating of the powdered ore in microwave sintering method. Furthermore, it was also observed that microwave sintered preforms exhibited relatively higher cold crushing strength and hardness than conventionally sintered preforms. Thus, the overall results revealed that microwave sintering yielded better properties considered in the present study.     

Interactions of Magnolia and Ziziphus extracts with selected central nervous system receptors

Ethnopharmacological relevance

Magnolia officinalis Rehder and Wilson [Magnoliaceae] bark and Ziziphus spinosa (Buhge) Hu ex. Chen. [Fam. Rhamnaceae] seed have a history of use in traditional Asian medicine for mild anxiety, nervousness and sleep-related problems.

Aim of the study

To identify pharmacological targets, extracts of Magnolia officinalis (ME), Ziziphus spinosa (ZE), and a proprietary fixed combination (MZE) were tested for affinity with central nervous system receptors associated with relaxation and sleep.

Methods

In vitro radioligand binding and cellular functional assays were conducted on: adenosine A₁, dopamine (transporter, D₁, D_2S, D₃, D_4.4 and D₅), serotonin (transporter, 5-HT_1A, 5-HT_1B, 5-HT_4e, 5-HT₆ and 5-HT₇) and the GABA benzodiazepine receptor.

Results

Interactions were demonstrated with the adenosine A₁ receptor, dopamine transporter and dopamine D₅ receptor (antagonist activity), serotonin receptors (5-HT_1B and 5-HT₆ antagonist activity) and the GABA benzodiazepine receptor at a concentration of 100 μg/ml or lower. ME had an affinity with adenosine A₁ (K_i of 9.2 ± 1.1 μg/ml) and potentiated the GABA activated chloride current at the benzodiazepine subunits of the GABA receptor (maximum effect at 50 μg/ml). ME had a modest antagonist action with 5-HT₆ and ZE with the 5-HT_1B receptor.

Conclusion

The interactions in the receptor binding models are consistent with the traditional anxiolytic and sleep-inducing activities of Magnolia officinalis bark and Ziziphus spinosa seed.     

Evaluating the long-term impact of faculty development programs on MCQ item analysis

Abstract

Purpose: Evaluating the long-term impact of faculty development programs (FDPs) can help monitor the effectiveness of the program and identify areas for development. This study examined long-term differences in confidence, knowledge, behaviors, and policies of faculty members who attended FDPs on multiple choice question (MCQ) item analysis and faculty members who did not attend the FDPs.

Methods: A cross-sectional study design was used, by administering a 24-item survey to a representative sample (simple random selection) of 61 faculty members at King Abdulaziz University Faculty of Medicine.

Results: Among respondents, 34% did not attend FDPs; 53% attended 1–3 FDPs; and 13% attended more than 3 FDPs on MCQ item analysis. Results showed that faculty knowledge on elements of MCQ item analysis was significantly greater (p?=?.01) for members who attended the FDPs. Faculty who attended FDPs on MCQ item analysis were twice more likely to conduct item analysis in general (p?=?.020) and four times more likely to conduct item analysis for more than 70% of module examinations (p?=?.005).

Conclusion: FDPs focused on MCQ item analysis can yield systematic changes on faculty confidence, knowledge, and behaviors. Moreover, FDPs also need support from the department and need sustained strategic support to ensure continued effectiveness.     

4-Hydroxycoumarin in heterocyclic synthesis. Part III. Synthesis of some new pyrano[2,3-d]pyrimidine, 2-substitute

The synthesis of new [1]benzopyrano[3',4':5,6]pyrano[2,3-d]pyrimidines and related heterocycles has been reported. The key intermediate 2-amino-3-cyano-4-methyl-4H,5H-pyrano[3,2-c][1]benzopyran-5-one (3) was obtained in one pot synthesis from the reaction of 4-hydroxycoumarin and acetaldehyde-malononitrile (2). The antimicrobial screening was performed for some of the synthesized compounds.     

Vildagliptin Recruits Regulatory T Cells in Patients Undergoing Primary Percutaneous Coronary Intervention

Regulatory T cells (Treg) has been documented to be protective against myocardial ischemia–reperfusion injury (MIRI). The administration of drugs which recruit Treg cells may participate in the cardioprotection of MIRI. The purpose of the present study was to investigate whether the add-on vildagliptin (vild) to standard treatment of MIRI prior to reperfusion could increase Treg recruitment, anti-inflammatory, and antioxidant effects of the standard treatment or not. Sixty diabetic patients with ST-segment elevation myocardial infarction were randomly divided into two equal groups: control group was given the standard medical treatment and vild group was given the standard medical treatment plus vild. There were no statistical differences between the mean of percentage of changes in nitric oxide, ischemia modified albumin, highly sensitive C reactive protein, and interferon-gamma levels in the studied groups. While, the percentages of changes of myeloperoxidase level, CD4+CD25+ Treg cells count, and transforming growth factor-beta1 level were significantly higher in vild group compared with control group. We concluded that addition of vild to standard medical treatment of MIRI could increase its effectiveness through recruitment of CD4+CD25+ Treg cells.