Current Drug Therapy - Online First

Dragon fruit is a tropical fruit from the cactus family, known for its high nutrient and fiber content. This study investigates the antioxidant potential of red pitaya (Hylocereus polyrhizus), comparing its ethanolic extract with its microencapsulated form using a gelatin-pectin matrix. Red pitaya is rich in betalains, which contribute to its strong antioxidant, anticancer, and antimicrobial properties. However, betalains are unstable and susceptible to degradation under various conditions.

The ethanolic extract of red pitaya was encapsulated through freeze-drying. The resulting nanocapsules were characterized using SEM and FTIR analyses. We also compared the stability of the extract and nanocapsules, total phenol content, and antioxidant activity.

The encapsulation efficiency was approximately 48%. The antioxidant activity of the nanocapsules, with a mean diameter of 0.41 nm, was evaluated using the DPPH assay, which revealed that the nanocapsules exhibited superior antioxidant capacity compared to the ethanolic extract. Although the total phenolic content of nanocapsules was lower than that of the extract, the nanocapsules effectively released phenolic compounds and demonstrated greater stability at high temperatures than the extract.

Encapsulation significantly improved the thermal stability and antioxidant performance of red pitaya extract, demonstrating its effectiveness in preserving sensitive bioactive compounds.

These findings suggest that encapsulation enhances the stability and efficacy of betalains, positioning the nanocapsules as a potential natural additive for functional foods and nutraceuticals.

Acne vulgaris is a dermatological condition that significantly affects the physical appearance and quality of life of patients. The emergence of antibiotic resistance has compromised the therapeutic efficacy of antibiotics in acne management. Burdock is a water-soluble bioactive agent that exhibits antimicrobial, anti-inflammatory, and antioxidant properties.

Burdock was loaded into w/o/w nano-emulsion using the reverse titration method. The globule size, zeta potential, entrapment efficiency, and percentage cumulative drug release of the nano-emulsion were evaluated. The nano-emulsion was incorporated into a Carbopol 940 (0.5%, 1%, and 1.5% w/w) gel, and the drug permeability of the nano-emulsion gel was evaluated. The formulations of the nano-emulsion were optimized using the Box-Behnken design.

The Burdock was loaded into w/o/w nano-emulsion by applying the Quality by Design (QbD) approach considering the effect of the factors (phase volume ratio: PVR, time of primary emulsification: TPE, and concentration of Transcutol P: TLP) on globule size (GS) and % entrapment efficiency (%EE) of the drug.

The optimized nano-emulsion was prepared using Burdock and showed a GS of 176.2 nm and an EE of 99.24% with a PVR of 4.60, a TPE of 3.1 minutes, and a TLP concentration of 8.92%.

The optimized nano-emulsion was transformed into a gel and characterized for morphology, viscosity, pH, drug content, in-vitro release, and ex vivo drug permeation. Finally, skin irritation study and histopathological evaluation suggested that the obtained nano-emulsion gel was effective in the treatment of Acne vulgaris.

Malaria, a life-threatening disease caused by Plasmodium parasites, still poses a severe threat to public health safety in Africa, South America, and Asia. It is transmitted via Anopheles mosquito bites and has been reported to be a major cause of toddler mortalities in these regions. Due to its mutation-mediated drug resistance and continued spread of the disease, there still exists a need to investigate and discover more effective antimalarial drugs. Hydromorphone is a semi-synthetic opioid agonist and a hydrogenated ketone of morphine with pain-relieving qualities and serves as a second-line drug to morphine in the treatment of both chronic and acute pain.

High-throughput virtual screen of hydromorphone analogues was done using Autodock Vina. The results of protein-ligand complexes were visualised using Discovery Studio Visualizer, and ligands with the best binding scores were used to perform MD simulations using GROMACS software.

The promising candidate derivatives included analogues of both hydromorphone and morphine with hydroxy and ether constituents in the benzene ring. The best performing docking scores were carried forward to molecular dynamics using the GROMACS software. The ligands showed stability during these simulations and thus serve as promising inhibitors of DXR.

During molecular docking, all ligands docked in chain A did not bind in the active site. This may be due to the small binding pocket in chain A. For chain B, eight ligands (four with NADPH and without NADPH) with the best docking score were further taken for molecular dynamics simulations, and their RMSDs were calculated after molecular dynamics, which all showed stability in the binding pocket.

The Hydromorphone derivatives explored in this study showed promising results when interacting with chain B of PfDXR (4gae) protein.

Diabetes management is critical for patient health, yet many individuals lack essential knowledge about their condition.

This study aimed to develop and validate a patient information leaflet (PIL) focused on diabetes, assessing its effectiveness in enhancing patient knowledge among individuals with diabetes.

The primary objective was to prepare and validate a patient information leaflet (PIL) on diabetes and evaluate its impact on patient knowledge among diabetic individuals. The secondary objective was to analyze demographic factors, education, family history, and comorbidities influencing baseline knowledge and post-intervention knowledge improvement.

Quasi-experimental pre and post-test design was carried out enrolling 78 inpatients and outpatients diagnosed with T1DM or T2DM. The PIL was developed using evidence-based resources and validated through expert panel reviews. Its readability was evaluated using Flesch Reading Ease (FRE) and Flesch-Kincaid Grade Level (FK-GL) scales, with additional validation through user testing. The leaflet’s design adhered to Baker-Able Leaflet Design (BALD) principles. Pre- and post-intervention knowledge was measured through a structured questionnaire, and participant feedback on the leaflet's content and layout was collected.

The FRE and FK-GL scores for the PIL were 60.3 and 8, respectively. The BALD scores for the English and Kannada versions were 25 and 24, respectively. User testing revealed significant improvements in knowledge, with mean scores increasing from 33.85 ± 23.43 to 93.23 ± 8.58 for the Kannada PIL and from 59.23 ± 24.31 to 93.08 ± 9.47 for the English PIL. A total of 85.9% of participants rated the leaflet as effective in improving their understanding of diabetes management.

The validated PIL significantly enhanced patient knowledge of diabetes. These findings suggest that such educational tools can effectively support patient education in both T1DM and T2DM populations.

Type 2 diabetes mellitus (T2DM) is the leading cause of chronic kidney disease (CKD). Thiamine has shown efficacy in microalbuminuria reduction, but its effect on estimated glomerular filtration rate (eGFR) is still uncertain.

To determine the effect of thiamine on increasing eGFR in patients with T2DM with CKD stage 3.

This RCT was conducted in 35 T2DM with CKD stage 3 patients. 18 received 300 mg thiamine once daily (150 mg/capsule) and 17 received a placebo for 24 weeks. The primary outcome was the difference in the median change in the eGFR with thiamine at 24 weeks. Secondary outcomes included median changes within and between groups in the serum creatinine level, HbA1C level, urinary albumin level, total cholesterol level, LDL level, HDL level, triglyceride level, and adverse events.

The baseline characteristics of the two groups were similar except for body mass index (BMI). After 24 weeks, the median change in eGFR was 1.59 ml/min/1.73 m2 of body-surface area (BSA) in thiamine group as compared to 1.78 ml/min/1.73 m2 of BSA in placebo group, leading to treatment difference of -0.19 ml/min/1.73 m2 of BSA (p = 0.61). The patients who received thiamine had a significant decrease in median HbA1c compared to the placebo (median change difference of -1.35, p < 0.01). The urinary albumin level and all lipid profiles were not significantly different between the two groups. No serious adverse events were reported.

The effects of the two agents on eGFR were not significantly different, but patients who received thiamine had a significant decrease in median HbA1C.

Deprescribing is a physician-led approach to mitigating polypharmacy, particularly among the elderly, to lower adverse events and medication errors. This study explores physicians' attitudes, practices, and barriers to deprescribing.

A cross-sectional survey, framed by existing literature and expert insights, was conducted among 150 physicians to gather data on their experiences with deprescribing, along with associated motivators and barriers. Descriptive statistics and chi-square analyses were utilized to identify factors influencing deprescribing practices.

Weekly deprescribing was practiced by 44% of participants and was associated with the average number of patients seen (p=0.048) and patient age group (p=0.019). Key motivators included cost reduction (70%) and decreased pill burden (66%), while barriers included time constraints (52%) and adherence to prescribing guidelines (50%). Prescribing guidelines (68%) and multidisciplinary approaches (40%) were proposed as suggestions by physicians.

Addressing barriers through structured guidelines, adequate time allocation, and multidisciplinary collaboration could enhance deprescribing practices.

Hypothyroidism causes various disorders in the reproductive system. The use of honey and black seed in traditional medicine is well-established.

possible effects of hydroalcoholic extract of black seed and honey (Dosin) on pituitary-gonadal hormones, spermatogenesis, as well as the level of lipid peroxidation and the expression level of inflammatory and apoptosis genes was determined.

Hypothyroidism was induced with methimazole, and the animals were then divided into four groups: control, hypothyroid, hypothyroid + Dosin 100, and hypothyroid + Dosin 200. Dosin was administered orally for 45 days and serum concentrations of LH, FSH, testosterone and malondialdehyde were measured by ELISA. Sperm analysis was also performed. Histopathological examination was conducted and the expression levels of genes related to apoptosis (Bax, Bad and Bcl-2) and inflammation (IL6, TNFα and IL10) were investigated.

Sperm analysis showed that motility, morphology, and count indices decreased in the hypothyroidism group and significantly improved in the treatment groups (P<0.05). Histological studies showed that the length, diameter and volume of seminiferous tubules, basement membrane thickness, number of Leydig and Sertoli cells and testosterone levels increased in treatment groups (P<0.05). The mean serum levels of LH, FSH and malondialdehyde decreased in treatment groups significantly (P<0.05). Also, the expression of inflammatory genes and Bax and Bad genes decreased in treatment groups while Bcl2 increased (P<0.05). The expression of IL6 and TNFα genes decreased in the treatment groups and IL10 increased significantly (P<0.05).

Dosin probably improves testicular spermatogenesis and strengthens the antioxidant, anti-inflammatory, and anti-apoptotic thyroid systems by regulating pituitary-gonadal hormones.