Journal of Advanced Pharmaceutical Technology & Research最新文献

Rhizophora stylosa Griff. roots contain bioactive metabolites and therapeutic potential. This study measured the antioxidants, toxicity and cytotoxicity from its dichloromethane extract and four derived fractions (RSD 1-4). The extracts showed strong antioxidant activity (IC₅₀ = 7.50 ppm) and toxicity (LC₅₀ = 31.92 ppm). Evaluation of each fraction showed that RSD 2 had the highest activity for antioxidant bioactivity with IC₅₀ of 45.40 ppm and toxicity with LC₅₀ value of 332.48 ppm. Cytotoxicity against MCF-7 cells showed that RSD 3 had the stronger effect, followed by RSD 2 with IC₅₀ values of 225.50 ppm and 155.90 ppm, respectively. Statistical analysis confirmed that differences in antioxidant and toxicity activities among extract and fractions were significant (P < 0.05), whereas cytotoxic activity differences were not statistically significant. Gas chromatography-mass spectrometry analysis of RSD 2 identified stigmasta-3,5-diene, α-amyrin, and lupeol as major components and potentially responsible for the bioactivities. In summary, dichloromethane root extract of R. stylosa Griff. may serve as phytomedicines for breast cancer.

[This corrects the article on p. 80 in vol. 16, PMID: 40510893.].

The study examined the mortality outcomes of extended-spectrum β-lactamase (ESBL)-producing bacteria in Enterobacteriaceae, specifically Klebsiella pneumoniae and Escherichia coli, and reviewed evidence on carbapenem-sparing regimens to avoid carbapenem use in treating ESBL infections, focusing on patients with bacteremia. This study analyzed 30-day all-cause mortality outcomes in adult patients over 18 years treated with carbapenem compared to other antibiotics for bloodstream infections caused by ESBL using Scopus, PubMed, and Sage Journal databases from 2015 to 2024, using pooled risk ratios and 95% confidence intervals for all outcomes. Eight studies found no significant differences between groups receiving carbapenems and other antibiotics. However, carbapenems were found to have a higher 30-day all-cause mortality rate than comparative antibiotics for ESBL in bacteremia. Two studies reported lower 30-day all-cause mortality rates when using carbapenems. There was no significant correlation between antibiotic use and ESBL-related mortality in bacteremia patients. Most carbapenem therapy users had a higher mortality rate than those using other antibiotics; however, the difference was not statistically significant.

Deep eutectic solvents (DESs) in pharmaceutical investigations are still largely unknown in terms of safety, environmental acceptability, and practical use. The investigation focus is primarily of attempts to improve solubility is examined using the co-crystallization approach, which follows similar principles to the production of eutectic mixtures. We will look into the eutectic mixture interaction between selected coformers (nicotinamide [NA], isonicotinamide, and citric acid as acceptors of hydrogen bond and atorvastatin calcium trihydrate [ATCH] as donors of hydrogen bond in the DES system, assisted by propylene glycol [PG]). The study found that the optimum interaction in the DES system for ATCH is using NA in PG as a carrier, with evaluation by polarization microscopy, Fourier transform infrared spectroscopy (FT-IR), and differential scanning calorimetry (DSC), verifying that the drug and the DES components have formed H-bonds. H-bond interactions had been recognized through FT-IR and DSC, revealing that the DESs with NA coformer can increase ATCH solubility, as shown in the phase diagram. The increase in solubility was fairly considerable, allowing ATCH to dissolve at high concentrations in DESs, with a solubility of 0.158 ± 0.098 mg/mL compared to 0.000597 ± 0.003 mg/mL in water. Thus, it is obtainable to conclude that among the selected coformers, the DES system with the potential for improving the solubility of ATCH is DESs with NA coformer assisted by PG.

Diabetic wounds are chronic complications in patients with diabetes mellitus characterized by an elongated proliferation period, leading to a longer wound closure time. The lack of topical remedies for diabetic wounds necessitates the development of formulations that effectively facilitate closure. Kratom (Mitragyna speciosa) leaves, containing polyphenolic compounds, have the potential to be developed into a film spray suitable for diabetic wound closure. This study aims to develop a film-spray formula of kratom leaves extracted using natural deep eutectic solvent (NADES) and to investigate its wound healing activity on type I diabetic rats. Polyphenol-rich NADES extracts were formulated with a film-forming base in concentrations of 2%, 3%, and 4% v/v. The sprays were assessed for pH, viscosity, drying time, and organoleptic properties and evaluated for their effectiveness in reducing wound diameter on streptozotocin-induced diabetic rats. All formulated sprays exhibited watery form, dark orange, and odor characteristics of kratom extract, and the stability test showed that no separation was observed. The wound healing activity evaluation revealed that the film spray containing 4% of kratom NADES extract on day 21 demonstrated significant healing effects on type I diabetic rats, including a reduction in wound diameter (83.99 ± 12.02%), a decrease in neutrophil cell count, and an increase in epithelial tissue thickness. Kratom NADES extract film-forming spray (4%) has the potential to shorten the closure time of diabetic wounds.

Gelatin, commonly used for capsule shells, is mostly imported from Europe and America to Indonesia. However, Indonesia's rich biodiversity offers abundant natural alternatives like arrowroot and alginate. The need for local raw material independence in pharmaceuticals drives this research. This study aims to determine whether arrowroot starch and sodium alginate with calcium chloride as a crosslinker can replace gelatin capsule shells. This study involved five capsule shell formulas (F1-F5), with evaluations on characteristics, swelling %, disintegration time, dispersive X-ray, Fourier-transform infrared (FTIR) analysis, and simplex lattice design (SLD) method optimization, using commercial capsules (CCs) as a control. We used the one-sample t-test. F3 showed the best results in weight uniformity (0.22 ± 0.01 g), %swelling (45.84 ± 0.08%), and disintegration time (8.22 ± 0.85 min), compared to the CC, i.e., weight uniformity (0.12 ± 0.003 g), %swelling (43.26 ± 0.03%), and disintegration time (6.19 ± 1.38 min). Morphologically, F3 was the most homogeneous, resembling CC. FTIR analysis showed hydroxyl band from carboxylic group shifts indicating crosslinking, with notable changes from 1416.6 to 1386.9/cm in F3 and 1417.7-1394.0/cm in F5 after CaCl₂ addition. SLD validation was performed on three model-generated equations using experimental data. The differences between predicted and experimental results were 34.54% (weight uniformity), 3.12% (swelling), and 5.35% (disintegration time). A one-sample t-test showed no significant differences (α > 0.05). Arrowroot starch and sodium alginate with calcium chloride crosslinker can be used as an alternative to capsule shells.

Sepsis, a life-threatening systemic inflammatory condition, is a leading cause of mortality worldwide. Its pathophysiology involves the activation of nuclear factor kappa beta (NF-κB), which promotes the release of proinflammatory cytokines. Acetylsalicylic acid (ASA), a widely used nonsteroidal anti-inflammatory drug, inhibits NF-κB but poses risks of peptic ulcer disease and nephrotoxicity. This study evaluates the efficacy of 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid (3-CH₂Cl), a novel salicylate derivative, in reducing NF-κB expression in the kidneys and lungs of lipopolysaccharide (LPS)-induced septic BALB/C mice. Mice were divided into four groups: untreated, LPS only, LPS + ASA (60 mg/kg BW), and LPS + 3-CH₂Cl (60 mg/kg BW). NF-κB expression was assessed via immunohistochemistry. LPS significantly increased NF-κB expression in both renal and pulmonary tissues compared to controls (P < 0.0001). While ASA treatment reduced NF-κB levels (P < 0.0001), 3-CH₂Cl demonstrated superior suppression in the renal cortex, renal medulla, and alveolar regions (P < 0.05). In addition, 3-CH₂Cl alleviated hypothermia in septic mice, comparable to ASA. Given its enhanced anti-inflammatory efficacy and reduced gastrointestinal risk, 3-CH₂Cl presents a promising alternative to ASA for sepsis-related inflammation management. Further studies are warranted to explore its clinical applications.

Blue light exposure can damage the retina, resulting in retinal atrophy and significant vision loss. Currently, no efficient animal models can observe retinal damage caused by blue light within a defined timeframe. Creating a BALB/c mouse model for blue light-induced retinal damage is expected to enhance research focused on the prevention and treatment of age-related macular degeneration. This study explores the potential effect of blue light exposure on the BALB/c mice model by analysing apoptosis and retinal degeneration. Anatomical Pathology Laboratory of Diponegoro University and The Integrated Research and Testing Laboratory of Gadjah Mada University. This study design was a posttest-only control group design. Ten five-week-old BALB/c mice were divided into two groups. The exposure group received 10,000 lux of blue light in the special cage for 2 weeks, 3 h daily. Caspase-3 expression was assessed through polymerase chain reaction testing, and retinal thickness was analyzed using hematoxylin and eosin staining. We used the Shapiro-Wilk test to evaluate data normality. Parametric t-tests and nonparametric Mann-Whitney tests were applied to compare groups, with P < 0.05 considered significant. The average whole retinal thickness of the exposed group was 152.812 ± 20.919 µm, while the control group was 214.948 ± 53.284 µm (P = 0.04). The average caspase-3 expression in the exposed group was 19.03 ± 8.57 µm, while the control group was 5.78 ± 2.63 µm (P = 0.011). This approach, utilizing animal models for blue light exposure, can be employed to learn about retinal damage caused by blue light.

Stainless steel temporary anchorage device (SS TAD) has toxic risk due to the content that may be released when exposed to the oral environment, and the mouthwash being used. This research aims to analyze the cytotoxicity of SS TAD and measure the inflammation level in cells after exposure to three types of mouthwash. SS TADs (n = 28) were divided into four groups (n = 7 per group) and immersed in the following mouthwash solutions for 90 days. The resulting eluates were then applied to BHK-21 fibroblast cell cultures and incubated for 24 h. Matrix metalloproteinase-8 (MMP-8) levels in the supernatants on days 1 and 7 were measured using enzyme-linked immunosorbent assay MMP-8 kit. BHK-21 fibroblast cells showed significant differences in reactivity (P < 0.05) after exposure to SS TAD eluate in povidone-iodine (PVP-I) and chitosan mouthwash, compared to control groups without SS TAD. Viability test revealed significant differences (P < 0.05) after exposure to SS TAD eluate in PVP-I mouthwash compared to PVP-I alone. The reactivity of BHK-21 fibroblast cells exposed to fluoride and distilled water was not significantly different (P > 0.05) from control groups without SS TAD. The viability of BHK-21 fibroblast cells exposed to fluoride and distilled water did not differ significantly from control groups without SS TAD. MMP-8 levels differed significantly between SS TAD eluate groups (P < 0.05) on day 1 and day 7, with day 7 levels significantly higher than day 1. The most recommended mouthwash is chitosan for TAD SS users rather than fluoride and PVP-I.

Some antituberculosis drugs were reported to have adverse effects. The study investigates the use of quercetin pulmospheres as an alternative to traditional antituberculosis drugs. Formulated with alginate and kappa carrageenan as F1, F2, and F3 (1:1, 1:2, and 1:3), the pulmospheres were observed for the release and deposition in rat lungs. Results show a sustained release of 50.47% ±0.43%-58.37% ±0.57% in 10 h above minimum inhibitory concentration (MIC) against Mycobacterium tuberculosis and provided Higuchi kinetics model. Pulmospheres delivered quercetin to the lungs and showed a deposition with high concentrations. The slowest rate was occurred in pulmospheres with polymer ratio of 1:2. Formula F2 showed the most optimal results with the lowest rhodamine B concentration of 11.934 ± 2.751-12.364 ± 0.070 µg/g and 6.987 ± 1.931-8.685 ± 2.672 µg/g for left and right lung, respectively, which produced same MIC compare to F1 and F3. The study suggests further evaluation of effective doses for antituberculosis.