Psoriasis is a prototypic example of an immune-mediated skin disorder, characterized by abnormal keratinocyte differentiation, barrier dysfunction, and excessive production of pro-inflammatory cytokines. Here, a psoriasis-like human reconstructed epidermis (RHE-Pso) model was established by cytokine treatment of HaCaT keratinocytes with a cytokine mixture (IL-1α, TNFα, IFN-γ). This model manifested a psoriasis-like phenotype, characterized by reduced TER values, altered epidermal histomorphology, as well as a reduction in Filaggrin (FLG) expression at the protein as well as mRNA levels, accompanied by a marked enhancement in the release of cytokines like IL-1α, IL-8, TNFα, and IFN-γ. Later, this RHE-Pso model has been employed to assess various pharmacologic as well as natural agents. Clobetasol propionate emerged as one of the most effective agents in reclaiming TER values, increasing FLG mRNA expression (3.40 ± 0.37-fold of control), as well as curtailing the release of cytokines. Retinoic acid increased FLG mRNA (2.85 ± 0.35-fold of control) as well as moderately inhibited cytokine secretion, whereas calcipotriol partially relieved barrier restoration. A comparative analysis of natural agents revealed that quercetin increased FLG mRNA as well as inhibited TNFα & IFN-γ levels, whereas resveratrol relieved TER values as well as specifically inhibited cytokine release. Conversely, curcumin exhibited minimal activity. Taken together, this data propose that the HaCaT-derived RHE-Pso model can act as a promsing pre-clinical in vitro model in defining anti-psoriasis drug leads as well as natural bioactive agents.
The Malvaceae (formerly Tiliaceae) family's Grewia serrulata DC has remarkable medicinal characteristics and its many parts are utilized in traditional medicine. However, scientific evidence supporting its pharmacological activities remains limited, particularly regarding the bioactivity of its leave extracts and solvent fractions. Therefore, the present study aimed to evaluate the phytochemical profile and antioxidant, anti-inflammatory, and antidiarrheal activities of the methanol extract of G. serrulata leaves and solvent fractions. To investigate the antioxidant effect, a 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging assay was conducted in vitro, while in vivo anti-inflammatory and antidiarrheal activities were evaluated using the carrageenan-induced paw edema model and the castor oil-induced diarrhea model in mice, respectively. G. serrulata methanol extract (GSME) and its n-Hexane fraction (GSNH) showed significant potential in DPPH scavenging at higher doses with showing IC50 values of 11.7886μg/mL and 89.86μg/mL, respectively. Also, GSME, GSNH & Dichloromethane fractions (GSDM) displayed significant (p <0.001) anti-inflammatory and antidiarrheal effects compared to control. GSME, GSNH & GSDM reduced inflammation at a rate of 88.48%, 66.03% & 58.46% during 4th hour of post-injection. GSME & GSNH demonstrated a highly significant (p <0.001) reduction (71.21% & 62.12% inhibition, respectively) in diarrhea, while Loperamide showed an inhibition of 72.73%. The findings indicate that G. serrulata leaves exhibit promising antioxidant, anti-inflammatory and antidiarrheal activities. The results provide preliminary pharmacological support for the traditional use of this plant and highlight its potential as a source of bioactive compounds for future drug discovery, though further investigations including bioassay-guided isolation, mechanistic investigations, and safety evaluations are required.
Type 2 diabetes mellitus (T2DM) is a chronic metabolic disorder that is increasing in prevalence and is a leading cause of death due to cardiovascular, renal, and neurological complications. Dipeptidyl peptidase-4 inhibitors (DPP-4i) have been increasingly used due to their ability to provide stable glycemic control and their suitability for elderly patients. The aim of this study was to investigate the effectiveness of treatment regimens containing DPP-4 inhibitor in outpatients with T2DM. A retrospective descriptive study conducted over 6 months, compared pre- and post-treatment outcomes on 308 T2DM outpatients who were prescribed DPP-4 inhibitors at Dong Nai General Hospital from January 2024 to May 2025. Results showed that the median age of patients was 67 years, with a higher proportion of females than males (60.4%). Most patients had comorbidities such as lipid disorder (93.2%) and hypertension (73.4%). The DPP-4 inhibitors prescribed were primarily sitagliptin and vildagliptin, administered at doses appropriate to renal function. Metformin, insulin, and sulfonylureas were the most commonly co-administered drugs with DPP-4 inhibitors. Following the DPP-4 inhibitor–based regimen, mean HbA1c decreased by 0.7%, FBG decreased by 0.94 mmol/L, and the proportion of patients achieving HbA1c < 7% increased to 28.2%, which was statistically significant (p < 0.05). In conclusion, DPP-4 inhibitors demonstrated a moderate glucose-lowering effect, making them suitable for elderly T2DM patients with comorbidities or a high risk of hypoglycemia. Drug use adhered to clinical guidelines and was appropriate in most cases.
The rising use of cannabis and its constituents for therapeutic and recreational purposes has intensified interest in understanding its neurobehavioral effects. Zebrafish (Danio rerio) have emerged as a robust model for behavioral neuroscience due to their genetic similarity to humans and conserved endocannabinoid system. This narrative review explores the behavioral effects of major cannabinoids including Δ9-tetrahydrocannabinol (THC) and cannabidiol (CBD) on anxiety, learning and memory, and social interaction in zebrafish. Findings indicate that THC induces dose-dependent anxiogenic effects, particularly at higher concentrations, characterized by hypolocomotion and increased bottom-dwelling. Conversely, CBD shows anxiolytic potential at moderate doses but may produce biphasic effects depending on dose and exposure timing. In cognitive assays, THC impairs learning and memory performance in spatial and associative tasks, while CBD’s effects vary based on administration phase. Limited studies on social behavior suggest cannabinoids may modulate sociability, although outcomes remain inconsistent. This review highlights methodological gaps, such as the underrepresentation of chronic exposure studies, sex-based analyses, and minor cannabinoids like CBC, CBG, and CBN. Furthermore, few studies integrate behavioral outcomes with molecular or neurophysiological endpoints. By consolidating current findings, this review underscores the potential of zebrafish as a translational model in cannabinoid research and advocates for more standardized, mechanistically informed investigations to clarify the behavioral impact of cannabis constituents.
Potentially inappropriate medications (PIMs) are associated with adverse outcomes in older adults. The Asian explicit criteria, compiled from 15 quality-assessed country-specific guidelines, provide a regionally relevant and comprehensive framework for evaluating PIM use. This study investigates the prevalence, predictors, and hospitalisation outcomes of PIM use, as defined by the Asian criteria, among older outpatients in Thailand. A retrospective cohort study was conducted using data on patients aged ≥60 years who received outpatient care, obtained from the electronic medical records of three public hospitals in Thailand. Outpatient prescriptions from 2023 were analysed to identify PIM use, categorised into disease-independent, disease-specific, and drug–drug interaction (DDI)-based groups. Predictors were examined using multivariable logistic regression, while associations with hospitalisation outcomes in 2024 were assessed using generalised linear models. Among 76,361 older outpatients (mean age: 69.59 ± 7.63 years; 55.66% female), 82.99% received at least one PIM. The prevalence of disease-independent, disease-specific, and DDI-based PIMs was 82.71%, 31.09%, and 10.24%, respectively. Predictors of PIM use included care at lower-level hospitals, female sex, multimorbidity, and polypharmacy, including hyperpolypharmacy. In adjusted analyses, overall PIM use was significantly associated with a 1.17-fold increased risk of all-cause hospitalisation, 1.86-fold for adverse drug event-related hospitalisation, 1.46-fold for in-hospital mortality, and a higher number of admissions. PIM use was widespread among older outpatients and associated with adverse hospitalisation outcomes. The Asian criteria facilitated a comprehensive and context-specific evaluation of PIMs in Asian settings. Integrating these criteria into clinical practice may enhance prescribing safety and help reduce PIM-related risks.
Pain, inflammation, and fever share overlapping mediator networks, supporting dose-sparing, multi-target combinations. We evaluated a standardized Melastoma malabathricum leaf extract (ME) combined with nanocurcumin (NC) using Chou-Talalay quantitative synergy analysis and multi-model in vivo validation. ME and NC were quality-controlled by chromatographic fingerprinting and physicochemical characterization. In LPS-stimulated RAW 264.7 macrophages, single-agent and fixed-ratio combination dose-response relationships were modeled by median-effect analysis to compute combination index (CI) and dose-reduction index (DRI). For in vivo validation, Swiss albino mice were randomized into five groups per model: (i) vehicle control, (ii) model-matched positive control (tramadol, meloxicam, or paracetamol), (iii) ME alone (200 mg/kg), (iv) NC alone (50 mg/kg), and (v) ME+NC combination. Efficacy was assessed using hot-plate and formalin nociception, carrageenan-induced paw edema, and Brewer’s yeast-induced pyrexia, with reference drugs to confirm assay sensitivity. ME+NC showed consistent synergism across effect levels (Fa 0.50-0.90), with CI 0.62-0.79 at Fa 0.50-0.75 and 0.58 at Fa 0.90, corresponding to practical dose-sparing (DRI ≈ 2.2-2.6 for ME and 2.7-3.1 for NC). In vivo, the combination produced the greatest improvements across pain, inflammation, and fever models versus either monotherapy, alongside larger reductions in pro-inflammatory cytokines and COX-2/iNOS and favorable shifts in oxidative stress markers, and was well tolerated under the study conditions, without evidence of overt short-term toxicity. Overall, ME+NC is a quality-controlled, CI/DRI-defined synergistic combination with coherent multi-symptom efficacy, warranting pharmacokinetic–pharmacodynamic optimization and evaluation in longer-term disease settings.
The rapid emergence of antibiotic-resistant Staphylococcus aureus strains poses a significant public health challenge, highlighting the need for novel antimicrobial agents. Filamentous fungi are prolific producers of bioactive secondary metabolites, yet many fungal taxa remain underexplored. In this study, ten fungal strains isolated from brown rice were cultured in Czapek–Dox broth and yeast malt broth to prepare crude extracts, which were screened for antibacterial activity against methicillin-sensitive (MSSA), methicillin-resistant (MRSA), vancomycin-intermediate (VISA), and vancomycin-resistant (VRSA) S. aureus isolates. Most extracts exhibited weak to moderate activity, whereas Acremonium sp. USSc24 displayed striking and consistent antibacterial effects, particularly in extracts produced from yeast malt broth. Disc diffusion and minimum inhibitory concentration assays confirmed broad-spectrum activity against MSSA, MRSA, and VISA strains, with no detectable inhibition of VRSA. Bioautography-guided fractionation localized antibacterial activity to a specific chromatographic fraction, and gas chromatography–mass spectrometry (GC–MS) analysis identified a chemically diverse mixture of compounds, including caryophyllene oxide, tetradecanamide, octadecenamide, and other sesquiterpenes, many of which have reported antimicrobial properties. These results suggest that the observed antibacterial activity is likely due to synergistic interactions among multiple secondary metabolites. Collectively, this study highlights Acremonium sp. USSc24 as a promising source of antibacterial compounds and provides a foundation for future isolation, structural elucidation, and in vivo evaluation of bioactive metabolites against drug-resistant S. aureus.
Polycystic kidney disease (PKD) is a genetic disorder characterized by the growth of numerous fluid-filled cysts in the kidneys. Ivermectin is an antiparasitic drug that has been reported to function as an agonist of the farnesoid X receptor (FXR). Activation of FXR has previously been shown to attenuate cyst progression. In the present study, we evaluated the pharmacological effects of ivermectin on renal cyst progression in vivo in a rat model of PKD and in vitro in renal cell-derived cysts. Daily subcutaneous administration of ivermectin (0.5 mg/kg body weight) for 12 weeks significantly reduced the kidney weight–to–body weight ratio and improved renal function in PKD rats compared with vehicle-treated controls. In addition, treatment with 2 µM ivermectin significantly inhibited Madin–Darby canine kidney (MDCK) cell-derived cyst formation by 31±5.3% compared to vehicle-treatment. These effects were associated with suppressed cell proliferation and reduced phosphorylation of extracellular signal-regulated kinases (ERK)1/2. In addition, ivermectin significantly attenuated in vitro cyst growth by 13±3.0% compared with control. This inhibitory effect on cyst growth was associated with reduced cystic fibrosis transmembrane conductance regulator (CFTR)– and TMEM16A-mediated chloride secretion by 36±3.1% and 12±2.8%, respectively, compared with control. Collectively, these findings demonstrate that ivermectin inhibits renal cyst progression both in vivo and in vitro, supporting its potential as a pharmacological modulator of cyst growth in PKD.
Exogenous hormones from food may accumulate in edible tissues, potentially increasing the health hazard to consumers. Their effects on metabolic disorders at low concentrations are poorly known. The aim of this study was to evaluate the effects of testosterone (TE), 17β-estradiol (E2) and melengestrol acetate (MGA) residues on some blood parameters to elucidate metabolic disorders in white mice. 112 Swiss Albino mice were divided into 4 groups including control group, TE-group, E2-group and MGA-group. Mice in test groups received oral TE 100 μg/kg, E2 100 μg/kg and MGA 50 μg/kg once daily, respectively. After 5 weeks, half of the mice were sacrificed, and the other half stopped receiving exogenous hormones for a week. Blood samples were collected at weeks 5 and 6 for biochemical parameters’ assessment. Results showed that after oral hormone administration for 5 weeks, plasma AST, cholesterol, triglycerides, total protein increased, while HDL-cholesterol decreased in TE-group compared to the control group (p<0.05). Cholesterol and triglycerides of TE-female group were different from the TE-male group p<0.05). After stopping hormone for 1 week, cholesterol, triglycerides, and total protein continued to increase, while HDL-cholesterol decreased insignificantly in the TE-group compared to the control group. AST activity of E2-group and glucose of the MGA-group continued to increased compared to the control group (p<0.05). The HDL-cholesterol of the MGA-female group was different from the MGA-male group (p<0.05). In conclusion, this study's findings serve as a warning that prolonged exposure to low concentrations of oral steroid hormones can cause changes in blood biochemical parameters.
Metformin-associated lactic acidosis (MALA) is a rare but potentially fatal condition characterized by bloodstream lactic acid levels exceeding 5.0 mmol/L, leading to acidemia (blood pH less than 7.35), with mortality rates reaching up to 50% if not promptly and appropriately managed. However, there is limited evidence regarding the risk factors associated with the occurrence of MALA in diabetic patients receiving metformin within the Thai context. The aim of research was to investigate factors associated with MALA in type 2 diabetic patients taking metformin. A retrospective matched case-control study was conducted in a total of 272 type 2 diabetic patients. Data were collected from Surin Hospital’s electronic medical records from 2017 to 2021. Descriptive statistics and Chi-square tests were used. Binary logistic regression analysis with Backward Likelihood ratio (LR) selection method was used to determine the optimal final model of the predictor of MALA occurrence, at significance level of 0.01. During the 5-year period, 58,206 patients received treatment with metformin and only 136 cases were diagnosed with MALA. The majority of participants were female (56.6%) and had an average age of 60 years. It was shown that history of using combined pain relief medications had a 38.29-fold higher likelihood of developing MALA compared to those who did not use this medication (OR = 38.29, 99% CI 5.96-245.87). This study highlighted the importance of implementing comprehensive monitoring system for diabetic patients, with consideration of identified risk factors. Such an approach can help reduce the risk of MALA and enhance patient safety and outcomes.
Southeast Asia's rapid growth of Universal Health Coverage (UHC) is increasingly hampered by growing healthcare costs and financial constraints. Although cost-containment instruments are widely implemented, their systemic trade-offs—particularly regarding health equity and service quality—remain poorly understood across the region's diverse health systems. This systematic review synthesizes empirical evidence on the effectiveness of supply-side and demand-side cost-containment instruments across five UHC outcome domains (financial protection, access, equity, quality, and efficiency) in Southeast Asian National Health Insurance schemes. Following PRISMA 2020 guidelines, we systematically searched Scopus and PubMed from inception to December 2025. Of 362 records, 21 empirical studies from five countries (Thailand, Indonesia, Vietnam, Philippines, Lao PDR) met inclusion criteria. Study quality was assessed using the Mixed Methods Appraisal Tool (MMAT). Evidence reveals a sharp divergence in policy performance. Synergistic strategic purchasing—exemplified by Thailand's integrated capitation, global budgets, and central procurement—achieved significant pro-poor equity (27–30% of subsidies concentrated in the poorest quintile) and 25% savings in pharmaceutical expenditures. Conversely, fragmented instruments in other settings triggered adverse provider behaviors, including cost-shifting to patients, induced utilization, and potential quality concerns. Even in relatively high-performing schemes, persistent inequities related to geography, gender, and chronic disease management remain unresolved. Cost-containment effectiveness depends fundamentally on governance maturity and policy integration, not technical design alone. To safeguard UHC sustainability, Southeast Asian policymakers should transition from fragmented cost-cutting toward data-driven, quality-linked strategic purchasing frameworks that actively monitor equity and outcomes.
Drug-related problems (DRPs) are a leading cause of treatment failure, hospital admissions, and mortality, particularly among older adults due to age-associated alterations in pharmacokinetics and pharmacodynamics. Vietnam is experiencing a rapidly aging population, with increasing rates of chronic diseases and polypharmacy, while its healthcare system continues to face challenges in delivering specialized geriatric care. This study aimed to evaluate the prevalence and determinants of DRPs in geriatric outpatient prescriptions and assess the impact of clinical pharmacist-led interventions on DRP reduction. A quasi-experimental study was conducted across three hospitals in Vietnam, analyzing prescriptions from patients aged ≥65 years. DRPs were identified and classified using the Pharmaceutical Care Network Europe (PCNE) criteria version 9.1. Clinical pharmacists implemented educational interventions targeting prescribers to address identified DRPs. Data were analyzed using descriptive statistics, t-tests or Mann-Whitney U tests for continuous variables, Chi-square tests for categorical variables, and multivariable logistic regression to identify factors associated with DRPs. In the pre-intervention phase, 1,651 prescriptions were reviewed; the mean patient age was 71.4 years, with 58.8% female. The proportion of prescriptions containing at least one DRP was 28.3%, with inappropriate drug indication being the most prevalent issue. Polypharmacy (≥5 medications) and a higher number of diagnoses per patient were significant predictors of DRPs. Post-intervention analysis demonstrated a statistically significant reduction in DRP prevalence. Clinical pharmacist-led interventions effectively reduced the prevalence of DRPs in geriatric outpatient settings (p < 0.001). These findings underscore the critical role of clinical pharmacists in optimizing medication regimens for older adults, thereby enhancing patient safety and treatment outcomes.
Ethosomes, a kind of vesicle, are microscopic structures that aid in the efficient delivery of drugs over the epidermal barrier by focusing their action on certain cells. Due to their unique composition and structural properties, ethosomes, which are innovative phospholipid vesicular carriers containing elevated concentrations of ethanol, provide efficient absorption and enhanced permeability through the skin. Pharmacosomes, which are drug-lipid complexes with improved drug dispersion and administration, are new drug delivery technologies being developed. Improved drug permeability and targeting are provided by sophisticated systems including aquasomes, cubosomes, and ethosomes, which increase the efficacy of drug delivery. Different techniques, including as the hot method, cold method, and dispersion approach, can be used to manufacture ethosomes, and each has an impact on the end product's properties. Ethosomes are a kind of lipid vesicle that show promise for drug delivery applications because they are flexible and enhance medication penetration into the circulation and deep skin layers. A comprehensive overview of drug delivery ethosomes, including their types, compositions, preparation methods, characterizations, marketed formulations, applications, and ultimately, future prospects, is also included in this article.
Ceftazidime (CP) is a third-generation bactericidal cephalosporin used to treat infections, such as pneumonia and meningitis. Despite its clinical use, the emerging threat of antimicrobial resistance makes the drug questionable. This study aims to entrap CP into niosomes, providing a unique mechanism for enhancing its antibacterial activity against selected pathogens. Five niosomal formulations with varying molar ratios of surfactant were prepared and tested for in vitro release and entrapment efficiency (EE). The most favorable formulation was further characterized using scanning electron microscopy (SEM), particle size (PS), polydispersity index (PDI), zeta potential (ZP), Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC). A three-month accelerated stability study was also conducted to determine its suitability under common storage conditions. The antibacterial activity against selected pathogens was assessed using the agar well diffusion method. The formulation containing the highest molar ratio of Span 60 was selected due to its superior entrapment efficiency (72.49 ± 0.23%) and diffusion performance (804.8 ± 145.4 μg/hr). This optimized formulation exhibited a spherical, vesicular morphology with favorable particle size, polydispersity index, and zeta potential. FTIR and DSC analyses confirmed successful entrapment of the active compound, while minimal changes in entrapment efficiency, zeta potential, and pH under cold storage indicated relative stability. Moreover, it demonstrated enhanced antibacterial activity against Klebsiella pneumoniae, Pseudomonas aeruginosa, and Staphylococcus aureus compared to the free drug. This study was the first to report that niosomal entrapment improves CP's antibacterial activity, establishing a framework for future advances in antimicrobial drug delivery.
Amorphous solid dispersions (ASDs) represent a promising approach to enhancing the oral bioavailability of poorly water-soluble drugs by forming stable, highly soluble amorphous states. Despite their advantages, significant challenges remain due to the metastable nature of ASDs, which often requires the incorporation of additives to inhibit crystallisation. This article explores the intricate interactions between drugs and polymers within ASDs, focusing on hydrogen bonding, ionic interactions, van der Waals forces, and hydrophobic interactions, and their roles in maintaining drug solubility and stability. It highlights that the drug release mechanism is complex and varies with drug loading, transitioning from polymer-controlled to drug-controlled release. Characterisation techniques such as thermal analysis, spectroscopy, and microscopy provide insights into the interactions and stability of ASDs. Despite advances, challenges remain regarding the complexity of interactions and the long-term stability of ASDs, necessitating further research into optimal polymer selection, drug-polymer ratios, and processing techniques. This study emphasises the need for a deeper understanding of drug-polymer interplay and its implications for the rational design of effective ASD formulations to improve drug delivery systems.
Carboplatin induced nephrotoxicity though life threatening with patients being treated symptomatically, has no specific drugs available for management. The current research was conducted to compare the nephroprotective potential of different doses of ethanolic leaf extract of Tinospora cordifolia (TC) against carboplatin-induced nephrotoxicity. 36 rats were divided into 6 groups (n=6). Groups 1 and 2 were given 1% sodium carboxymethylcellulose (CMC) 1ml/kg/day orally and TC extract, 400 mg/kg/day orally for 14 days respectively. Carboplatin 90 mg/kg intraperitoneal single dose was administered to group 3 on day 5. TC extract, 200, 400, and 600 mg/kg/day were administered to groups 4, 5, and 6 respectively for 14 days along with carboplatin on day 5. Serum was collected on days 0, 7, and 14 to evaluate renal function. Renal tissue was used to estimate antioxidant levels and for histopathological investigations. Results were analyzed using ANOVA followed by Tukey’s test and paired t-test. A significant (p<0.05) increase was seen in serum urea, creatinine and oxidative stress markers and reduction in antioxidants, catalase, total thiol, in the carboplatin-treated group as compared to control. All three doses of the ethanolic leaf extract of TC exhibited significant nephroprotective effects against carboplatin-induced nephrotoxicity, likely through antioxidant and anti-inflammatory mechanisms. This was supported by decreased levels of blood urea and serum creatinine, along with histopathological evidence of renal tissue recovery.
Polypharmacy and the use of potentially inappropriate medications (PIMs) are common among terminal cancer patients with multiple comorbidities. These are associated with increased treatment burden, diminished quality of life, and adverse clinical outcomes. This study investigates the prevalence, patterns, and associated risk factors of polypharmacy and PIMs use among hospice patients at a community hospital in Thailand. A descriptive, retrospective cross-sectional study was conducted among cancer patients aged ≥20 years who attended palliative care clinics at a community hospital between January 2018 and December 2023. Patients receiving active anticancer treatment were excluded. Polypharmacy was defined as the concurrent use of five or more medications. PIMs were identified using the STOPP-Frail, and the OncPal criteria. Logistic regression analysis was performed to identify factors associated with polypharmacy and PIMs use. A total of 65 patients were included (61.5% male; mean age 70.4 years). Polypharmacy was observed in around 40.0% during the last 6 months of life. PIMs use was found in 64.6%- 72.3% in the same periods. Antihypertensives, lipid-lowering agents, and vitamins/minerals were the most prescribed drugs. During the final six months, patients with more than two comorbidities had an increased risk of receiving PIMs when on polypharmacy. Polypharmacy was significantly associated with PIMs use in the final three and one months of life, with multivariate analysis confirming the association during the last three months. Polypharmacy and PIMs use are increasingly prevalent among terminal cancer patients receiving hospice care in Thailand. In the future, implementing systematic deprescribing strategies may help ensure appropriate medication use and improve the quality of end-of-life care.
Psoriasis is chronic inflammatory skin disease arbitrated by the immune system, so the inflammatory response portrays a vital role in the progress and severity of this disease. Unfortunately, conventional psoriasis treatment currently has limitations, including, expensive, has a high risk of side effects and worsening the prognosis of psoriasis if treatment is stopped. Therefore, the development of effective and efficient herbal medicine is desired to treat psoriasis. This research is designed to prove the huge potential of nanoemulgel containing Jatropha curcas leaves extract (JCE-NE-gel) as a topical treatment for psoriasis. This study used 24 BALB/c mice induced with 62.5 mg imiquimod cream 5% twice a day for 7 consecutive days. In addition, the effectiveness of JCE-NE-gel as anti-psoriasis was evaluated using PASI scores, epidermis thickness via histopathology and TNF-α expression via immunohistochemistry. The results of in vivo studies showed that the 2.5% JCE-NE-gel group was able to improve the physiological appearance of psoriasis skin on the 14th day of the study. It was also able to reduce the PASI score for 66.7% (p < 0.05). In addition, histopathological results showed a significant decrease in the epidermis thickness of 2.5% JCE-NE-gel group mice for 78.9% (p < 0.05). A decrease in TNF-α expression was also seen in the 2.5% JCE-NE-gel group for 56.9% (p < 0.05). This research proves that the nano formulation was able to increase the permeability of Jatropha curcas leaves extract into the epidermis and dermis of the skin. This study also proves that nanoemulgel formulation loaded Jatropha curcas extract (JCE-NE-gel) could be reflected as a promising treatment for psoriasis disorders via suppressing TNF-α expression.
Oral administration of a drug is the most common, ideal and preferred route of administration. The main problem of oral drug formulations is their low bioavailability arising from poor aqueous solubility of drugs. The study developed bilastine-loaded lipid-based self-nanoemulsifying drug delivery systems (SNEDDS) in liquid formulations. The components used in the SNEDDS formulations included lipid (Capmul PG-NF), surfactant (Tween 40), and co-surfactant (Plurol Oleique). The optimized formulation was characterized through in-vivo analysis. The liquid-SNEDDS (L-SNEDDS) formulation [TP3PO1 (2:8)] demonstrated greater potential, showing a reduced particle size of 142.5nm, zeta potential −22.6mV, PDI 0.183, and a drug loading efficiency of 99.71 ± 0.67%, respectively. The optimized formulation of L-SNEDDS [TP3PO1 (2:8)] showed a stable nanoemulsion, and FT-IR studies indicated no interaction between the drug and excipients. The in-vivo pharmacokinetic study of the optimized bilastine-loaded L-SNEDDS formulation performed using albino rats (weight of single rat 250±25 g) showed that the area under the curve AUC0–24 for the optimized formulation [TP3PO1 (2:8)] was significantly higher 1129.45 ± 10.815 µg/mL/h compared to the drug suspension 179.96 ± 2.368 µg/mL/h. Cmax was also higher for TP3PO1 (2:8) 90.368 ± 2.596 µg/mL compared to the drug suspension 34.32 ± 2.31µg/mL. The plasma half-life (t1/2) of the optimized formulation TP3PO1 (2:8) was increased significantly 22.45 ± 0.251 hrs compared to that of the drug suspension 18.57 ± 0.312 hrs. Overall, a range of lipid-based SNEDDS liquid formulations was successfully developed and appears to be a promising alternative for improving the solubility of poorly water-soluble drugs and evaluating pharmacokinetic parameters.
Boesenbergia rotunda (L.) extract is characterized by the presence of pinostrobin (PNS) as its major active component. PNS expresses several pharmacological activities such as antioxidant, anti-inflammatory, antiviral, anticancer, and anti-aromatase activities. Similar to other flavonoids, PNS has poor water solubility, resulting in low bioavailability and limiting its clinical application. These physicochemical constraints pose significant challenges for effective transdermal delivery, particularly in achieving sufficient drug penetration across the stratum corneum. To address these limitations, the development of an effective drug delivery system that can improve both the solubility and transdermal permeation of PNS is warranted. This study aimed to develop an optimized microemulsion (ME) formulation for the transdermal delivery of B. rotunda extract, focusing on PNS. Various oils, surfactants, and co-surfactants were screened, and different surfactant to co-surfactant ratios were evaluated through pseudo-ternary phase diagrams and optimized using Design Expert software. The developed ME was characterized for physical appearance, droplet size, polydispersity index (PDI), zeta potential, pH, entrapment efficiency, in vitro release and ex vivo skin permeation. For the result, the optimized formulation was with a fixed surfactant to co-surfactant ratio of 3:1. The optimized ME consisted of 63.34% Labrasol® and Transcutol®, 18.33% limonene, and 18.33% water, which the mean droplet size, PDI, zeta potential and entrapment efficiency were discovered as 156.00.80 nm, 0.210.02, 0.050.03 mV, and 99.79%, respectively. In vitro drug release studies demonstrated that the ME exhibited a higher release rate than the oil solution but a lower release rate than the extract in ethanol solution over a 24-hour period. Ex vivo skin permeation studies revealed that the optimized ME demonstrated significantly higher skin permeation than the control formulations. In conclusion, these findings suggest that the developed ME is a promising carrier system for enhancing the transdermal delivery of PNS.
