Journal of Pharmacy and Pharmacology最新文献

Viscoelastic properties of polymer mixtures containing micro-ribbons and microfibres for the 3D printing of pharmaceutical dosage forms by fused deposition modelling. 含有微带和微纤维的聚合物混合物的粘弹性特性，用于熔融沉积建模的药物剂型3D打印。

IF 3.2 4区医学

Journal of Pharmacy and Pharmacology Pub Date : 2026-05-02 DOI: 10.1093/jpp/rgag044

Marwan Algellay, Satyajit D Sarker, Matthew Roberts, Lucy A Bosworth, Touraj Ehtezazi

{"title":"Viscoelastic properties of polymer mixtures containing micro-ribbons and microfibres for the 3D printing of pharmaceutical dosage forms by fused deposition modelling.","authors":"Marwan Algellay, Satyajit D Sarker, Matthew Roberts, Lucy A Bosworth, Touraj Ehtezazi","doi":"10.1093/jpp/rgag044","DOIUrl":"https://doi.org/10.1093/jpp/rgag044","url":null,"abstract":"Objectives: To match the disintegration time of conventional oral films with 3D printed fast-dissolving oral films (FDFs), micro-composites have been used in the formulation. However, in certain cases the 3D-printer failed to produce desired films.Methods: The viscoelastic properties were evaluated for polyvinyl alcohol and polyvinylpyrrolidone filaments containing chitosan micro-ribbons and cellulose microfibres as micro-composites with the hypothesis that intermittent nozzle blockage was the mechanism responsible for the observed printing failures.Key findings: Domination of loss modulus over storage modulus was observed for successful printing. Micro-composites improved the viscoelastic properties of filaments including filaments that failed to print. The novelty of this research was that poor viscoelastic properties could not be accounted for the failure of FDF 3D printing for formulations with high micro-composite contents. Filaments of these formulations exhibited rough surfaces with visible aggregates. These observations suggested intermittent nozzle blockage by aggregated micro-composites could have been the cause of 3D printing failure. This hypothesis was supported by successful printing when printer nozzle diameter increased.Conclusions: The domination of loss modulus over storage modulus was essential for filaments to achieve successful FDF 3D printing. However, micro-composites at high concentrations in the formulation may induced nozzle blockage leading to printing failures.","PeriodicalId":16960,"journal":{"name":"Journal of Pharmacy and Pharmacology","volume":"78 5","pages":""},"PeriodicalIF":3.2,"publicationDate":"2026-05-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147839364","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Effect of Tribulus terrestris L. extract in the management of polycystic ovarian syndrome in rat model. 蒺藜提取物对多囊卵巢综合征大鼠模型的治疗作用。

IF 3.2 4区医学

Journal of Pharmacy and Pharmacology Pub Date : 2026-05-02 DOI: 10.1093/jpp/rgag042

Hadia Abdul Qayyum, Haseeb Anwar, Ghulam Hussain, Arslan Iftikhar, Imran Mukhtar, Sidra Altaf, Humaira Muzaffar

{"title":"Effect of Tribulus terrestris L. extract in the management of polycystic ovarian syndrome in rat model.","authors":"Hadia Abdul Qayyum, Haseeb Anwar, Ghulam Hussain, Arslan Iftikhar, Imran Mukhtar, Sidra Altaf, Humaira Muzaffar","doi":"10.1093/jpp/rgag042","DOIUrl":"https://doi.org/10.1093/jpp/rgag042","url":null,"abstract":"Objectives: Oxidative stress is considered to be a significant factor in the complex disorder known as polycystic ovarian syndrome (PCOS). In this study, we investigated whether using the traditional medicinal plant Tribulus terrestris L. to lower oxidative stress could help alleviate the symptoms of PCOS.Methods: In this randomized controlled trial, rats were given oral estradiol (4 mg/kg/bw) to induce PCOS, and they were split into four groups: treatment (T. terrestris L. extract, 7 mg/kg/bw), standard control (metformin, 300 mg/kg/bw), positive control, and negative control. Blood and ovarian tissues were taken for histological, hormonal, molecular, and biochemical examinations after 21 days.Key findings: Treatment with T. terrestris L. extract resulted in decreased levels of FSH, LH, estrogen, insulin, TOS, and MDA, as well as downregulated expression of IL-6, IL-1, IGF-1, and CYP-19, in comparison to the positive control. Histological examination revealed healthier ovarian morphology with more corpus luteum and fewer cystic follicles, and TAC levels rose.Conclusion: The results imply that T. terrestris may help combat hormonal disruption and oxidative stress in PCOS, but human studies are still required for confirmation.","PeriodicalId":16960,"journal":{"name":"Journal of Pharmacy and Pharmacology","volume":"78 5","pages":""},"PeriodicalIF":3.2,"publicationDate":"2026-05-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147839429","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

A novel Platycladus orientalis essential oil with functional properties: antioxidant defense, cognitive improvement, and immune enhancement for potential nutraceutical use. 一种具有抗氧化防御、改善认知和增强免疫功能的新型侧柏精油，具有潜在的营养保健用途。

IF 3.2 4区医学

Journal of Pharmacy and Pharmacology Pub Date : 2026-05-02 DOI: 10.1093/jpp/rgag045

Mengyuan Zhu, Xuanqi Fu, Yue Lv, Puyou Liao, Xiang Wang, Pengfei Cui

{"title":"A novel Platycladus orientalis essential oil with functional properties: antioxidant defense, cognitive improvement, and immune enhancement for potential nutraceutical use.","authors":"Mengyuan Zhu, Xuanqi Fu, Yue Lv, Puyou Liao, Xiang Wang, Pengfei Cui","doi":"10.1093/jpp/rgag045","DOIUrl":"https://doi.org/10.1093/jpp/rgag045","url":null,"abstract":"Context: A specialized essential oil extracted from the heartwood of Platycladus orientalis via supercritical CO₂ extraction shows distinct chemical and physicochemical properties compared with conventional leaf-derived oil, with potential applications in functional foods and alternative medicine.Objective: To systematically evaluate the acute toxicity, antioxidant capacity, memory-enhancing effects, and immunomodulatory properties of wood-derived P. orientalis essential oil (POEO), and to explore its multi-target mechanisms via molecular docking.Material and methods: The oil was extracted using supercritical CO₂. We tested its acute toxicity in mice. Its antioxidant, memory-enhancing, and immune-boosting effects were measured using standardized biological tests. We also used computer simulations (molecular docking) to see how the oil's key compounds might interact with specific target proteins in the body.Results: POEO demonstrated a favourable safety profile with low acute toxicity, while also significantly enhancing the body's natural antioxidant defenses. Furthermore, medium and high doses improved spatial memory in mice and strongly enhanced immune responses, notably increasing natural killer cell activity by 98%. Molecular docking suggested potential interactions between major POEO constituents and several proteins associated with antioxidant, neurological, and immune pathways. These findings provide preliminary insights into possible molecular targets and generate hypotheses for future mechanistic investigations. POEO is safe and shows strong potential as a natural product for improving antioxidant status, memory, and immune function. It's observed bioactivity and predicted multi-target interactions support its potential for further development in functional foods and alternative medicine.","PeriodicalId":16960,"journal":{"name":"Journal of Pharmacy and Pharmacology","volume":"78 5","pages":""},"PeriodicalIF":3.2,"publicationDate":"2026-05-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147839436","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Oleanolic acid ameliorates collagen induced arthritis in rats through the gut microbiota. 齐墩果酸通过肠道菌群改善大鼠胶原诱导的关节炎。

IF 3.2 4区医学

Journal of Pharmacy and Pharmacology Pub Date : 2026-05-02 DOI: 10.1093/jpp/rgag040

Chipu Liu, Yue Zhao, Xiaoran Su, Yajie Sun, Yugai Jia

{"title":"Oleanolic acid ameliorates collagen induced arthritis in rats through the gut microbiota.","authors":"Chipu Liu, Yue Zhao, Xiaoran Su, Yajie Sun, Yugai Jia","doi":"10.1093/jpp/rgag040","DOIUrl":"https://doi.org/10.1093/jpp/rgag040","url":null,"abstract":"Objectives: Oleanolic acid (OA) is a natural anti-inflammatory triterpenoid. This study investigates its therapeutic potential against rheumatoid arthritis (RA), a chronic autoimmune condition characterized by inflammatory activity, and explores the novel mechanism of gut microbiota modulation in a rat model.Methods: The anti-arthritic effect of OA was assessed in collagen-induced arthritis (CIA) in rats following oral or intravenous administration. Arthritis severity, joint pathology, and mesenteric Th17/Treg cell frequencies were evaluated. The role of gut microbiota was investigated using 16S rRNA sequencing and antibiotic ablation.Key findings: Oral, but not intravenous, OA administration significantly alleviated arthritis and joint damage in CIA rats, indicating a gastrointestinal-dependent mechanism. Therapeutically, oral OA modulated gut microbiota by reducing Prevotella abundance and restored immune balance by decreasing Th17 and increasing Treg cell frequencies. This protective effect was abolished by co-treatment with antibiotics, confirming gut microbiota-dependency.Conclusions: Taken together, our findings show that the improvement in CIA after oral administration of OA is mainly due to changes in the structure and function of the gut microbiota. This study, therefore, suggests that OA is a promising therapeutic candidate for RA, based on its ability to restore the intestinal microenvironment.","PeriodicalId":16960,"journal":{"name":"Journal of Pharmacy and Pharmacology","volume":"78 5","pages":""},"PeriodicalIF":3.2,"publicationDate":"2026-05-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147816555","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Modulation of vascular remodeling and vasoconstriction by α-phellandrene in hypoxia-induced pulmonary hypertension. α-茶树烯对缺氧肺动脉高压血管重构和血管收缩的调节作用。

IF 3.2 4区医学

Journal of Pharmacy and Pharmacology Pub Date : 2026-05-02 DOI: 10.1093/jpp/rgag046

Zhan Ting Yang, Yi Wen Wang, Hai Jun Bai, Xu Pan, Dian Xiang Lu, Zhan Qiang Li, Gu Yue Bai, Hui Yang

{"title":"Modulation of vascular remodeling and vasoconstriction by α-phellandrene in hypoxia-induced pulmonary hypertension.","authors":"Zhan Ting Yang, Yi Wen Wang, Hai Jun Bai, Xu Pan, Dian Xiang Lu, Zhan Qiang Li, Gu Yue Bai, Hui Yang","doi":"10.1093/jpp/rgag046","DOIUrl":"https://doi.org/10.1093/jpp/rgag046","url":null,"abstract":"Objectives: This study investigated α-phellandrene (PE)'s therapeutic effects on hypoxia-induced pulmonary hypertension (HPH), with emphasis on pulmonary vasoconstriction and vascular remodeling.Methods: A rat model of HPH was successfully established and then the hemodynamic indexes were assessed. HE and Masson's staining were performed to observe tissue morphological changes and fibrosis. Immunohistochemistry and immunofluorescence were used to quantify Collagen I/III, and alpha-smooth muscle actin (α-SMA). malondialdehyde, glutathione, superoxide dismutase, and glutathione peroxidase assays for antioxidant status. Western blotting to analyse the protein expression levels in lung tissue of HPH rats.Key findings: Our results indicate that PE significantly mitigated HPH, as evidenced by reductions in right ventricular (RV) systolic pressure, RV hypertrophy (evaluated via the RV/BW ratio and Fulton index), and key structural changes. PE effectively diminished pulmonary vascular remodeling, demonstrated by decreased vascular wall thickness and area, along with downregulation of Collagen I/III and α-SMA expression. Mechanistically, the protective effects of PE were associated with modulation of the AKT/eNOS/sGC/PKG pathway, a critical regulator of vascular tone and remodeling, as well as a reduction in oxidative stress and apoptosis.Conclusion: These findings highlight that PE alleviates HPH through a multifaceted approach targeting vasoconstriction and vascular remodeling, underscoring its potential as a novel therapeutic agent.","PeriodicalId":16960,"journal":{"name":"Journal of Pharmacy and Pharmacology","volume":"78 5","pages":""},"PeriodicalIF":3.2,"publicationDate":"2026-05-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147839420","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Cynandione A improves white adipose tissue homeostasis in high-fat diet-fed mice. Cynandione A改善高脂肪喂养小鼠的白色脂肪组织稳态。

IF 3.2 4区医学

Journal of Pharmacy and Pharmacology Pub Date : 2026-05-02 DOI: 10.1093/jpp/rgag038

Atsushi Sawamoto, Misaki Shiba, Satoshi Okuyama, Chan Jae Cho, Jae Hyun Kim, Mitsunari Nakajima

{"title":"Cynandione A improves white adipose tissue homeostasis in high-fat diet-fed mice.","authors":"Atsushi Sawamoto, Misaki Shiba, Satoshi Okuyama, Chan Jae Cho, Jae Hyun Kim, Mitsunari Nakajima","doi":"10.1093/jpp/rgag038","DOIUrl":"https://doi.org/10.1093/jpp/rgag038","url":null,"abstract":"Objectives: Cynandione A (CA), a major bioactive compound isolated from Cynanchum wilfordii Radix, is a crude drug traditionally used in East Asia. We have previously demonstrated that CA induces a beige adipocyte-like phenotype in vitro. This study aimed to investigate the in vivo effects of CA on white adipose tissue (WAT) function.Methods: C57BL/6 J mice were fed a high-fat diet (HFD) and administered CA (5 or 15 mg/kg, intraperitoneally, once daily) for eight weeks. Body weight, glucose tolerance, insulin sensitivity, and serum parameters were evaluated. Histological analyses of WAT and liver were performed, and gene and protein expression related to beige adipocyte features and mitochondrial biogenesis were assessed in inguinal WAT (iWAT).Key findings: CA treatment did not affect body weight, glucose tolerance, insulin sensitivity, or serum parameters. However, adipocyte size was significantly reduced in inguinal and epididymal WAT in mice treated with CA at 15 mg/kg (43.8% reduction, P < .001; 33.1% reduction, P = .021, respectively). Moreover, CA increased the expression of beige adipocyte-specific genes (Tmem26, 2.8-fold, P < .001; Cd137, 3.8-fold, P < .001) and mitochondrial marker proteins (UCP1, 2.1-fold, P = .007; TOM20, 2.2-fold, P < .001; VDAC, 1.6-fold, P = .019) in iWAT.Conclusions: CA modulates WAT plasticity and improves WAT homeostasis in HFD-fed mice.","PeriodicalId":16960,"journal":{"name":"Journal of Pharmacy and Pharmacology","volume":"78 5","pages":""},"PeriodicalIF":3.2,"publicationDate":"2026-05-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147816451","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Geraniol induces apoptosis in gastric cancer cells by inhibiting the Wnt/β-catenin pathway. 香叶醇通过抑制Wnt/β-catenin通路诱导胃癌细胞凋亡。

IF 3.2 4区医学

Journal of Pharmacy and Pharmacology Pub Date : 2026-04-03 DOI: 10.1093/jpp/rgag034

Xiao-Lan Yu, Si-Jia Guo, Qi-Rui Cai, Zi-Wen Guo, Hong-Wei Dong, Qi Wang, Shu-Jun Zhang, Jia-Ren Liu

{"title":"Geraniol induces apoptosis in gastric cancer cells by inhibiting the Wnt/β-catenin pathway.","authors":"Xiao-Lan Yu, Si-Jia Guo, Qi-Rui Cai, Zi-Wen Guo, Hong-Wei Dong, Qi Wang, Shu-Jun Zhang, Jia-Ren Liu","doi":"10.1093/jpp/rgag034","DOIUrl":"https://doi.org/10.1093/jpp/rgag034","url":null,"abstract":"Significance: Geraniol (GI), an acyclic monoterpene alcohol, exhibits diverse anti-cancer activities. However, its potential effects against gastric cancer remain poorly understood.Aims: The present study aimed to explore whether GI promotes apoptosis in gastric cancer cells, and decipher the possible mechanism underlying this effect.Methods: The cell viability and cell cycle distribution of SGC-7901 cells and MKN45 cells were evaluated using MTT assay, MB assay, and flow cytometry. The expression of Bax, Bcl-2, and glycogen synthase kinase-3 (GSK-3β) proteins, the mitochondrial membrane potential (MMP), and cell apoptosis in SGC-7901 cells were determined using Western blotting, JC-1 staining, immunofluorescence analysis, and Annexin V/propidium iodide double staining. In addition, cell apoptosis and the expression of proliferating cell nuclear antigen, Cleaved-caspase-3, Bax, Bcl-2, and GSK-3β proteins in the xenografts were determined using terminal deoxynucleotidyl transferase biotin-dUTP nick-end labeling, immunohistochemistry, and Western blotting.Key findings: GI significantly inhibited the viability of gastric cancer cells and arrested the cell cycle at the G0/G1 phase in a dose-dependent manner. GI also promoted apoptosis and decreased the MMP in gastric cancer cells. Moreover, GI significantly upregulated the Bax/Bcl-2 ratio and downregulated the expression of pGSK-3β and β-catenin both in vitro and in vivo, while increasing the expression of Cleaved-caspase-3 in SGC-7901 cell xenografts. Furthermore, GI reversed the anti-apoptotic effect of the GSK-3β inhibitor-LiCl, confirming its pro-apoptotic role.Conclusion: GI suppresses gastric cancer progression both in vitro and in vivo, by inducing apoptosis through inhibition of the Wnt/β-catenin pathway.","PeriodicalId":16960,"journal":{"name":"Journal of Pharmacy and Pharmacology","volume":"78 4","pages":""},"PeriodicalIF":3.2,"publicationDate":"2026-04-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147619044","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Pharmacological evaluation of Orai-1 inhibitor in 3-nitropropionic acid-induced Huntington disease. Orai-1抑制剂在3-硝基丙酸诱导的亨廷顿病中的药理学评价。

IF 3.2 4区医学

Journal of Pharmacy and Pharmacology Pub Date : 2026-04-03 DOI: 10.1093/jpp/rgag030

Veerta Sharma, Shareen Singh, Thakur Gurjeet Singh

{"title":"Pharmacological evaluation of Orai-1 inhibitor in 3-nitropropionic acid-induced Huntington disease.","authors":"Veerta Sharma, Shareen Singh, Thakur Gurjeet Singh","doi":"10.1093/jpp/rgag030","DOIUrl":"https://doi.org/10.1093/jpp/rgag030","url":null,"abstract":"Objectives: Huntington's disease (HD) is a neurodegenerative condition characterized by a gradual decline in motor skills, cognitive function, and mental health. The 3-nitropropionic acid (3-NPA) model simulates HD-like pathology, which involves calcium dysregulation. To establish a structural basis for targeting Orai-1, in-silico docking was conducted prior to assessing the neuroprotective effects of the Orai-1 inhibitor Synta-66 in a 3-NPA-induced HD model.Methods: Mice were randomly divided into five groups (n = 8): normal control, 3-NPA (10 mg/kg, i.p.), 3-NPA combined with tetrabenazine (3 mg/kg, i.p.), 3-NPA combined with Synta-66 (5 mg/kg, i.p.), and 3-NPA combined with Synta-66 (10 mg/kg, i.p.). In-silico docking was used to evaluate the interactions of Synta-66 with Orai-1 and other targets related to neurodegeneration. Various parameters including behavioural, biochemical, oxidative stress, and neuroinflammatory markers were assessed. Additionally, the ELISA expression of Orai-1 protein and Ca2+ levels were measured.Key findings: In-silico analysis revealed that Synta-66 binds effectively with Orai-1 and its related targets. In vivo studies showed that 3-NPA caused notable motor impairments, biochemical changes, neuroinflammation, and disruptions in Ca2+ regulation. Administration of Synta-66 led to a dose-dependent recovery of body weight, enhancement of behavioural performance, normalization of biochemical and neuroinflammatory indicators, and a decrease in Orai-1 protein levels and intracellular Ca2+ concentrations, similar to the effects of tetrabenazine.Conclusion: The findings suggest the therapeutic potential of targeting Orai-1 channel using the inhibitor Synta-66 could serve as a neuroprotective treatment in a 3-NPA-induced HD model in mice.","PeriodicalId":16960,"journal":{"name":"Journal of Pharmacy and Pharmacology","volume":"78 4","pages":""},"PeriodicalIF":3.2,"publicationDate":"2026-04-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147674407","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Compaction of co-amorphous griseofulvin/amino acid powders at elevated temperatures and their "in-tablet" stability. 非晶灰黄霉素/氨基酸粉末在高温下的压实及其片内稳定性。

IF 3.2 4区医学

Journal of Pharmacy and Pharmacology Pub Date : 2026-04-03 DOI: 10.1093/jpp/rgag035

Ioannis Partheniadis, Maria Tsouka, Ioannis Nikolakakis

{"title":"Compaction of co-amorphous griseofulvin/amino acid powders at elevated temperatures and their \"in-tablet\" stability.","authors":"Ioannis Partheniadis, Maria Tsouka, Ioannis Nikolakakis","doi":"10.1093/jpp/rgag035","DOIUrl":"https://doi.org/10.1093/jpp/rgag035","url":null,"abstract":"Objectives: Equimolar griseofulvin (GRI) co-amorphous systems (CAMS) with amino-acids (AAs) were prepared by hot-melt-extrusion and evaluated for compactibility and \"in-tablet\" stability at ambient (21-23°C), intermediate (43-46°C), and high temperature [87-92°C, near CAMS' glass transition (Tg)].Methods: Compression was studied by \"in-die\" measurements. Tablet strength and morphology were evaluated by diametrical compression and electron microscopy, moisture uptake by dynamic sorption, and solid-state stability by X-ray powder diffraction and micro-spatially offset low-frequency Raman spectroscopy.Key findings: CAMS powders exhibited lower Heckel yield pressure (Py) and compaction work (Wc) but higher elastic recovery than crystalline physical mixtures (PMs). However, the strength of PM and CAMS tablets prepared at low or intermediate temperatures were comparable, due to balancing the effects of deformability (Py) and surface interaction (Wc). Compression near CAMS' Tg gave weak tablets. CAMS tablets exhibited low moisture sorption and remained amorphous after 90 days at 45°C/75% relative humidity, confirming excellent stability, whereas tablets of amorphous drug recrystallized after 30 days. Low-frequency Raman spectroscopy revealed details that escaped crystallography. Isolated residual drug crystals were detected, suggesting further finer-tuning for optimal GRI/AA ratio.Conclusion: These findings indicate the potential of GRI/AA CAMS for direct compression providing that adequate flowability is assured.","PeriodicalId":16960,"journal":{"name":"Journal of Pharmacy and Pharmacology","volume":"78 4","pages":""},"PeriodicalIF":3.2,"publicationDate":"2026-04-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147674404","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Attenuation of cerebral ischemia-reperfusion injury by exogenous hydrogen sulphide: involvement of the Nrf2/HO-1 pathway in NLRP3 inflammasome inhibition. 外源性硫化氢对脑缺血再灌注损伤的减弱：Nrf2/HO-1通路参与NLRP3炎性体抑制。

IF 3.2 4区医学

Journal of Pharmacy and Pharmacology Pub Date : 2026-04-03 DOI: 10.1093/jpp/rgag032

Wei Hua, Yilei Sun, Mingze Sun, Yiying Liu, Hongxue Sun, Huinan Chen, Weihua Zhang, Shuainan Ma

{"title":"Attenuation of cerebral ischemia-reperfusion injury by exogenous hydrogen sulphide: involvement of the Nrf2/HO-1 pathway in NLRP3 inflammasome inhibition.","authors":"Wei Hua, Yilei Sun, Mingze Sun, Yiying Liu, Hongxue Sun, Huinan Chen, Weihua Zhang, Shuainan Ma","doi":"10.1093/jpp/rgag032","DOIUrl":"https://doi.org/10.1093/jpp/rgag032","url":null,"abstract":"Objectives: Cerebral ischemia-reperfusion injury (CIRI) presents a major therapeutic challenge in stroke management, where oxidative stress and neuroinflammation synergistically exacerbate neuronal damage. This study examined whether exogenous hydrogen sulphide (H₂S) protects against CIRI by simultaneously modulating the nuclear erythroid 2-related factor 2 (Nrf2)/heme oxygenase 1 (HO-1) antioxidant response and inhibiting nuclear factor kappa-B (NF-κB) and Nod-like receptor (NLR) family, pyrin domain-containing 3 (NLRP3) inflammasome engagement in mice.Methods: Animal models were subjected to middle cerebral artery occlusion and reperfusion (MCAO/R) in mice, and neurological deficits were subsequently assessed using a rating scale and 2,3,5-triphenyltetrazolium chloride (TTC) staining to evaluate MCAO/R damage. The expression level of reactive oxygen species (ROS) was detected using an assay kit. The levels of Nrf2/HO-1 pathway and NLRP3 inflammasome were examined by Western blot and immunohistochemical staining.Key findings: The experimental data showed that exogenous administration of H₂S was effective in improving behavioral disorders and reducing infarct volume. Treatment with exogenous H₂S regulated the expression of the Nrf2/HO-1 signalling pathway, while H₂S effectively inhibited the expression of NF-κB and the formation of the NLRP3 inflammasome, as evidenced by reduced levels of phosphorylated NF-κB subunit p65 (p-p65), NLRP3, apoptosis-associated speck-like protein (ASC), and activated Caspase-1, and led to decreased maturation of the proinflammatory cytokines interleukin (IL)-1β and IL-18.Conclusion: This study demonstrated that exogenous administration of H₂S exerted neuroprotective effects by regulating the Nrf2/HO-1 antioxidant pathway and inhibiting NLRP3 inflammasome activation.","PeriodicalId":16960,"journal":{"name":"Journal of Pharmacy and Pharmacology","volume":"78 4","pages":""},"PeriodicalIF":3.2,"publicationDate":"2026-04-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147674437","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0