Pharmacia最新文献

{"title":"Enhanced sensitivity of nasopharyngeal carcinoma cells to cisplatin by triptolide: in vitro analysis of synergistic effects and mechanisms","authors":"Pingping Sun, J. Yan, Yao Zeng, J Chen, Shuxia Li","doi":"10.3897/pharmacia.72.e164874","DOIUrl":"https://doi.org/10.3897/pharmacia.72.e164874","url":null,"abstract":"Cisplatin (DDP) resistance severely limits the efficacy of chemotherapy for nasopharyngeal carcinoma (NPC). This study investigated the potential of triptolide (TPL) to enhance DDP sensitivity in human nasopharyngeal carcinoma CNE-1 cells and explored the underlying mechanisms. Apoptosis was assessed by Hoechst 33528 staining and flow cytometry. Gene and protein expression of Bcl-2 family members (Bcl-2 and Bax) and MAPK pathway activation (ERK1/2 and JNK) were analyzed using real-time PCR and western blotting. Our data revealed that TPL exerts concentration-dependent pro-apoptotic effects and synergistically augments the anti-proliferative effects of DDP on CNE-1 cells, with combined treatment inducing apoptosis more potently than either agent alone. The TPL+DDP group exhibited marked Bcl-2 suppression at both the transcriptional and translational levels, coupled with Bax upregulation at the transcriptional level compared with monotherapy, while Bax protein expression remained unchanged. Furthermore, TPL selectively activated MAPK signaling, significantly increasing phosphorylation of ERK1/2 and JNK, whereas no activation was observed for p38. Collectively, TPL enhances DDP sensitivity by modulating the Bcl-2/Bax balance and engaging ERK/JNK pathways, suggesting its clinical potential as a chemosensitizer in NPC treatment.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":"72 1","pages":"1-10"},"PeriodicalIF":0.0,"publicationDate":"2025-12-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pharmacia.pensoft.net/article/164874/download/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147897862","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Dual GLP-1/GIP agonist tirzepatide modulates hepatic mitochondrial fusion–fission gene expression and oxidative stress in diabetic rats","authors":"S. Fakhir, Inam Sameh Arif, Huda Jaber Waheed","doi":"10.3897/pharmacia.72.e175259","DOIUrl":"https://doi.org/10.3897/pharmacia.72.e175259","url":null,"abstract":"Type 2 diabetes mellitus (T2DM) is closely linked to oxidative stress–induced mitochondrial dysfunction, disrupting the balance between fusion and fission processes and driving hepatic injury. Tirzepatide (TZP), a dual GLP-1/GIP receptor agonist, is recognized for its potent glycemic and weight-lowering effects, yet its influence on hepatic mitochondrial dynamics in diabetes remains unclear. In this study, diabetes was induced in Wistar rats using a high-fat diet and streptozotocin, followed by treatment with varying doses of TZP. Diabetic animals exhibited marked hyperglycemia, insulin resistance, elevated lipid peroxidation, reduced antioxidant capacity, and altered expression of mitochondrial fusion and fission markers, accompanied by significant hepatic inflammation and degeneration. TZP administration improved glycemic indices, restored redox balance, enhanced the expression of fusion-related genes (Mfn1, Mfn2, Opa1), and suppressed the expression of fission-related genes (Drp1, Fis1) in a dose-dependent manner. Medium and high doses notably preserved liver histoarchitecture and reduced inflammatory changes. These findings suggest that TZP mitigates T2DM-associated hepatic injury by favoring mitochondrial fusion, alleviating oxidative stress, and protecting tissue integrity. The results provide mechanistic insights into TZP’s hepatoprotective potential and highlight the need for further validation at protein and functional levels.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":"72 1","pages":"1-16"},"PeriodicalIF":0.0,"publicationDate":"2025-11-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147333331","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Design and evaluation of electrospun fibers for unidirectional buccal delivery of atorvastatin","authors":"Zainab Farhan Muaiz, Masar Basim Mohsin Mohamed","doi":"10.3897/pharmacia.72.e167634","DOIUrl":"https://doi.org/10.3897/pharmacia.72.e167634","url":null,"abstract":"This study focused on atorvastatin calcium trihydrate (ATV), which is characterized by low bioavailability due to high intestinal metabolism and the hepatic first-pass effect. The buccal route is suitable for addressing ATV-related issues and aids in diminishing swallowing difficulties in older adults, the primary beneficiaries. The novelty of this work lies in the use of the electrospinning technique to produce ATV-loaded electrospun fibers, aiming to stabilize the drug in an amorphous form to enhance its dissolution in saliva and to incorporate it into a unidirectional tablet to control drug release in a single direction. ATV fibers were prepared using polyvinylpyrrolidone (PVP) with various co-solvents (propylene glycol, glycerin, Tween 80) and ethanol concentrations. The selected electrospun fibers formulated with a high amount of ethanol (F8) demonstrated 93.9% drug release, a disintegration time of 3 min, and nanosized fibers and were chosen for tablet preparations. The batches exhibited adequate mucoadhesion, and their drug release within 4 hours was 25.5%, 83.27%, 70.27%, and 100% for batches B1, B2, B3, and B4, respectively. The most prominent factor affecting the release rate was the addition of 7.5 mg of the super-disintegrant croscarmellose sodium. Permeation studies showed that 68.27% of ATV permeated through B4 over 24 hours, indicating that electrospun ATV-loaded PVP fibers can be efficiently formulated into mucoadhesive buccal tablets with rapid disintegration, drug release, and effective permeation, suggesting a strong prospect for buccal tablets in populations with swallowing difficulties.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":"72 1","pages":"1-13"},"PeriodicalIF":0.0,"publicationDate":"2025-10-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pharmacia.pensoft.net/article/167634/download/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147331323","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Development and characterization of furosemide-loaded binary amorphous solid dispersion to enhance solubility and dissolution for pediatric oral administration","authors":"Mays Fadhil Mohammed-Kadhum, Ghaidaa S. Hameed","doi":"10.3897/pharmacia.72.e156784","DOIUrl":"https://doi.org/10.3897/pharmacia.72.e156784","url":null,"abstract":"Binary co-amorphous systems, as solid dispersions of an active pharmaceutical ingredient with low molecular weight excipients, improve solubility, physical stability, and bioavailability relative to crystalline forms. This study aimed to enhance the solubility and dissolution of furosemide by developing a binary amorphous solid dispersion (BASD) and formulating it into granules for pediatric administration via a straw. Furosemide was blended with hydroxy methylcellulose E6, polyvinylpyrrolidone K30 (PVP), or Soluplus® in a 1:2 ratio using solvent evaporation, and the best formulation was produced via wet granulation. The furosemide-loaded BASD-PVP K30 (Formula F) demonstrated superior FTIR, DSC, and XRPD profiles. In vitro release testing showed that over 87.18% of furosemide was liberated within 120 minutes in a water solution containing 0.1% Tween 80. Moreover, the granules of Formula F9 exhibited excellent flow, disintegrated within 5–6 seconds, and released 79.86% of furosemide within four hours in a two-step dissolution study (0.1 N HCl and pH 6.8 phosphate buffer). Stability testing over three months revealed no perceptible changes in appearance or drug content. These findings support the effectiveness of BASD granules in enhancing furosemide dissolution and their potential for pediatric administration.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":"72 1","pages":"1-19"},"PeriodicalIF":0.0,"publicationDate":"2025-07-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pharmacia.pensoft.net/article/156784/download/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147332791","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Evaluation of therapeutic effectiveness of antituberculosis injection based on conversion time in drug-resistant tuberculosis","authors":"Emy Oktaviani, K. Anggadiredja, Lia Amalia","doi":"10.3897/pharmacia.71.e118795","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e118795","url":null,"abstract":"Drug-resistant tuberculosis is a condition in which Mycobacterium tuberculosis is resistant to first-line anti-tuberculosis drugs, namely isoniazid and rifampicin, which are the two most effective anti-tuberculosis agents. Conversion time is a parameter to assess whether the therapeutic effect of injection has been achieved by carrying out two acid-resistant bacilli (ARB) sputum examinations within a maximum period of 2 consecutive months. Kanamycin and capreomycin are injectable drugs that are used in the intensive phase. This cross-sectional study aimed to evaluate the therapeutic effect of injection using ARB sputum conversion time and to analyze other factors related to ARB sputum conversion time. The study used retrospective data from patients’ medical records, collected with purposive sampling technique. The results of the study showed that from 101 patients who met the inclusion criteria 57.4% used kanamycin and 42.6% received capreomycin. The therapeutic effect was achieved in 87.1%. There was no significant correlation between the type of injection therapy and therapeutic effectiveness (p-value = 0.983). In conclusion, therapy using injections for drug-resistant tuberculosis is effective but still requires close monitoring due to the high adverse drug reaction (ADR).","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":"61 9","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-07-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141806840","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Comparative quantitative profiling of rare justicidin B in in vitro cultivated Linum species","authors":"Rada Nedelcheva, Y. Zarev, I. Ionkova","doi":"10.3897/pharmacia.71.e131544","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e131544","url":null,"abstract":"This research investigates the production and optimization of justicidin B from L. austriacum and L. alpinum in vitro cultures, aiming for high yields of this pharmacologically significant arylnaphthalene lignan. Various cultivation techniques were employed, including shoot, root, and callus cultures, with different media formulations to induce justicidin B biosynthesis. In vitro shoots, callus, and root cultures of both Linum species were successfully established to enhance justicidin B production. Quantification of the lignan was performed using LC-HRESI-MS analysis, comparing the quantities to those of isolated and identified justicidin B from L. leonii hairy root extract. The results show that the in vitro root cultures of L. alpinum produced 1.3 times more justicidin B than those of L. austriacum (7.24 μg/mg DW and 5.31 μg/mg DW, respectively). Additionally, the shoot cultures of L. alpinum yielded 4.5 times more justicidin B than those of L. austriacum (4.34 μg/mg DW and 0.96 μg/mg DW, respectively).","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":"138 29","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-07-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141811024","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Effect of Camellia flava (Pitard) Sealy flower extract on the degeneration of Islets of Langerhans and insulin resistance in alloxan-induced hyperglycemia model on Swiss albino mice","authors":"Huu Lac Thuy Nguyen, Thi Thu Phuong Ha, Ngoc Phuc Nguyen, Nguyen Hoang Linh Phan, Dang Thuy Hien Nguyen, Van Dat Truong, Minh-Nhut Truong, Thao-My Nguyen-Hoang, Thi Nghia Luu, Ngoc Phuc Nguyen, Thanh Binh Nguyen, H. Mai","doi":"10.3897/pharmacia.71.e126255","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e126255","url":null,"abstract":"Diabetes has always been a matter of concern to health experts as well as the community due to the increasing number of patients with diabetes and the severe consequences it may cause. Many attempts have been made to discover new treatment options for diabetes, and herbal medicines are currently considered to have great potential. This study was conducted to evaluate the effect of Camellia flava flower extract on the degeneration of the islets of Langerhans and insulin resistance in an alloxan-induced hyperglycemia model in Swiss albino mice. Hyperglycemic conditions were induced by alloxan (55 mg/kg, i.v.). The animals were then treated with glibenclamide (10 mg/kg, p.o.) and flower extract at doses of 1.09 and 2.19 g/kg, p.o. The results showed that the blood glucose, AUC, HbA1c, and HOMA-IR levels of two groups of mice receiving flower extract were considerably lower than those of the hyperglycemic untreated group (p < 0.05). The body weights of these two groups were also lower than the untreated group on the last day of the experiment, though the differences were not significant (p > 0.05). However, this was not observed when assessing insulin levels as well as relative organ weights. In biochemical tests, creatinine and AST and ALT concentrations were evaluated. There was no significant variation in creatinine and AST concentrations between the five experimental groups, whereas mice treated with glibenclamide and flower extract at both doses showed a remarkable decline in ALT concentration (p < 0.05). The hepatic histomicrographs were consistent with ALT results, while the H&E staining of kidneys showed no difference between groups. Histomicrographs of the pancreas revealed that the treatment groups using glibenclamide and flower extract had larger islets of Langerhans than those of the alloxan-treated group. Based on these results, this study demonstrated that Camellia flava flower extract exerted several beneficial effects, including blood sugar level reduction, weight loss promotion, and organ protection, hence making it a new potential herbal medication for the management of diabetes.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":"64 5","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-07-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141810432","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Design and optimization of pantoprazole sodium mucoadhesive hydrogel microcapsules for the healing of peptic ulcers","authors":"Rashad M. Kaoud, Mustafa Hasan Alwan, Mohammed Amran, Hayder Adnan Fawzi","doi":"10.3897/pharmacia.71.e118323","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e118323","url":null,"abstract":"Hydrogels have gained much focus as a gastro-retentive technology for drug delivery. The current study aimed to design an oral mucoadhesive sustained-release dosage form to lower peptic ulcer complications (PUC). Using the Box-Behnken statistical design, the preparation method was developed by incorporating pantoprazole sodium (PZS) into hydrogel microcapsules (HGMC). The PZS was incorporated into the HGMC via an ion gelation technique, with sodium alginate as the gelling agent, calcium chloride as the crosslinking agent, and chitosan as the agent for sustained release.\u0000 The optimized formulation of PZS-HGMC showed a diameter of 2.506 mm, a swelling rate of 838.2%, and an encapsulation efficiency of 93.8%. Scanning electron microscopy images revealed the microcapsules’ spherical shape. The in vitro release of the PZS from the HGMC after two hours in a simulated gastric fluid was 13.2%1±0.08%, compared with the apparent solubility of the pure PZS under the same conditions (95.24%±3.2%). After 24 hours, the percent of PZS released from the optimized formula was 69.84±2.4%, which indicates a sustained release pattern. The results from the in vivo study demonstrated improved healing of the induced ulcers in rats when treated with the PZS-HGMC formulation as compared to the standard PZS therapy; therefore, the obtained mucoadhesive HGMC was considered a potential drug delivery strategy for PUC therapy.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":" 44","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-07-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141824114","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Development and evaluation of curcumin-loaded vesicular carriers: impact of formulation variables","authors":"D. Momekova, Viliana Gugleva, Petar Petrov","doi":"10.3897/pharmacia.71.e127997","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e127997","url":null,"abstract":"Vesicular carriers are a well-established approach to improving the technological and biopharmaceutical characteristics of the loaded cargo. The current manuscript is focused on the development and evaluation in a comparative aspect of two types of vesicles—ethosomes and transfersomes loaded with the phytoconstituent curcumin. The formulation variables affecting their physiochemical and cytotoxic properties are outlined as well. A series of ethosomes and transfersomes based on Lipoid S75 and ethanol, or edge activator, were prepared using the thin film hydration method and subjected to comprehensive evaluation by dynamic light scattering (DLS) analysis, transmission electron microscopy (TEM), entrapment efficiency evaluation, in vitro release, and cytotoxicity studies. Ethosomes based on Lipoid S75 (4% w/w) and ethanol (30% v/v) showed suitable physicochemical characteristics (hydrodynamic diameter of 578.6 nm, monomodal size distribution, high curcumin entrapment efficiency (78.2%)), and superior antiproliferative activity compared to free drug and transfersomal nanocarriers.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":"8 6","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-07-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141640722","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Molecular mechanism elucidation of Ocimum basilicum as anticancer using system bioinformatic approach supported by in vitro assay","authors":"Kurnia Agustini, Frangky Sangande, Nuralih Nuralih, Armansyah Maulana Harahap, Sri Ningsih, Anton Bahtiar","doi":"10.3897/pharmacia.71.e127395","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e127395","url":null,"abstract":"Breast cancer (BC) is a multifactorial disease involving many pathways and target molecules. Multi-target therapy through multi-compound herbal medicines is an alternative strategy to treat BC. In the present study, we elucidate the molecular mechanism of Ocimum basilicum (OB) as an anticancer agent using system bioinformatic approach and investigate its cytotoxic effect against MCF-7 cells. We performed network pharmacology (NP) and molecular docking studies to provide scientific information regarding the underlying anti-BC mechanism of OB. Based on topology parameters obtained from protein-protein interaction (PPI), we identified six potential targets that play a significant role in the network including SRC, PI3KCA, EGFR, ESR1, AKT1, and MAPK1. Furthermore, consensus docking suggested rutin, quercetin-3-O-diglucoside, and kaempferol-3-O-β-D-rutinoside as the potential compounds of OB. Moreover, Kyoto Encyclopedia of Genes and Genomes (KEGG) analysis demonstrated that the cytotoxic effect of OB might be related to the modulation of several pathways such as PI3K-Akt, VEGF, and HIF-1, breast cancer, and estrogen signaling pathways. The in vitro assay revealed that various extracts of OB demonstrated cytotoxic effects against MCF-7 with IC50 = 231 µg/mL (OB ethanolic extract), 408 µg/mL (OB methanolic extract), 479 µg/mL (OB ethyl acetate extract), 1887 µg/mL (OB n-hexanoic extract) and 767 µg/mL (OB butanolic extract) respectively.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":"27 5","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-07-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141646802","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}