Acta Pharmaceutica最新文献_第7页

Exploring adherence in patients with advanced breast cancer: focus on CDK4/6 inhibitors. 探索晚期乳腺癌患者的依从性：关注 CDK4/6 抑制剂。

IF 2.8 4区医学

Acta Pharmaceutica Pub Date : 2023-12-26 Print Date: 2023-12-01 DOI: 10.2478/acph-2023-0045

Matea Baković, Martina Bago, Lucija Benić, Magdalena Krajinović, Tajana Silovski, Natalija Dedić Plavetić, Lu Turković, Miranda Sertić, Maja Ortner Hadžiabdić

{"title":"Exploring adherence in patients with advanced breast cancer: focus on CDK4/6 inhibitors.","authors":"Matea Baković, Martina Bago, Lucija Benić, Magdalena Krajinović, Tajana Silovski, Natalija Dedić Plavetić, Lu Turković, Miranda Sertić, Maja Ortner Hadžiabdić","doi":"10.2478/acph-2023-0045","DOIUrl":"10.2478/acph-2023-0045","url":null,"abstract":"Treatment adherence is crucial for optimal outcomes in advanced breast cancer, but can be challenging due to various factors, i.e. patients' attitudes and behavior upon diagnosis, and complex therapies with high adverse effect rates. Our aim was to explore the adherence to oral anticancer medications (OAM) in women with advanced breast cancer, focusing on cyclin-dependent kinase 4 and 6 inhibitors (CDKI), and identify factors associated with the adherence. We conducted a cross-sectional study at the University Hospital Centre Zagreb, Croatia, involving women with stage IV advanced breast cancer receiving OAM. Data collection included a questionnaire assessing socio-demographic and clinical information, Beck Depression Inventory-II for depressive symptoms, Medication Adherence Report Scale (MARS-5) for adherence to OAM, and Beliefs about Medicines Questionnaire. Plasma concentrations of CDKI were confirmed by LC-MS/MS in three randomly selected participants. A total of 89 women were included. The most prescribed OAMs were anti-estrogen (71.3 %) and CDKI (60.9 %). MARS-5 scores (mean: 24.1 ± 1.6) correlated with CDKI plasma concentrations. Forgetfulness was the primary reason for non-adherence (25.9 %). Women receiving CDKI (p = 0.018), without depressive symptomatology (p = 0.043), and with more positive beliefs about medicines were more adherent (p < 0.05). This study enhances understanding of medication adherence in advanced breast cancer and identifies influential factors.","PeriodicalId":7034,"journal":{"name":"Acta Pharmaceutica","volume":"73 4","pages":"633-654"},"PeriodicalIF":2.8,"publicationDate":"2023-12-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139039338","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

Preparation of astaxanthin/zeaxanthin-loaded nanostructured lipid carriers for enhanced bioavailability: Characterization-, stability-and permeability study. 制备虾青素/玉米黄质纳米结构脂质载体以提高生物利用度：特性、稳定性和渗透性研究。

IF 2.8 4区医学

Acta Pharmaceutica Pub Date : 2023-12-26 Print Date: 2023-12-01 DOI: 10.2478/acph-2023-0038

Kristina Radić, Ana Isabel Barbosa, Salette Reis, Marijan Marijan, Sofia Antunes Costa Lima, Dubravka Vitali Čepo

{"title":"Preparation of astaxanthin/zeaxanthin-loaded nanostructured lipid carriers for enhanced bioavailability: Characterization-, stability-and permeability study.","authors":"Kristina Radić, Ana Isabel Barbosa, Salette Reis, Marijan Marijan, Sofia Antunes Costa Lima, Dubravka Vitali Čepo","doi":"10.2478/acph-2023-0038","DOIUrl":"10.2478/acph-2023-0038","url":null,"abstract":"Astaxanthin (ASTA) and zeaxanthin (ZEA) are xanthophyll carotenoids showing a wide spectrum of health-promoting properties. However, their utilization is limited, mostly due to poor water solubility, limited bioavailability, and a tendency to oxidate, as well as photo- and thermal instability. The aim of this work was to develop ASTA- and ZEA-loaded nano-structured lipid carriers (NLCs) that would protect them against degradation and improve their intestinal stability/permeability. Obtained NLCs were characterized by an effective diameter of 294 nm for ASTA-NLC and 280 nm for ZEA-NLC; polydispersity index (PDI) lower than 0.2; and zeta potential of -29.4 mV and -29.0 mV, respectively. Interestingly, despite similar physicochemical characteristics, our investigation revealed differences in the encapsulation efficiency of ASTA-NLC and ZEA-NLC (58.0 % vs. 75.5 %, respectively). Obtained NLCs were stable during a 21 day-storage period in the dark at room temperature or at 4 °C. Investigation of gastrointestinal stability showed no change in effective diameter and PDI under gastric conditions while both parameters significantly changed under intestinal conditions. Our results showed for the first time that both ASTA- and ZEA-NLCs intestinal absorption investigated in the in vitro model is significantly increased (in relation to pure compounds) and is affected by the presence of mucus. This study provides useful data about the advantages of using NLC as a delivery system for ASTA and ZEA that might facilitate their applications in the food and pharmaceutical industry.","PeriodicalId":7034,"journal":{"name":"Acta Pharmaceutica","volume":"73 4","pages":"581-599"},"PeriodicalIF":2.8,"publicationDate":"2023-12-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139039342","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

Prescribers' approval rate of pharmacist-initiated interventions to optimise patients' clinical status of hypertension in the ambulatory care setting. 处方者对药剂师发起的干预措施的认可率，以优化门诊护理环境中患者的高血压临床状态。

IF 2.8 4区医学

Acta Pharmaceutica Pub Date : 2023-12-26 Print Date: 2023-12-01 DOI: 10.2478/acph-2023-0047

Andrea Brajković, Lucija Ana Bićanić, Helena Orehovački, Ingrid Prkačin, Djenane Ramalho De Oliveira, Iva Mucalo

{"title":"Prescribers' approval rate of pharmacist-initiated interventions to optimise patients' clinical status of hypertension in the ambulatory care setting.","authors":"Andrea Brajković, Lucija Ana Bićanić, Helena Orehovački, Ingrid Prkačin, Djenane Ramalho De Oliveira, Iva Mucalo","doi":"10.2478/acph-2023-0047","DOIUrl":"10.2478/acph-2023-0047","url":null,"abstract":"This perspective, pre- and post-intervention study with a one-year follow-up primarily aimed to ascertain prescribers' approval rate of pharmacists' interventions and clinical status of hypertension following comprehensive medication management (CMM) intervention in the ambulatory care clinic. Between January 2018 and January 2022 overall 100 patients with hypertension and other comorbidities were referred to the CMM services at the Health Centre Zagreb - Centar (HCZC). Out of 275 interventions directed to prescribers, 73.1 % of interventions were approved, 12.4 % were rejected and 14.5 % were not reviewed. The percentage of patients with a blood pressure goal increased from 45 % at the initial consultation to 82.5 % at the patients' latest encounter (p < 0.001). The average number of drug therapy problems (DTPs) per patient totaled 3.53 ± 1.80, where 98 % of patients had one or more DTPs, 48 % had 4 or more DTPs, whereas 26 % had 5 or more DTPs. Sub-therapeutic dosage (32.6 %) and the need for additional drug therapy (30.9 %) were the two most commonly identified DTPs. These results reinforce the need to integrate pharmacy-led services in the primary care setting with the aim of improving patients' health outcomes.","PeriodicalId":7034,"journal":{"name":"Acta Pharmaceutica","volume":"73 4","pages":"723-734"},"PeriodicalIF":2.8,"publicationDate":"2023-12-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139039343","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

Simultaneous determination of macrolides in water samples by solid-phase extraction and capillary electrophoresis. 利用固相萃取和毛细管电泳同时测定水样中的大环内酯类化合物。

IF 2.8 4区医学

Acta Pharmaceutica Pub Date : 2023-12-26 Print Date: 2023-12-01 DOI: 10.2478/acph-2023-0041

Dragana Mutavdžić Pavlović, Sandra Babić, Mirta Čizmić, Miranda Sertić, Tea Pinušić

{"title":"Simultaneous determination of macrolides in water samples by solid-phase extraction and capillary electrophoresis.","authors":"Dragana Mutavdžić Pavlović, Sandra Babić, Mirta Čizmić, Miranda Sertić, Tea Pinušić","doi":"10.2478/acph-2023-0041","DOIUrl":"10.2478/acph-2023-0041","url":null,"abstract":"Solid-phase extraction (SPE) coupled with capillary electrophoresis (CE) for the determination of macrolide antibiotics (azithromycin, clarithromycin, roxithromycin, tylosin) and tiamulin in water samples was described in this article. These compounds were extracted with different types of sorbents ( Oasis HLB, C18, C8, SDB, and Strata-X) and different masses of sorbents (60 mg, 200 mg, and 500 mg) using different organic solvents (methanol, ethanol, and acetonitrile) and different pH values of water samples (pH 7.00, 8.00, and 9.00). It was found that the highest extraction efficiency of the studied compounds was obtained with 200 mg/3 mL C18 cartridges with methanol as eluent at pH 9.00 of the water sample. The developed SPE-CE method for macrolide antibiotics and tiamulin was validated for linearity, precision, repeatability, the limit of detection (LOD), the limit of quantification (LOQ), and recovery. Good linearity was obtained in the range of 0.3-30 mg L-1 depending on the drug, with correlation coefficients higher than 0.9958 in all cases except clarithromycin (0.9873). Expanded measurement uncertainties were calculated for each pharmaceutical, accounting for 20.31 % (azithromycin), 38.33 % (tiamulin), 28.95 % (clarithromycin), 26.99 % (roxithromycin), and 21.09 % (tiamulin). Uncertainties associated with precision and calibration curves contributed the most to the combined measurement uncertainty. The method was successfully applied to the analysis of production waste-water from the pharmaceutical industry.","PeriodicalId":7034,"journal":{"name":"Acta Pharmaceutica","volume":"73 4","pages":"515-535"},"PeriodicalIF":2.8,"publicationDate":"2023-12-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139039344","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

Xanthoxyletin blocks the RANK/RANKL signaling pathway to suppress the growth of human pancreatic cancer cells. 黄酮素能阻断 RANK/RANKL 信号通路，从而抑制人类胰腺癌细胞的生长。

IF 2.8 4区医学

Acta Pharmaceutica Pub Date : 2023-09-14 Print Date: 2023-09-01 DOI: 10.2478/acph-2023-0024

Xin Zhang, Luming Li, Yan Wu

{"title":"Xanthoxyletin blocks the RANK/RANKL signaling pathway to suppress the growth of human pancreatic cancer cells.","authors":"Xin Zhang, Luming Li, Yan Wu","doi":"10.2478/acph-2023-0024","DOIUrl":"10.2478/acph-2023-0024","url":null,"abstract":"Xanthoxyletin is a vital plant-derived bioactive coumarin. It has been shown to exhibit anticancer effects against different human cancers. Nonetheless, the anticancer effects of xanthoxyletin against human pancreatic cancer cells have not been evaluated. Against this backdrop, the present study was designed to evaluate the anticancer effects of xanthoxyletin in human pancreatic cancer cells and to decipher the underlying molecular mechanisms. The results revealed a significant (p < 0.05) upregulation of receptor activator of NF-kappaB (RANK), receptor activator of NF-kappaB ligand (RANKL) and osteoprotegerin (OPG) in human pancreatic tissues and cell lines at both transcriptional and translational levels. The administration of pancreatic cancer cells with xanthoxyletin diminished the viability of Capan-2 cells in a concentration-dependent manner and led to a significant decline in RANK, RANKL, and OPG expression. Silencing of RANK and xanthoxyletin treatment declined the viability of Capan-2 pancreatic cancer cells via induction of apoptosis. However, pancreatic cancer cells overexpressing RANK could rescue the growth inhibitory effects. Collectively, xanthoxyletin targets the RANK/RANKL signaling pathway in pancreatic cancer cells to induce cell apoptosis and may prove to be an important lead molecule.","PeriodicalId":7034,"journal":{"name":"Acta Pharmaceutica","volume":"73 3","pages":"503-513"},"PeriodicalIF":2.8,"publicationDate":"2023-09-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10287720","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

Formulation and optimization of polymeric nanoparticles loaded with riolozatrione: a promising nanoformulation with potential antiherpetic activity. 利奥扎特里酮聚合物纳米颗粒的配方和优化:一种具有潜在抗疱疹活性的纳米制剂。

IF 2.8 4区医学

Acta Pharmaceutica Pub Date : 2023-09-01 DOI: 10.2478/acph-2023-0028

Guadalupe Y Solís-Cruz, Rocío Alvarez-Roman, Verónica M Rivas-Galindo, Sergio Arturo Galindo-Rodríguez, David A Silva-Mares, Iván A Marino-Martínez, Magdalena Escobar-Saucedo, Luis A Pérez-López

{"title":"Formulation and optimization of polymeric nanoparticles loaded with riolozatrione: a promising nanoformulation with potential antiherpetic activity.","authors":"Guadalupe Y Solís-Cruz, Rocío Alvarez-Roman, Verónica M Rivas-Galindo, Sergio Arturo Galindo-Rodríguez, David A Silva-Mares, Iván A Marino-Martínez, Magdalena Escobar-Saucedo, Luis A Pérez-López","doi":"10.2478/acph-2023-0028","DOIUrl":"https://doi.org/10.2478/acph-2023-0028","url":null,"abstract":"Riolozatrione (RZ) is a diterpenoid compound isolated from a dichloromethane extract of the Jatropha dioica root. This compound has been shown to possess moderate antiherpetic activity in vitro. However, because of the poor solubility of this compound in aqueous vehicles, generating a stable formulation for potential use in the treatment of infection is challenging. The aim of this work was to optimize and physio-chemically characterize Eudragit® L100-55-based polymeric nanoparticles (NPs) loaded with RZ (NPR) for in vitro antiherpetic application. The NPs formulation was initially optimized using the dichloromethane extract of J. dioica, the major component of which was RZ. The optimized NPR formulation was stable, with a size of 263 nm, polydispersity index < 0.2, the zeta potential of -37 mV, and RZ encapsulation efficiency of 89 %. The NPR showed sustained release of RZ for 48 h with release percentages of 95 and 97 % at neutral and slightly acidic pH, respectively. Regarding in vitro antiherpetic activity, the optimized NPR showed a selectivity index for HSV-1 of ≈16 and for HSV-2 of 13.","PeriodicalId":7034,"journal":{"name":"Acta Pharmaceutica","volume":"73 3","pages":"457-473"},"PeriodicalIF":2.8,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10283477","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

Astragaloside IV inhibits pathological functions of gastric cancer-associated fibroblasts through regulation of the HOXA6/ZBTB12 axis. 黄芪甲苷通过调控HOXA6/ZBTB12轴抑制胃癌相关成纤维细胞的病理功能。

IF 2.8 4区医学

Acta Pharmaceutica Pub Date : 2023-09-01 DOI: 10.2478/acph-2023-0033

Haibo Liu, Shicheng Luo, Xiaofeng Sha, Zhiping Chen, Dongdong Yang

{"title":"Astragaloside IV inhibits pathological functions of gastric cancer-associated fibroblasts through regulation of the HOXA6/ZBTB12 axis.","authors":"Haibo Liu, Shicheng Luo, Xiaofeng Sha, Zhiping Chen, Dongdong Yang","doi":"10.2478/acph-2023-0033","DOIUrl":"https://doi.org/10.2478/acph-2023-0033","url":null,"abstract":"Cancer-associated fibroblasts (CAFs) play critical roles in the tumor microenvironment and exert tumor-promoting or tumor-retarding effects on cancer development. Astragaloside IV has been suggested to rescue the pathological impact of CAFs in gastric cancer. This study aimed to investigate the potential mechanism of astragaloside IV in the regulation of CAF pathological functions in gastric cancer development. Homeobox A6 (HOXA6), and Zinc Finger and BTB Domain Containing 12 (ZBTB12) are highly expressed in gastric CAFs compared with normal fibroblasts (NFs) based on the GSE62740 dataset. We found that astragaloside IV-stimulated CAFs suppressed cell growth, migration, and invasiveness of gastric cancer cells. HOXA6 and ZBTB12 were downregulated after astragaloside IV treatment in CAFs. Further analysis revealed that HOXA6 or ZBTB12 knockdown in CAFs also exerted inhibitory effects on the malignant phenotypes of gastric cells. Additionally, HOXA6 or ZBTB12 overexpression in CAFs enhanced gastric cancer cell malignancy, which was reversed after astragaloside IV treatment. Moreover, based on the hTFtarget database, ZBTB12 is a target gene that may be transcriptionally regulated by HOXA6. The binding between HOXA6 and ZBTB12 promoter in 293T cells and CAFs was further confirmed. HOXA6 silencing also induced the downregulation of ZBTB12 mRNA and protein in CAFs. Astragaloside IV was demonstrated to regulate the expression of ZBTB12 by mediating the transcriptional activity of HOXA6. Our findings shed light on the therapeutic value of astragaloside IV for gastric cancer.","PeriodicalId":7034,"journal":{"name":"Acta Pharmaceutica","volume":"73 3","pages":"423-439"},"PeriodicalIF":2.8,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10283478","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: 2

Is epinephrine still the drug of choice during cardiac arrest in the emergency department of the hospital? A meta-analysis. 在医院的急诊科，肾上腺素仍然是心脏骤停时的首选药物吗?一个荟萃分析。

IF 2.8 4区医学

Acta Pharmaceutica Pub Date : 2023-09-01 DOI: 10.2478/acph-2023-0022

Min Hou, Su Dong, Qing Kan, Meng Ouyang, Yun Zhang

{"title":"Is epinephrine still the drug of choice during cardiac arrest in the emergency department of the hospital? A meta-analysis.","authors":"Min Hou, Su Dong, Qing Kan, Meng Ouyang, Yun Zhang","doi":"10.2478/acph-2023-0022","DOIUrl":"https://doi.org/10.2478/acph-2023-0022","url":null,"abstract":"Epinephrine is the first-line emergency drug for cardiac arrest and anaphylactic reactions but is reported to be associated with many challenges resulting in its under- or improper utilization. Therefore, in this meta-analysis, the efficacy and safety of epinephrine as a first-line cardiac emergency drug for both out-of-hospital and in-hospital patients was assessed. Pertinent articles were searched in central databases like PubMed, Scopus, and Web of Science, using appropriate keywords as per the PRISMA guidelines. Retrospective and prospective studies were included according to the predefined PICOS criteria. RevMan and MedCalc software were used and statistical parameters such as odds ratio and risk ratio were calculated. Twelve clinical trials with a total of 208,690 cardiac arrest patients from 2000 to 2022 were included, in accordance with the chosen inclusion criteria. In the present meta-analysis, a high odds ratio (OR) value of 3.67 (95 % CI 2.32-5.81) with a tau2 value of 0.64, a chi2 value of 12,446.86, df value of 11, I2 value of 100 %, Z-value 5.53, and a p-value < 0.00001 were reported. Similarly, the risk ratio of 1.89 (95 % CI 1.47-2.43) with a tau2 value of 0.19, chi2 value of 11,530.67, df value of 11, I2 value of 100 %, Z-value of 4.95, and p-value < 0.000001. The present meta-analysis strongly prefers epinephrine injection as the first cardiac emergency drug for both out-of-hospital and in-hospital patients during cardiac arrest.","PeriodicalId":7034,"journal":{"name":"Acta Pharmaceutica","volume":"73 3","pages":"325-339"},"PeriodicalIF":2.8,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10287719","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

Insights into the formulation properties, biocompatibility, and permeability of poorly water-soluble methoxyflavones with PEG400 and propylene glycol. 低水溶性甲氧基黄酮与PEG400和丙二醇的配方特性、生物相容性和渗透性的深入研究。

IF 2.8 4区医学

Acta Pharmaceutica Pub Date : 2023-09-01 DOI: 10.2478/acph-2023-0030

Fredrick Nwude Eze, Chaweewan Jansakul, Teerapol Srichana

{"title":"Insights into the formulation properties, biocompatibility, and permeability of poorly water-soluble methoxyflavones with PEG400 and propylene glycol.","authors":"Fredrick Nwude Eze, Chaweewan Jansakul, Teerapol Srichana","doi":"10.2478/acph-2023-0030","DOIUrl":"https://doi.org/10.2478/acph-2023-0030","url":null,"abstract":"Herein, thermal and non-thermal techniques were used to elucidate the putative physical and chemical interactions between poorly water-soluble Kaempferia methoxyflavones and PEG400/propylene glycol. Additionally, the biocompatibility of methoxyflavone-glycol solutions was evaluated using Caco-2 cells whereas the absorptive transport was investigated by measuring the apparent permeability coefficient (P app) of the methoxyflavones and transepithelial electrical resistance (TEER) of the Caco-2 cell monolayer. Data from differential scanning calorimetry, Fourier-transform infrared (FTIR), and proton nuclear magnetic resonance (1H NMR) spectroscopic analysis revealed physico-chemical compatibility between the three methoxyflavones and PEG400/propylene glycol. Furthermore, PEG400 and propylene glycol solutions of the methoxyflavones were shown to be compatible with Caco-2 cells at pharmacologically effective concentrations. In vitro transport studies across the Caco-2 cell monolayer revealed high P app values of 24.07 × 10-6 to 19.63 × 10-6 cm s-1 for PEG400 solutions of the methoxyflavones. The TEER values of the Caco-2 cell monolayers indicated that the increased drug transport was partly due to increased tight junction openings, but without compromising the epithelial barrier integrity. The good pharmaceutical and biocompatibility profiles, as well as improved transport of the methoxyflavones in PEG400 and propylene glycol solutions, are suggestive of the worthiness of this approach for further consideration pertaining to the development of these drugs into oral liquid dosage forms.","PeriodicalId":7034,"journal":{"name":"Acta Pharmaceutica","volume":"73 3","pages":"385-404"},"PeriodicalIF":2.8,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10287722","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

Rosuvastatin effects on the HDL proteome in hyperlipidemic patients. 瑞舒伐他汀对高脂血症患者HDL蛋白组的影响。

IF 2.8 4区医学

Acta Pharmaceutica Pub Date : 2023-09-01 DOI: 10.2478/acph-2023-0034

Ana Vavlukis, Kristina Mladenovska, Katarina Davalieva, Marija Vavlukis, Aleksandar Dimovski

{"title":"Rosuvastatin effects on the HDL proteome in hyperlipidemic patients.","authors":"Ana Vavlukis, Kristina Mladenovska, Katarina Davalieva, Marija Vavlukis, Aleksandar Dimovski","doi":"10.2478/acph-2023-0034","DOIUrl":"https://doi.org/10.2478/acph-2023-0034","url":null,"abstract":"The advancements in proteomics have provided a better understanding of the functionality of apolipoproteins and lipoprotein-associated proteins, with the HDL lipoprotein fraction being the most studied. The focus of this study was to evaluate the HDL proteome in dyslipidemic subjects without an established cardiovascular disease, as well as to test whether rosuvastatin treatment alters the HDL proteome. Patients with primary hypercholesterolemia or mixed dyslipidemia were assigned to 20 mg/day rosuvastatin and blood samples were drawn at study entry and after 12 weeks of treatment. A label-free LC-MS/MS protein profiling was conducted, coupled with bioinformatics analysis. Sixty-nine HDL proteins were identified, belonging to four main biological function clusters: lipid transport and metabolism; platelet activation, degranulation, and aggregation, wound response and wound healing; immune response; inflammatory and acute phase response. Five HDL proteins showed statistically significant differences in the abundance (Anova ≤ 0.05), before and after rosuvastatin treatment. Platelet factor 4 variant (PF4V1), Pregnancy-specific beta-1-glycoprotein 2 (PSG2), Profilin-1 (PFN1) and Keratin type II cytoskeletal 2 epidermal (KRT2) showed decreased expressions, while Integrin alpha-IIb (ITGA2B) showed an increased expression after treatment with rosuvastatin. The ELISA validation of PFN1 segregated the subjects into responders and non-responders, as PFN1 levels after rosuvastatin were shown to mostly depend on the subjects' inflammatory phenotype. Findings from this study introduce novel insights into the HDL proteome and statin pleiotropism.","PeriodicalId":7034,"journal":{"name":"Acta Pharmaceutica","volume":"73 3","pages":"363-384"},"PeriodicalIF":2.8,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10276850","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