Pharmacia最新文献_第8页

Evaluation of types and concentration of bile salts impact on physical properties of nisoldipine-loaded bilosomes 评估胆盐类型和浓度对尼索地平双糖体物理性质的影响

Pharmacia Pub Date : 2024-02-09 DOI: 10.3897/pharmacia.71.e116917

Ghada Hamid Naji, F. J. Al Gawhari

{"title":"Evaluation of types and concentration of bile salts impact on physical properties of nisoldipine-loaded bilosomes","authors":"Ghada Hamid Naji, F. J. Al Gawhari","doi":"10.3897/pharmacia.71.e116917","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e116917","url":null,"abstract":"Background: Bilosomes are lipid vesicles that exhibit flexibility and deformability. They consist of phospholipids and amphiphilic bile salts. Compared to the normal vesicular systems such as liposomes and niosomes, bilosomes provide several notable advantages, including simplified manufacturing, cost-effectiveness, and enhanced stability.\u0000 Aim: The main objective of the present work was to evaluate the effect of different bile salts on the physical properties that include entrapment efficiency, vesicle size, and polydispersity index(PDI). In addition, in vitro drug release for nisoldipine (NSD) loaded bilosomes was evaluated.\u0000 Methods: Nisoldipine-loaded bilosomes were made using a thin film hydration technique. Cholesterol along with surfactant (span 60) was employed, and the formulation also contained several different bile salts, including sodium deoxycholate (SDC), sodium glycocholate (SGC), and sodium taurocholate (STC).\u0000 Results: The developed NSD bilosomes exhibited an entrapment efficiency ranging from 44.2 ± 0.3 to 82.36 ± 0.80% and a vesicle size diameter in the nanometric dimensions (166 ± 1.83 to 237.8 ± 3.3 nm). An in-vitro release study revealed that formulas prepared with SDC bile salts showed higher drug release than SGC and STC formulas.\u0000 Increasing the bile salt amount from 5 mg to 10 mg increases entrapment efficiency with increasing vesicle size. Further increase in bile salt led to decreased entrapment efficiency with increased vesicle size. SDC gives the best result in terms of entrapment efficiency and acceptable size. STC provides the largest particle size due to its high molecular weight compared to SGC and SDC.\u0000 Conclusion: The SDC bile salt component is better suited for manufacturing NSD bilosomes. This is because this component yields the best results regarding high entrapment efficiency, nano size, and prolonged drug release.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":"213 4","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139848830","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}

引用次数: 0

Evaluation of types and concentration of bile salts impact on physical properties of nisoldipine-loaded bilosomes 评估胆盐类型和浓度对尼索地平双糖体物理性质的影响

Pharmacia Pub Date : 2024-02-09 DOI: 10.3897/pharmacia.71.e116917

Ghada Hamid Naji, F. J. Al Gawhari

{"title":"Evaluation of types and concentration of bile salts impact on physical properties of nisoldipine-loaded bilosomes","authors":"Ghada Hamid Naji, F. J. Al Gawhari","doi":"10.3897/pharmacia.71.e116917","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e116917","url":null,"abstract":"Background: Bilosomes are lipid vesicles that exhibit flexibility and deformability. They consist of phospholipids and amphiphilic bile salts. Compared to the normal vesicular systems such as liposomes and niosomes, bilosomes provide several notable advantages, including simplified manufacturing, cost-effectiveness, and enhanced stability.\u0000 Aim: The main objective of the present work was to evaluate the effect of different bile salts on the physical properties that include entrapment efficiency, vesicle size, and polydispersity index(PDI). In addition, in vitro drug release for nisoldipine (NSD) loaded bilosomes was evaluated.\u0000 Methods: Nisoldipine-loaded bilosomes were made using a thin film hydration technique. Cholesterol along with surfactant (span 60) was employed, and the formulation also contained several different bile salts, including sodium deoxycholate (SDC), sodium glycocholate (SGC), and sodium taurocholate (STC).\u0000 Results: The developed NSD bilosomes exhibited an entrapment efficiency ranging from 44.2 ± 0.3 to 82.36 ± 0.80% and a vesicle size diameter in the nanometric dimensions (166 ± 1.83 to 237.8 ± 3.3 nm). An in-vitro release study revealed that formulas prepared with SDC bile salts showed higher drug release than SGC and STC formulas.\u0000 Increasing the bile salt amount from 5 mg to 10 mg increases entrapment efficiency with increasing vesicle size. Further increase in bile salt led to decreased entrapment efficiency with increased vesicle size. SDC gives the best result in terms of entrapment efficiency and acceptable size. STC provides the largest particle size due to its high molecular weight compared to SGC and SDC.\u0000 Conclusion: The SDC bile salt component is better suited for manufacturing NSD bilosomes. This is because this component yields the best results regarding high entrapment efficiency, nano size, and prolonged drug release.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":" 21","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139788969","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}

引用次数: 0

Potent antioxidant activity of black grass jelly (Mesona palustris BL) leaf extract and fractions 黑草冻（Mesona palustris BL）叶提取物和馏分的强抗氧化活性

Pharmacia Pub Date : 2024-02-08 DOI: 10.3897/pharmacia.71.e117435

Dytha Andri Deswati, K. Anggadiredja, Afrillia Nuryanti Garmana

引用次数: 0

Cost-effectiveness of cardiomyopathy ambulatory care with sacubitril/valsartan vs standard therapy after COVID-19 in Kazakhstan 在哈萨克斯坦，COVID-19 后使用沙库比特利/缬沙坦与标准疗法进行心肌病日间护理的成本效益对比

Pharmacia Pub Date : 2024-02-08 DOI: 10.3897/pharmacia.71.e115952

Dana Dadanbekova, K. Zhakipbekov, Almat T Kodasbayev, U. Datkhayev, G. Petrova, K. Tachkov

{"title":"Cost-effectiveness of cardiomyopathy ambulatory care with sacubitril/valsartan vs standard therapy after COVID-19 in Kazakhstan","authors":"Dana Dadanbekova, K. Zhakipbekov, Almat T Kodasbayev, U. Datkhayev, G. Petrova, K. Tachkov","doi":"10.3897/pharmacia.71.e115952","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e115952","url":null,"abstract":"The aim of this study is to evaluate the cost-effectiveness of 2 different therapies of cardiomyopathy (CM) after COVID -19. The focus of the study is fixed dose combination (FDC) of sacubitril/valsartan and standard therapy in Kazakhstan. This is written from the point of view of the health insurance institution.\u0000 Information for the age, gender, CM therapy, number of hospitalizations, COVID-19 infection, and past cardiovascular surgeries of 237 patients with incidents of CM which required a hospitalization after a COVID-19 infection was collected. Selected patients were divided into two groups: the cost of FDC and standard therapy and the annual cost of their therapy was calculated. The incremental cost-effectiveness ratio was calculated by dividing the cost of medication therapy by the number of hospitalizations between the two compared groups. Robustness of the results was tested with deterministic and probabilistic sensitivity analyses. The study was performed in City cardiology centre of Almaty in Kazakhstan during 2020–2022.\u0000 Results show that FDC is more costly but more effective, leading to fewer hospitalizations. ICER accounts for €-2,743.08 per hospitalization saved in the group on FDC vs standard of therapy.\u0000 Sacubitril/valsartan is cost-effective in ambulatory conditions in comparison with standard therapy of cardiomyopathy after COVID-19 leading to savings due to the decrease in the number of hospitalizations.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":" 2","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139791276","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}

引用次数: 0

Potent antioxidant activity of black grass jelly (Mesona palustris BL) leaf extract and fractions 黑草冻（Mesona palustris BL）叶提取物和馏分的强抗氧化活性

Pharmacia Pub Date : 2024-02-08 DOI: 10.3897/pharmacia.71.e117435

Dytha Andri Deswati, K. Anggadiredja, Afrillia Nuryanti Garmana

引用次数: 0

Assessment of anxiety and depression among professional healthcare workers during the COVID-19 pandemic – observational cross-sectional study 评估 COVID-19 大流行期间专业医护人员的焦虑和抑郁情况--观察性横断面研究

Pharmacia Pub Date : 2024-02-08 DOI: 10.3897/pharmacia.71.e115198

Mohammed Mahmood Mohammed, Hayder Adnan Fawzi

引用次数: 0

Assessment of anxiety and depression among professional healthcare workers during the COVID-19 pandemic – observational cross-sectional study 评估 COVID-19 大流行期间专业医护人员的焦虑和抑郁情况--观察性横断面研究

Pharmacia Pub Date : 2024-02-08 DOI: 10.3897/pharmacia.71.e115198

Mohammed Mahmood Mohammed, Hayder Adnan Fawzi

引用次数: 0

Cost-effectiveness of cardiomyopathy ambulatory care with sacubitril/valsartan vs standard therapy after COVID-19 in Kazakhstan 在哈萨克斯坦，COVID-19 后使用沙库比特利/缬沙坦与标准疗法进行心肌病日间护理的成本效益对比

Pharmacia Pub Date : 2024-02-08 DOI: 10.3897/pharmacia.71.e115952

Dana Dadanbekova, K. Zhakipbekov, Almat T Kodasbayev, U. Datkhayev, G. Petrova, K. Tachkov

{"title":"Cost-effectiveness of cardiomyopathy ambulatory care with sacubitril/valsartan vs standard therapy after COVID-19 in Kazakhstan","authors":"Dana Dadanbekova, K. Zhakipbekov, Almat T Kodasbayev, U. Datkhayev, G. Petrova, K. Tachkov","doi":"10.3897/pharmacia.71.e115952","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e115952","url":null,"abstract":"The aim of this study is to evaluate the cost-effectiveness of 2 different therapies of cardiomyopathy (CM) after COVID -19. The focus of the study is fixed dose combination (FDC) of sacubitril/valsartan and standard therapy in Kazakhstan. This is written from the point of view of the health insurance institution.\u0000 Information for the age, gender, CM therapy, number of hospitalizations, COVID-19 infection, and past cardiovascular surgeries of 237 patients with incidents of CM which required a hospitalization after a COVID-19 infection was collected. Selected patients were divided into two groups: the cost of FDC and standard therapy and the annual cost of their therapy was calculated. The incremental cost-effectiveness ratio was calculated by dividing the cost of medication therapy by the number of hospitalizations between the two compared groups. Robustness of the results was tested with deterministic and probabilistic sensitivity analyses. The study was performed in City cardiology centre of Almaty in Kazakhstan during 2020–2022.\u0000 Results show that FDC is more costly but more effective, leading to fewer hospitalizations. ICER accounts for €-2,743.08 per hospitalization saved in the group on FDC vs standard of therapy.\u0000 Sacubitril/valsartan is cost-effective in ambulatory conditions in comparison with standard therapy of cardiomyopathy after COVID-19 leading to savings due to the decrease in the number of hospitalizations.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":"123 7","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139851120","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}

引用次数: 0

In silico and in vitro screening of pyrrole-based Hydrazide-Hydrazones as novel acetylcholinesterase inhibitors 作为新型乙酰胆碱酯酶抑制剂的吡咯基肼基肼酮的硅学和体外筛选

Pharmacia Pub Date : 2024-02-05 DOI: 10.3897/pharmacia.71.e114120

E. Mateev, Ali Irfan, Alexandrina Mateeva, M. Kondeva-Burdina, Maya Georgieva, A. Zlatkov

{"title":"In silico and in vitro screening of pyrrole-based Hydrazide-Hydrazones as novel acetylcholinesterase inhibitors","authors":"E. Mateev, Ali Irfan, Alexandrina Mateeva, M. Kondeva-Burdina, Maya Georgieva, A. Zlatkov","doi":"10.3897/pharmacia.71.e114120","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e114120","url":null,"abstract":"Virtual screening is emerging as a highly applied technique and gained prominence as widely used method for the search and identification of potential hits, significantly reducing the time needed to discover novel and effective compounds compared to high-throughput screening. Recently, the superiority of simulations with multiple programs compared to a single software docking has been discussed. The aim of this work was to apply consensus docking, molecular mechanics/generalized Born surface area (MM/GBSA) free binding energy recalculations, and in vitro evaluations on an in-house dataset of recently synthesized pyrrole-based hydrazide-hydrazones in the search for novel acetylcholinesterase (AChE) inhibitors. Two licensed softwares – GOLD 5.3 and Glide, were employed for the virtual screenings, and several chemotherapeutic potential hits were identified. Furthermore, MM/GBSA free binding energy recalculations were provided to enhance the robustness of the in silico results. The MM/GBSA scores of the top ten pyrrole-based hydrazide-hydrazones were ranging from -60.44 to -70.93 Kcal/mol. Subsequent, in vitro evaluations of the top ranked compounds revealed that 12d exhibited the highest AChE inhibitory activity, with a 55% inhibition rate at a concentration of 10 μM. Moreover, this prominent pyrrole-based AChE inhibitor formed stable complex with the active site of the enzyme. Interactions with the active amino residues Tyr72 and Tyr286 indicated that 12d was located near the peripheral anionic site of the enzyme. Additionally, in silicoADME investigations using QikProp demonstrated that 12d possesses optimal pharmacokinetic properties. In conclusion, this study identified a novel pyrrole-based AChE inhibitor 12d through a combination of computational and experimental findings.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":"34 3","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139803196","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}

引用次数: 0

In silico and in vitro screening of pyrrole-based Hydrazide-Hydrazones as novel acetylcholinesterase inhibitors 作为新型乙酰胆碱酯酶抑制剂的吡咯基肼基肼酮的硅学和体外筛选

Pharmacia Pub Date : 2024-02-05 DOI: 10.3897/pharmacia.71.e114120

E. Mateev, Ali Irfan, Alexandrina Mateeva, M. Kondeva-Burdina, Maya Georgieva, A. Zlatkov

{"title":"In silico and in vitro screening of pyrrole-based Hydrazide-Hydrazones as novel acetylcholinesterase inhibitors","authors":"E. Mateev, Ali Irfan, Alexandrina Mateeva, M. Kondeva-Burdina, Maya Georgieva, A. Zlatkov","doi":"10.3897/pharmacia.71.e114120","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e114120","url":null,"abstract":"Virtual screening is emerging as a highly applied technique and gained prominence as widely used method for the search and identification of potential hits, significantly reducing the time needed to discover novel and effective compounds compared to high-throughput screening. Recently, the superiority of simulations with multiple programs compared to a single software docking has been discussed. The aim of this work was to apply consensus docking, molecular mechanics/generalized Born surface area (MM/GBSA) free binding energy recalculations, and in vitro evaluations on an in-house dataset of recently synthesized pyrrole-based hydrazide-hydrazones in the search for novel acetylcholinesterase (AChE) inhibitors. Two licensed softwares – GOLD 5.3 and Glide, were employed for the virtual screenings, and several chemotherapeutic potential hits were identified. Furthermore, MM/GBSA free binding energy recalculations were provided to enhance the robustness of the in silico results. The MM/GBSA scores of the top ten pyrrole-based hydrazide-hydrazones were ranging from -60.44 to -70.93 Kcal/mol. Subsequent, in vitro evaluations of the top ranked compounds revealed that 12d exhibited the highest AChE inhibitory activity, with a 55% inhibition rate at a concentration of 10 μM. Moreover, this prominent pyrrole-based AChE inhibitor formed stable complex with the active site of the enzyme. Interactions with the active amino residues Tyr72 and Tyr286 indicated that 12d was located near the peripheral anionic site of the enzyme. Additionally, in silicoADME investigations using QikProp demonstrated that 12d possesses optimal pharmacokinetic properties. In conclusion, this study identified a novel pyrrole-based AChE inhibitor 12d through a combination of computational and experimental findings.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":"91 2","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139863122","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}

引用次数: 0