Pub Date : 2023-06-29DOI: 10.3390/scipharm91030032
K. Chandra, Sansa Dutta, H. Kolya, C. Kang
Cancer is a genetic disorder and its treatment usually requires a long time and expensive diagnosis. While chemotherapy is the most conventional approach in treating most cancers, patients often suffer from undesired side effects due to various pharmacokinetic aspects. To address this issue, target-oriented drug-delivery systems (DDS) or pulsatile drug-delivery systems (PDDS) have recently been developed as an alternative tool that takes care of the entire pharmacodynamic activities of drug action. Hydroxyethyl starch (HES) has emerged as an effective clinical tool for delivering anticancer agents into target cells. These systems have demonstrated significant potential as anticancer drug carrier conjugates through their innate pharmacokinetic properties with their safety profile. This review focuses primarily on the structural aspect during the use of HES or HES-based polymers as carriers for delivering well-known anticancer drugs. This review also indicates a perspective on the long-term research needed for the sake of improving modern drug-delivery systems based on HES polymers and in the form of nanocarriers.
{"title":"Structural Aspect of Hydroxyethyl-Starch–Anticancer-Drug-Conjugates as State-of-the-Art Drug Carriers","authors":"K. Chandra, Sansa Dutta, H. Kolya, C. Kang","doi":"10.3390/scipharm91030032","DOIUrl":"https://doi.org/10.3390/scipharm91030032","url":null,"abstract":"Cancer is a genetic disorder and its treatment usually requires a long time and expensive diagnosis. While chemotherapy is the most conventional approach in treating most cancers, patients often suffer from undesired side effects due to various pharmacokinetic aspects. To address this issue, target-oriented drug-delivery systems (DDS) or pulsatile drug-delivery systems (PDDS) have recently been developed as an alternative tool that takes care of the entire pharmacodynamic activities of drug action. Hydroxyethyl starch (HES) has emerged as an effective clinical tool for delivering anticancer agents into target cells. These systems have demonstrated significant potential as anticancer drug carrier conjugates through their innate pharmacokinetic properties with their safety profile. This review focuses primarily on the structural aspect during the use of HES or HES-based polymers as carriers for delivering well-known anticancer drugs. This review also indicates a perspective on the long-term research needed for the sake of improving modern drug-delivery systems based on HES polymers and in the form of nanocarriers.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2023-06-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44652832","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}
Pub Date : 2023-06-28DOI: 10.3390/scipharm91030031
A. Parlar, B. Gurel, Mehmet Reşit Sönmez, Meral Yüce
Alterations in the biological activity of the molecules under stress conditions have not been documented as widely in the literature yet. This study was designed to reveal the functional impacts of various oxidation conditions on a model mAb, a commercial anti-VEGF IgG molecule. The responses to antigen binding, cell proliferation, FcRn receptors, and C1q binding, which rarely appear in the current literature, were investigated. The authors report peptide mapping data, post-translational modification (PTM) analysis, cell proliferation performance, and antigen (VEGF), C1q, and FcRn binding activities of the mAb under various stress conditions. The oxidation-prone site of the mAb was determined as Met252 in the DTLMISR peptide. The VEGF binding activity and anti-cell proliferation activity of the mAbs did not alter, while C1q and FcRn binding capacity significantly decreased under oxidative stress conditions. The full report is vital for many scientific and industrial processes about mAbs. The authors recommend performing functional analyses in addition to the structural studies while investigating the impacts of stress factors on therapeutic mAbs.
{"title":"Analytical Investigation of Forced Oxidized Anti-VEGF IgG Molecules: A Focus on the Alterations in Antigen and Receptor Binding Activities","authors":"A. Parlar, B. Gurel, Mehmet Reşit Sönmez, Meral Yüce","doi":"10.3390/scipharm91030031","DOIUrl":"https://doi.org/10.3390/scipharm91030031","url":null,"abstract":"Alterations in the biological activity of the molecules under stress conditions have not been documented as widely in the literature yet. This study was designed to reveal the functional impacts of various oxidation conditions on a model mAb, a commercial anti-VEGF IgG molecule. The responses to antigen binding, cell proliferation, FcRn receptors, and C1q binding, which rarely appear in the current literature, were investigated. The authors report peptide mapping data, post-translational modification (PTM) analysis, cell proliferation performance, and antigen (VEGF), C1q, and FcRn binding activities of the mAb under various stress conditions. The oxidation-prone site of the mAb was determined as Met252 in the DTLMISR peptide. The VEGF binding activity and anti-cell proliferation activity of the mAbs did not alter, while C1q and FcRn binding capacity significantly decreased under oxidative stress conditions. The full report is vital for many scientific and industrial processes about mAbs. The authors recommend performing functional analyses in addition to the structural studies while investigating the impacts of stress factors on therapeutic mAbs.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2023-06-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47189700","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}
Pub Date : 2023-06-27DOI: 10.3390/scipharm91030030
Chaowalit Monton, Thaniya Wunnakup, Jirapornchai Suksaeree, L. Charoenchai, Natawat Chankana
This study aimed to prepare tablets of black pepper extract using the Design of Experiments (DOE) approach. The levels of three factors—compressional force, croscarmellose sodium (CCS), and microcrystalline cellulose (MCC)—were screened using the one-factor-at-a-time technique, followed by the DOE utilizing the Box–Behnken design. The respective variations for each factor were as follows: compressional force (1500–2500 psi), CCS (1–3%), and MCC (32–42%). The results indicated that compressional force significantly decreased tablet thickness and friability, while increasing hardness and prolonging disintegration time. CCS significantly shortened disintegration time but did not affect tablet thickness, hardness, and friability. MCC, on the other hand, significantly increased tablet thickness and hardness, while significantly decreasing friability. Furthermore, the study observed interactions among factors and quadratic effects of each factor, which significantly influenced tablet properties. The optimal tablet formulation consisted of 2.2% CCS, 37% MCC, and a compressional force of 2000 psi. These tablets had a weight of 198.39 ± 0.49 mg, a diameter of 9.67 ± 0.01 mm, a thickness of 1.98 ± 0.02 mm, a hardness of 7.36 ± 0.24 kP, a friability of 0.11 ± 0.02%, and a disintegration time of 5.59 ± 0.39 min. The actual values obtained using the optimal conditions closely matched the predicted values, with a low percent error (less than 5%). In conclusion, the application of the DOE approach successfully developed tablets of black pepper extract, which can be utilized as food supplement products.
{"title":"Impact of Compressional Force, Croscarmellose Sodium, and Microcrystalline Cellulose on Black Pepper Extract Tablet Properties Based on Design of Experiments Approach","authors":"Chaowalit Monton, Thaniya Wunnakup, Jirapornchai Suksaeree, L. Charoenchai, Natawat Chankana","doi":"10.3390/scipharm91030030","DOIUrl":"https://doi.org/10.3390/scipharm91030030","url":null,"abstract":"This study aimed to prepare tablets of black pepper extract using the Design of Experiments (DOE) approach. The levels of three factors—compressional force, croscarmellose sodium (CCS), and microcrystalline cellulose (MCC)—were screened using the one-factor-at-a-time technique, followed by the DOE utilizing the Box–Behnken design. The respective variations for each factor were as follows: compressional force (1500–2500 psi), CCS (1–3%), and MCC (32–42%). The results indicated that compressional force significantly decreased tablet thickness and friability, while increasing hardness and prolonging disintegration time. CCS significantly shortened disintegration time but did not affect tablet thickness, hardness, and friability. MCC, on the other hand, significantly increased tablet thickness and hardness, while significantly decreasing friability. Furthermore, the study observed interactions among factors and quadratic effects of each factor, which significantly influenced tablet properties. The optimal tablet formulation consisted of 2.2% CCS, 37% MCC, and a compressional force of 2000 psi. These tablets had a weight of 198.39 ± 0.49 mg, a diameter of 9.67 ± 0.01 mm, a thickness of 1.98 ± 0.02 mm, a hardness of 7.36 ± 0.24 kP, a friability of 0.11 ± 0.02%, and a disintegration time of 5.59 ± 0.39 min. The actual values obtained using the optimal conditions closely matched the predicted values, with a low percent error (less than 5%). In conclusion, the application of the DOE approach successfully developed tablets of black pepper extract, which can be utilized as food supplement products.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2023-06-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44942111","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}
Pub Date : 2023-06-24DOI: 10.3390/scipharm91030029
L. Bracht, J. Constantin, R. Peralta, A. Bracht
The actions of Eli Lilly-rDNA glucagon and Novo Nordisk-rDNA glucagon on glycogen catabolism and related parameters were investigated using the bivascularly perfused rat liver. The technique allows glucagon to be supplied to a selective portion of the hepatic periportal region (≈39%) when the former is infused into the hepatic artery in retrograde perfusion. Both glucagon preparations were equally effective in influencing metabolism (glucose output, glycolysis and O2 uptake) when supplied to all cells along the liver sinusoids. When only a selective periportal region of the liver was supplied with the hormone, however, the action of Novo Nordisk-rDNA glucagon was proportional to the accessible cell space, whereas the action of Eli Lilly-rDNA glucagon greatly exceeded the action that was expected for the accessible space. Chromatographically, both rDNA preparations were not pure, but their impurities were not the same. The impurities in Eli Lilly-rDNA glucagon resembled those found in the similarly acting pancreatic Eli Lilly glucagon. It was concluded that the space-extrapolating action of Eli Lilly-rDNA glucagon is caused by a yet-to-be-identified impurity. The hypothesis was raised that an impurity in certain glucagon preparations can enhance cell-to-cell propagation of the glucagon signal, possibly via gap junctional communication.
{"title":"Escherichia coli (Lilly) and Saccharomyces cerevisiae (Novo) rDNA Glucagon: An Assessment of Their Actions When Supplied Selectively to Periportal Cells in the Bivascularly Perfused Rat Liver","authors":"L. Bracht, J. Constantin, R. Peralta, A. Bracht","doi":"10.3390/scipharm91030029","DOIUrl":"https://doi.org/10.3390/scipharm91030029","url":null,"abstract":"The actions of Eli Lilly-rDNA glucagon and Novo Nordisk-rDNA glucagon on glycogen catabolism and related parameters were investigated using the bivascularly perfused rat liver. The technique allows glucagon to be supplied to a selective portion of the hepatic periportal region (≈39%) when the former is infused into the hepatic artery in retrograde perfusion. Both glucagon preparations were equally effective in influencing metabolism (glucose output, glycolysis and O2 uptake) when supplied to all cells along the liver sinusoids. When only a selective periportal region of the liver was supplied with the hormone, however, the action of Novo Nordisk-rDNA glucagon was proportional to the accessible cell space, whereas the action of Eli Lilly-rDNA glucagon greatly exceeded the action that was expected for the accessible space. Chromatographically, both rDNA preparations were not pure, but their impurities were not the same. The impurities in Eli Lilly-rDNA glucagon resembled those found in the similarly acting pancreatic Eli Lilly glucagon. It was concluded that the space-extrapolating action of Eli Lilly-rDNA glucagon is caused by a yet-to-be-identified impurity. The hypothesis was raised that an impurity in certain glucagon preparations can enhance cell-to-cell propagation of the glucagon signal, possibly via gap junctional communication.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2023-06-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45143854","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}
Pub Date : 2023-06-14DOI: 10.3390/scipharm91020028
V. Oberemok, O. Andreeva, E. E. Alieva, Anastasiya Bilyk
The modern world, swaddled in the benefits of civilization, has fostered the development of science and the introduction of products of technological progress. This has allowed serious individual health problems, including those associated with viral diseases, to become targets for prophylaxis, treatment, and even cure. Human immunodeficiency viruses, hepatitis viruses, coronaviruses, and influenza viruses are among the most disturbing infectious agents in the human experience. Influenza appears to be one of the oldest viruses known to man; these viruses were among the first to cause major epidemics and pandemics in human history, collectively causing up to 0.5 million deaths worldwide each year. The main problem in the fight against influenza viruses is that they mutate constantly, which leads to molecular changes in antigens, including outer membrane glycoproteins, which play a critical role in the creation of modern vaccines. Due to the constant microevolution of the virus, influenza vaccine formulas have to be reviewed and improved every year. Today, flu vaccines represent an eternal molecular race between a person and a virus, which neither entity seems likely to win.
{"title":"New Advances and Perspectives of Influenza Prevention: Current State of the Art","authors":"V. Oberemok, O. Andreeva, E. E. Alieva, Anastasiya Bilyk","doi":"10.3390/scipharm91020028","DOIUrl":"https://doi.org/10.3390/scipharm91020028","url":null,"abstract":"The modern world, swaddled in the benefits of civilization, has fostered the development of science and the introduction of products of technological progress. This has allowed serious individual health problems, including those associated with viral diseases, to become targets for prophylaxis, treatment, and even cure. Human immunodeficiency viruses, hepatitis viruses, coronaviruses, and influenza viruses are among the most disturbing infectious agents in the human experience. Influenza appears to be one of the oldest viruses known to man; these viruses were among the first to cause major epidemics and pandemics in human history, collectively causing up to 0.5 million deaths worldwide each year. The main problem in the fight against influenza viruses is that they mutate constantly, which leads to molecular changes in antigens, including outer membrane glycoproteins, which play a critical role in the creation of modern vaccines. Due to the constant microevolution of the virus, influenza vaccine formulas have to be reviewed and improved every year. Today, flu vaccines represent an eternal molecular race between a person and a virus, which neither entity seems likely to win.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2023-06-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44504755","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}
Pub Date : 2023-05-31DOI: 10.3390/scipharm91020027
Deepak Kulkarni, D. Gadade, Nutan Chapaitkar, S. Shelke, S. Pekamwar, Rushikesh Aher, Ankita Ahire, Manjusha Avhale, Rupali Badgule, Radhika Bansode, Bhujang Bobade
Microneedles are gaining popularity as a new paradigm in the area of transdermal drug delivery for biomedical and healthcare applications. Efficient drug delivery with minimal invasion is the prime advantage of microneedles. The concept of the microneedle array provides an extensive surface area for efficient drug delivery. Various types of inorganics (silicon, ceramic, metal, etc.) and polymeric materials are used for the fabrication of microneedles. The polymeric microneedles have various advantages over other microneedles fabricated using inorganic material, such as biocompatibility, biodegradation, and non-toxicity. The wide variety of polymers used in microneedle fabrication can provide a broad scope for drug delivery and other biomedical applications. Multiple metallic and polymeric microneedles can be functionalized by polymer coatings for various biomedical applications. The fabrication of polymeric microneedles is shifting from conventional to advanced 3D and 4D printing technology. The multifaceted biomedical applications of polymeric microneedles include drug delivery, vaccine delivery, biosensing, and diagnostic applications. Here, we provide the overview of the current and advanced information on polymers used for fabrication, the selection criteria for polymers, biomedical applications, and the regulatory perspective of polymer-based and polymer-coated microneedles, along with a patent scenario.
{"title":"Polymeric Microneedles: An Emerging Paradigm for Advanced Biomedical Applications","authors":"Deepak Kulkarni, D. Gadade, Nutan Chapaitkar, S. Shelke, S. Pekamwar, Rushikesh Aher, Ankita Ahire, Manjusha Avhale, Rupali Badgule, Radhika Bansode, Bhujang Bobade","doi":"10.3390/scipharm91020027","DOIUrl":"https://doi.org/10.3390/scipharm91020027","url":null,"abstract":"Microneedles are gaining popularity as a new paradigm in the area of transdermal drug delivery for biomedical and healthcare applications. Efficient drug delivery with minimal invasion is the prime advantage of microneedles. The concept of the microneedle array provides an extensive surface area for efficient drug delivery. Various types of inorganics (silicon, ceramic, metal, etc.) and polymeric materials are used for the fabrication of microneedles. The polymeric microneedles have various advantages over other microneedles fabricated using inorganic material, such as biocompatibility, biodegradation, and non-toxicity. The wide variety of polymers used in microneedle fabrication can provide a broad scope for drug delivery and other biomedical applications. Multiple metallic and polymeric microneedles can be functionalized by polymer coatings for various biomedical applications. The fabrication of polymeric microneedles is shifting from conventional to advanced 3D and 4D printing technology. The multifaceted biomedical applications of polymeric microneedles include drug delivery, vaccine delivery, biosensing, and diagnostic applications. Here, we provide the overview of the current and advanced information on polymers used for fabrication, the selection criteria for polymers, biomedical applications, and the regulatory perspective of polymer-based and polymer-coated microneedles, along with a patent scenario.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2023-05-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45491060","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}
Pub Date : 2023-05-16DOI: 10.3390/scipharm91020026
Sergii Demchenko, R. Lesyk, O. Yadlovskyi, S. Holota, Sergii Yarmoluk, Sergii Tsyhankov, A. Demchenko
Non-steroidal anti-inflammatory drugs (NSAIDs) are one of the oldest and most widely used groups of drugs nowadays. However, the problem of searching for and creating new NSAIDs remains open, primarily due to the risks owing to their short- and long-term use. In this context, triazole-azepine hybrid molecules are attractive and prospective objects for the rational design of novel potential NSAIDs. In the present work studies of 3-aryl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepines as potential non-steroidal anti-inflammatory agents are reported. Evaluation of drug-like properties for all tested triazole-azepine hybrids was performed in silico using SwissADME. The screening of analgesic and anti-inflammatory activities was performed in vivo using acid-induced writhing and carrageenin-induced hind paw oedema models in mice. Derivatives with activity levels more potent compared with reference drugs ketorolac and diclofenac sodium were identified. Preliminary SAR was performed based on the screening results.
{"title":"Fused Triazole-Azepine Hybrids as Potential Non-Steroidal Antiinflammatory Agents","authors":"Sergii Demchenko, R. Lesyk, O. Yadlovskyi, S. Holota, Sergii Yarmoluk, Sergii Tsyhankov, A. Demchenko","doi":"10.3390/scipharm91020026","DOIUrl":"https://doi.org/10.3390/scipharm91020026","url":null,"abstract":"Non-steroidal anti-inflammatory drugs (NSAIDs) are one of the oldest and most widely used groups of drugs nowadays. However, the problem of searching for and creating new NSAIDs remains open, primarily due to the risks owing to their short- and long-term use. In this context, triazole-azepine hybrid molecules are attractive and prospective objects for the rational design of novel potential NSAIDs. In the present work studies of 3-aryl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepines as potential non-steroidal anti-inflammatory agents are reported. Evaluation of drug-like properties for all tested triazole-azepine hybrids was performed in silico using SwissADME. The screening of analgesic and anti-inflammatory activities was performed in vivo using acid-induced writhing and carrageenin-induced hind paw oedema models in mice. Derivatives with activity levels more potent compared with reference drugs ketorolac and diclofenac sodium were identified. Preliminary SAR was performed based on the screening results.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2023-05-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46356659","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}
Pub Date : 2023-05-04DOI: 10.3390/scipharm91020025
V. Kokova, E. Apostolova
Etifoxine is an anxiolytic drug with a dual mechanism of action. In contrast to conventional benzodiazepine anxiolytics, which induce cognitive dysfunction and myorelaxation, no memory impairment nor a decrease in motor activity is observed with etifoxine. This study aims to evaluate the effects of etifoxine on locomotor activity and passive learning in rats with diazepam-induced memory deficit. Male Wistar rats were treated intraperitoneally for 7 days with: (1) saline; (2) diazepam 2.5 mg/kg bw or (3) diazepam 2.5 mg/kg bw and etifoxine in a dose of 50 mg/kg bw. Activity cage test was used for evaluation of locomotor activity, and step-through and step-down tests were performed to study the passive learning. Etifoxine increased the number of horizontal movements on the 7th and 14th days of the experiment. The drug exhibits anti-amnesic effect in a model of diazepam-induced anterograde amnesia by enhancing long-term memory in passive learning tests. The data obtained suggest that etifoxine can reduce the benzodiazepine-induced cognitive deficit. Moreover, such a combination can alleviate the negative influence of benzodiazepines on locomotor activity. However, additional studies are necessary to translate these results into clinical practice.
{"title":"Effect of Etifoxine on Locomotor Activity and Passive Learning in Rats with Diazepam-Induced Cognitive Deficit","authors":"V. Kokova, E. Apostolova","doi":"10.3390/scipharm91020025","DOIUrl":"https://doi.org/10.3390/scipharm91020025","url":null,"abstract":"Etifoxine is an anxiolytic drug with a dual mechanism of action. In contrast to conventional benzodiazepine anxiolytics, which induce cognitive dysfunction and myorelaxation, no memory impairment nor a decrease in motor activity is observed with etifoxine. This study aims to evaluate the effects of etifoxine on locomotor activity and passive learning in rats with diazepam-induced memory deficit. Male Wistar rats were treated intraperitoneally for 7 days with: (1) saline; (2) diazepam 2.5 mg/kg bw or (3) diazepam 2.5 mg/kg bw and etifoxine in a dose of 50 mg/kg bw. Activity cage test was used for evaluation of locomotor activity, and step-through and step-down tests were performed to study the passive learning. Etifoxine increased the number of horizontal movements on the 7th and 14th days of the experiment. The drug exhibits anti-amnesic effect in a model of diazepam-induced anterograde amnesia by enhancing long-term memory in passive learning tests. The data obtained suggest that etifoxine can reduce the benzodiazepine-induced cognitive deficit. Moreover, such a combination can alleviate the negative influence of benzodiazepines on locomotor activity. However, additional studies are necessary to translate these results into clinical practice.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2023-05-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41635313","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}
The Zingiber montanum herbal compress remedy is a type of herbal medicine that can be used as an alternative treatment for improving pain symptoms. This study aimed to evaluate the clinical efficacy of a Z. montanum herbal compress remedy for pain relief. PubMed, Scopus, ScienceDirect, and Thai databases were systematically searched for relevant articles published from inception to December 2022. Only randomized clinical trials (RCTs) wherein the efficacy of the Z. montanum remedy was compared to that of a placebo or non-steroidal anti-inflammatory drugs (NSAIDs) were included. Six RCTs with a total of 812 patients were included in the analysis. The efficacy of the Z. montanum remedy had a significantly decreased pain score compared to the placebo (SMD = −0.63; 95% CI = −1.20, −0.06; I2 = 90%), but there was no significant difference when compared to NSAIDs (SMD = −0.61; 95% CI = −1.41, 0.81; I2 = 73%). Moreover, the efficacy of the Z. montanum remedy in terms of the flexibility score (SMD = 0.59; 95% CI −0.56, 1.74; I2 = 86.0%) and quality of life (SMD = 0.34; 95% CI −0.38, 1.05; I2 = 81.0%) was similar to that of the placebo. This meta-analysis demonstrates that the use of the Z. montanum herbal compress remedy significantly reduces the pain scores reported by patients.
{"title":"Effectiveness of Zingiber montanum Herbal Compress Remedy for Pain Management: An Updated Systematic Review and Meta-Analysis","authors":"Kanjana Worasing, Bunleu Sungthong, Wiraphol Phimarn","doi":"10.3390/scipharm91020024","DOIUrl":"https://doi.org/10.3390/scipharm91020024","url":null,"abstract":"The Zingiber montanum herbal compress remedy is a type of herbal medicine that can be used as an alternative treatment for improving pain symptoms. This study aimed to evaluate the clinical efficacy of a Z. montanum herbal compress remedy for pain relief. PubMed, Scopus, ScienceDirect, and Thai databases were systematically searched for relevant articles published from inception to December 2022. Only randomized clinical trials (RCTs) wherein the efficacy of the Z. montanum remedy was compared to that of a placebo or non-steroidal anti-inflammatory drugs (NSAIDs) were included. Six RCTs with a total of 812 patients were included in the analysis. The efficacy of the Z. montanum remedy had a significantly decreased pain score compared to the placebo (SMD = −0.63; 95% CI = −1.20, −0.06; I2 = 90%), but there was no significant difference when compared to NSAIDs (SMD = −0.61; 95% CI = −1.41, 0.81; I2 = 73%). Moreover, the efficacy of the Z. montanum remedy in terms of the flexibility score (SMD = 0.59; 95% CI −0.56, 1.74; I2 = 86.0%) and quality of life (SMD = 0.34; 95% CI −0.38, 1.05; I2 = 81.0%) was similar to that of the placebo. This meta-analysis demonstrates that the use of the Z. montanum herbal compress remedy significantly reduces the pain scores reported by patients.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2023-05-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44790235","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}
Pub Date : 2023-04-25DOI: 10.3390/scipharm91020023
V. R. Timergalieva, C. Gennari, F. Cilurzo, F. Selmin, R. I. Moustafine
The aim of this study is to compare three different dissolution methods to assess the drug release from oral lyophilisates, based on interpolyelectrolyte complexes (IPECs). IPECs were prepared by mixing solutions of a linear polymer, Eudragit® EPO, with a polymer with a cross-linked structure, Noveon® AA-1 or Carbopol® 10 Ultrez (in ratios of 1:2 and 1:1, respectively). Metformin or metronidazole were used as model drugs to achieve a systemic or local effect. A comparative assessment of the drug release kinetics was carried out using artificial saliva and three different set-ups: a paddle stirrer (USP apparatus 2), a flow cell (USP apparatus 4) and a Franz diffusion cell. The results demonstrated that oral lyophilisates disintegrated within 1 min. In the case of metformin, the drug release was completed in about 90 min independently of the set-up. The static conditions in the Franz diffusion cell and USP apparatus 2 permitted the aggregation of the IPEC; therefore, the release profiles show a significant difference compared to the USP apparatus 4.
{"title":"Comparative Evaluation of Metformin and Metronidazole Release from Oral Lyophilisates with Different Methods","authors":"V. R. Timergalieva, C. Gennari, F. Cilurzo, F. Selmin, R. I. Moustafine","doi":"10.3390/scipharm91020023","DOIUrl":"https://doi.org/10.3390/scipharm91020023","url":null,"abstract":"The aim of this study is to compare three different dissolution methods to assess the drug release from oral lyophilisates, based on interpolyelectrolyte complexes (IPECs). IPECs were prepared by mixing solutions of a linear polymer, Eudragit® EPO, with a polymer with a cross-linked structure, Noveon® AA-1 or Carbopol® 10 Ultrez (in ratios of 1:2 and 1:1, respectively). Metformin or metronidazole were used as model drugs to achieve a systemic or local effect. A comparative assessment of the drug release kinetics was carried out using artificial saliva and three different set-ups: a paddle stirrer (USP apparatus 2), a flow cell (USP apparatus 4) and a Franz diffusion cell. The results demonstrated that oral lyophilisates disintegrated within 1 min. In the case of metformin, the drug release was completed in about 90 min independently of the set-up. The static conditions in the Franz diffusion cell and USP apparatus 2 permitted the aggregation of the IPEC; therefore, the release profiles show a significant difference compared to the USP apparatus 4.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2023-04-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47603624","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}
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