Jawaher Abdullah Alamoudi, Yosif Almoshari, Hadil Faris Alotaibi
Abstract: Objectives: The objective of this study was to prepare carboplatin-loaded cubosomes using high sheer homogenization technique. Materials and Methods: The cubosomes were prepared using Glyceryl Monooleate (GMO) as a lipophilic carrier along with pluronic F-127 (PF-127) and tween 80 as additive of the formulation. All the ingredients were subjected to chemical compatibility studies by Fourier Transform Infra-Red (FTIR) spectroscopy, thermal analysis using Differential Scanning Calorimetry (DSC), whereas X-ray Diffraction (XRD) studies were performed to evaluate the nature of drug in pure form as well as in formulation. The prepared cubosomes were characterized for their size and surface charge, surface morphology, drug release studies and drug permeation studies. Results: FTIR has confirmed the chemical compatibilities of the ingredients, while DSC has exhibited the thermal stabilities of the drug in alone as well as in cubosomes. The XRD has reviled that drug was crystalline, but upon incorporation in cubosmes, the crystallinity has reduced remarkably. The prepared cubosomes were of nanosized (diameter of 227 nm) and cubical in shape. The in vitro drug release and drug permeation studies have showed that concentration of both GMO and PF-127 has effected the release as well as permeation of the drug. However, in 3 hr studies the maximum amount of drug release was ~84% and that of permeation was ~74%. Conclusion: Conclusively, the selected composition of the formulation was suitable enough to prepare the nanosized cubosomes showing suitable entrapment efficiency of the drug.
{"title":"Formulation and Evaluation of Pluronic F-127 Assisted Carboplatin Cubosomes","authors":"Jawaher Abdullah Alamoudi, Yosif Almoshari, Hadil Faris Alotaibi","doi":"10.5530/ijper.57.4.150","DOIUrl":"https://doi.org/10.5530/ijper.57.4.150","url":null,"abstract":"Abstract: Objectives: The objective of this study was to prepare carboplatin-loaded cubosomes using high sheer homogenization technique. Materials and Methods: The cubosomes were prepared using Glyceryl Monooleate (GMO) as a lipophilic carrier along with pluronic F-127 (PF-127) and tween 80 as additive of the formulation. All the ingredients were subjected to chemical compatibility studies by Fourier Transform Infra-Red (FTIR) spectroscopy, thermal analysis using Differential Scanning Calorimetry (DSC), whereas X-ray Diffraction (XRD) studies were performed to evaluate the nature of drug in pure form as well as in formulation. The prepared cubosomes were characterized for their size and surface charge, surface morphology, drug release studies and drug permeation studies. Results: FTIR has confirmed the chemical compatibilities of the ingredients, while DSC has exhibited the thermal stabilities of the drug in alone as well as in cubosomes. The XRD has reviled that drug was crystalline, but upon incorporation in cubosmes, the crystallinity has reduced remarkably. The prepared cubosomes were of nanosized (diameter of 227 nm) and cubical in shape. The in vitro drug release and drug permeation studies have showed that concentration of both GMO and PF-127 has effected the release as well as permeation of the drug. However, in 3 hr studies the maximum amount of drug release was ~84% and that of permeation was ~74%. Conclusion: Conclusively, the selected composition of the formulation was suitable enough to prepare the nanosized cubosomes showing suitable entrapment efficiency of the drug.","PeriodicalId":13407,"journal":{"name":"Indian Journal of Pharmaceutical Education and Research","volume":"186 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135645447","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}
Abstract: Background: The malarial scenario has significantly varied in the past few decades; whether it is funding or the range of sophisticated life-saving tools that have been improved, the disease burden has reduced, and even a few nations are on the verge of their elimination. Despite these, drug resistance is the major hurdle in the fight against malaria. Aim: Identifying new drug candidates with negligible toxicity are imperative to overcome the existing problem. The proposed study aims to identify new potential lead molecules via targeting the ADP-dependent DNA helicase RecQ of Plasmodium falciparum (isolate 3D7) using Target-Based Virtual Screening (TBVS), molecular docking, and dynamics simulations. Materials and Methods: Ligand molecules were retrieved from a comprehensive digital library of the MCULE database having millions of investigational compounds. Pfizer’s rule of five and the number of halogen atoms (3-5) were considered the basic primary filters of TBVS. The AutoDockVina (ADV) and GROningenMAchine for Chemical Simulations software were used to assess the molecular interactions and stability of protein-ligand complexes, respectively. Results: The primary filters of the TBVS work-pipeline depicted 2,597,040 chemical hits from over a hundred million small molecules. The toxicity tool sifted twenty-one molecules whose HIA and BBB permeation were evaluated through the Egan-Egg model. Five ligand hits were shortlisted with zero violation of drug-likeness and contain three or more hydrogen bonds. ADME, docking, and MD parameters depicted a molecule MCULE-1255186442-0-1 as a promising drug candidate. Conclusion: Druggable properties of identified ligands are inferred purely from the in silico experiments, so before its therapeutic implications, wet-lab validations are imperative. Keywords: Malaria, Plasmodium falciparum, DNA helicase, PfWrn, Docking, MD simulation.
摘要:背景:在过去的几十年里，疟疾的情况发生了显著变化;无论是在资金方面还是在先进的救生工具方面，疾病负担都有所减轻，甚至有几个国家即将消除这种负担。尽管如此，耐药性仍是抗击疟疾的主要障碍。目的:寻找毒性可忽略的新候选药物是克服现有问题的迫切需要。本研究旨在利用基于靶标的虚拟筛选(TBVS)、分子对接和动力学模拟等手段，针对恶性疟原虫(分离物3D7) adp依赖性DNA解旋酶RecQ，寻找新的潜在先导分子。材料和方法:从mcle数据库的综合数字图书馆中检索配体分子，该数据库包含数百万种研究化合物。辉瑞的5规则和卤素原子数(3-5)被认为是TBVS的基本过滤器。使用AutoDockVina (ADV)和GROningenMAchine for Chemical simulation软件分别评估蛋白质-配体复合物的分子相互作用和稳定性。结果:TBVS工作管道的初级过滤器描述了来自超过1亿个小分子的2,597,040个化学命中。毒性工具筛选了21个分子，通过Egan-Egg模型评估其HIA和血脑屏障通透性。五种配体被列入候选名单，没有违反药物相似性，并且含有三个或更多氢键。ADME、对接和MD参数将分子MCULE-1255186442-0-1描述为有前景的候选药物。结论:所鉴定的配体的药物性质完全是从硅实验中推断出来的，因此在其治疗意义之前，湿实验室验证是必要的。关键词:疟疾，恶性疟原虫，DNA解旋酶，PfWrn，对接，MD模拟
{"title":"Identifying Potential Drug Candidates against Plasmodium falciparum (Isolate 3D7) through Targeting ADP-dependent DNA Helicase RecQ: An in silico Approach","authors":"Marya Ahsan, Ayaz Khurram Mallick","doi":"10.5530/ijper.57.4.124","DOIUrl":"https://doi.org/10.5530/ijper.57.4.124","url":null,"abstract":"Abstract: Background: The malarial scenario has significantly varied in the past few decades; whether it is funding or the range of sophisticated life-saving tools that have been improved, the disease burden has reduced, and even a few nations are on the verge of their elimination. Despite these, drug resistance is the major hurdle in the fight against malaria. Aim: Identifying new drug candidates with negligible toxicity are imperative to overcome the existing problem. The proposed study aims to identify new potential lead molecules via targeting the ADP-dependent DNA helicase RecQ of Plasmodium falciparum (isolate 3D7) using Target-Based Virtual Screening (TBVS), molecular docking, and dynamics simulations. Materials and Methods: Ligand molecules were retrieved from a comprehensive digital library of the MCULE database having millions of investigational compounds. Pfizer’s rule of five and the number of halogen atoms (3-5) were considered the basic primary filters of TBVS. The AutoDockVina (ADV) and GROningenMAchine for Chemical Simulations software were used to assess the molecular interactions and stability of protein-ligand complexes, respectively. Results: The primary filters of the TBVS work-pipeline depicted 2,597,040 chemical hits from over a hundred million small molecules. The toxicity tool sifted twenty-one molecules whose HIA and BBB permeation were evaluated through the Egan-Egg model. Five ligand hits were shortlisted with zero violation of drug-likeness and contain three or more hydrogen bonds. ADME, docking, and MD parameters depicted a molecule MCULE-1255186442-0-1 as a promising drug candidate. Conclusion: Druggable properties of identified ligands are inferred purely from the in silico experiments, so before its therapeutic implications, wet-lab validations are imperative. Keywords: Malaria, Plasmodium falciparum, DNA helicase, PfWrn, Docking, MD simulation.","PeriodicalId":13407,"journal":{"name":"Indian Journal of Pharmaceutical Education and Research","volume":"19 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135645966","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}
Abstract: Introduction: Pharmacokinetics is one of the main courses of pharmacy majors in medical colleges and universities. The course is highly practical involving multidisciplinary collaboration, with strong logical reasoning and complex calculations. But the widespread traditional teaching methods resulted in poor practical application ability, self-learning ability, and problem-solving ability of students. Objectives: To enhance the students' knowledge and problem-solving ability, we focused on the curriculum reform of pharmacokinetics. Materials and Methods: It was based on the online and offline mixed teaching mode including revising the training program and syllabus, reconstructing the teaching staff, constructing online courses, designing class teaching, and careful teaching implementation, and construction of evaluation system. Finally, questionnaire survey was conducted to evaluate the implementation effect about the "online + offline" hybrid teaching mode. Results: It showed that the mixed online and offline teaching mode can help to solve the problem of difficulty in both teaching and learning the pharmacodynamics course. It changed the students' rigid learning methods that are not conducive to the cultivation of applied high-quality pharmaceutical talents. Moreover, this teaching reform enhanced the students' problem-solving ability. It achieved the course goals of cultivating students to be competent in medication guidance, drug quality control, and supervision positions, and to have the basic ideas and abilities to innovatively research and solve drug quality problems. Conclusion: This blended teaching mode may be an effective alternative to conventional approaches in pharmaceutical education. Keywords: Curriculum, Blended teaching mode, Pharmacokinetics, Pharmaceutical students.
{"title":"Design and Application of the Blended Teaching Mode in the Curriculum of Pharmacokinetics","authors":"Zhongbing Liu, Shuzao Wang, Yan Lin, Meiling Zhou, Pei Jing, Zhirong Zhong","doi":"10.5530/ijper.57.4.141","DOIUrl":"https://doi.org/10.5530/ijper.57.4.141","url":null,"abstract":"Abstract: Introduction: Pharmacokinetics is one of the main courses of pharmacy majors in medical colleges and universities. The course is highly practical involving multidisciplinary collaboration, with strong logical reasoning and complex calculations. But the widespread traditional teaching methods resulted in poor practical application ability, self-learning ability, and problem-solving ability of students. Objectives: To enhance the students' knowledge and problem-solving ability, we focused on the curriculum reform of pharmacokinetics. Materials and Methods: It was based on the online and offline mixed teaching mode including revising the training program and syllabus, reconstructing the teaching staff, constructing online courses, designing class teaching, and careful teaching implementation, and construction of evaluation system. Finally, questionnaire survey was conducted to evaluate the implementation effect about the \"online + offline\" hybrid teaching mode. Results: It showed that the mixed online and offline teaching mode can help to solve the problem of difficulty in both teaching and learning the pharmacodynamics course. It changed the students' rigid learning methods that are not conducive to the cultivation of applied high-quality pharmaceutical talents. Moreover, this teaching reform enhanced the students' problem-solving ability. It achieved the course goals of cultivating students to be competent in medication guidance, drug quality control, and supervision positions, and to have the basic ideas and abilities to innovatively research and solve drug quality problems. Conclusion: This blended teaching mode may be an effective alternative to conventional approaches in pharmaceutical education. Keywords: Curriculum, Blended teaching mode, Pharmacokinetics, Pharmaceutical students.","PeriodicalId":13407,"journal":{"name":"Indian Journal of Pharmaceutical Education and Research","volume":"30 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135646287","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}
Xiaoli Zhou, Hesham S Almoallim, Balasubramani Ravindran, Rui Qin
Abstract: Background: Alzheimer's Disease (AD), a neurodegenerative disorder characterized by dementia, is linked to ROS-induced stress, neuroinflammation, and gut microbiota imbalance. Objectives: The antioxidant and anti-inflammatory properties of citrollenol have already been reported. The current research was aimed at discovering the salutary properties of citrollenol against Aluminum Chloride (AlCl3 )-induced AD in rats. Materials and Methods: The AlCl3 was used to induce the AD in rats and then treated with citrollenol (25 and 50 mg/kg/bw). The behavioral tests were conducted on both control and treated rats. The levels of antioxidants and acetylcholine esterase were assessed using kits. The histopathological and immunohistochemical analyses were performed on the brain tissues. Results: The findings revealed that the AlCl3 -induced group had a loss of memory capability as well as an increase in the production of proinflammatory and neurodegenerative disorder-related AD proteins; otherwise, these characteristics were contrasted in the citrollenol-treated groups. Citrollenol-induced rats showed higher production of antioxidant enzyme levels and lower MDA status. Additionally, citrollenol abrogates proinflammatory mediator expression by suppressing NF-κB signaling and regulating microglial activation. Conclusion: Citrollenol can drawnback the AD brain tissue appearance of pathology study by leaking dysfunction in memory, learning capability, production of higher antioxidant enzymes levels, changing immunomodulatory cytokines levels in AlCl3 induced rats, exhibiting that AD pathogenesis may be represented by treatment with citrollenol via the neurodegenerative disorder causes from AD. Keywords: Alzheimer’s, AlCl3 , NF-kB, Malonaldehyde, Citrollenol, Neuroinflammation
{"title":"Citrollenol Abrogates Neuroinflammatory Pathway Regulated via Induction of NF-kB in AlCl3 Induced Alzheimer’s Disease – Molecular Approach","authors":"Xiaoli Zhou, Hesham S Almoallim, Balasubramani Ravindran, Rui Qin","doi":"10.5530/ijper.57.4.127","DOIUrl":"https://doi.org/10.5530/ijper.57.4.127","url":null,"abstract":"Abstract: Background: Alzheimer's Disease (AD), a neurodegenerative disorder characterized by dementia, is linked to ROS-induced stress, neuroinflammation, and gut microbiota imbalance. Objectives: The antioxidant and anti-inflammatory properties of citrollenol have already been reported. The current research was aimed at discovering the salutary properties of citrollenol against Aluminum Chloride (AlCl3 )-induced AD in rats. Materials and Methods: The AlCl3 was used to induce the AD in rats and then treated with citrollenol (25 and 50 mg/kg/bw). The behavioral tests were conducted on both control and treated rats. The levels of antioxidants and acetylcholine esterase were assessed using kits. The histopathological and immunohistochemical analyses were performed on the brain tissues. Results: The findings revealed that the AlCl3 -induced group had a loss of memory capability as well as an increase in the production of proinflammatory and neurodegenerative disorder-related AD proteins; otherwise, these characteristics were contrasted in the citrollenol-treated groups. Citrollenol-induced rats showed higher production of antioxidant enzyme levels and lower MDA status. Additionally, citrollenol abrogates proinflammatory mediator expression by suppressing NF-κB signaling and regulating microglial activation. Conclusion: Citrollenol can drawnback the AD brain tissue appearance of pathology study by leaking dysfunction in memory, learning capability, production of higher antioxidant enzymes levels, changing immunomodulatory cytokines levels in AlCl3 induced rats, exhibiting that AD pathogenesis may be represented by treatment with citrollenol via the neurodegenerative disorder causes from AD. Keywords: Alzheimer’s, AlCl3 , NF-kB, Malonaldehyde, Citrollenol, Neuroinflammation","PeriodicalId":13407,"journal":{"name":"Indian Journal of Pharmaceutical Education and Research","volume":"59 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135645309","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}
Abstract: Aim/Background: The oral-based drug delivery system has a great pace in this era of novel discoveries. The globe is running toward new medical dosage forms, but from the primer days of drug discovery to now, a major issue faced by pharmaceutical scientists is solubility and bioavailability issues. The nanoemulsions are the best suitable formulations which can upsurge the bioavailability of the insoluble drugs. In the past three years, many research activities have been conducted due to the pandemic situation. Almost all nations have concentrated on scientific and medical research during this process. Materials and Methods: In recent days, quercetin hydrate has been found to have anti-malarial activity for which the bioavailability can be uplifted by using Nanoemulsion formulations. The authors used the high-energy process for formulating the nanoemulsions with the support of design expert software, where it was easy to find the number of trials to be performed. Various tools are used for the optimization of formulations for novel drug delivery systems. These tools have been found advantageous as they lead to a reduction in the number of experiments and less wastage of costly reagents. The purpose of the selection of a Central Composite Design (CCD) was that it required fewer runs over various other designs. Results: According to the design expert, CCD software was accessible for 17 runs, which corresponded to 17 groupings or formulations. Batches produced by the experimental design were formulated and assessed for globule size and dispersibility. Conclusion: Even though quercetin hydrate has been approved as a remedy for the treatment of various disorders, its poor oral bioavailability due to poor aqueous solubility and variable absorption is still a challenge in its clinical applications. Quercetin hydrate-loaded nanoemulsion fabricated with Opuntia ficus indica seed oil, PEG400, tween 80, and ethanol resulted in getting nano-sized particles that help in drug solubility and bioavailability. This work illustrated the importance of nanoemulsion to enhance the bioavailability of Quercetin hydrate. Keywords: Quercetin hydrate, Bioavailability, Design expert, Globule size, Nanoemulsion.
{"title":"Quality by Design based Quercetin Hydrate Nanoemulsions for Enhanced Solubility by Reducing Particle Size","authors":"Lakavath Sunil Kumar, Hindustan Abdul Ahad","doi":"10.5530/ijper.57.4.118","DOIUrl":"https://doi.org/10.5530/ijper.57.4.118","url":null,"abstract":"Abstract: Aim/Background: The oral-based drug delivery system has a great pace in this era of novel discoveries. The globe is running toward new medical dosage forms, but from the primer days of drug discovery to now, a major issue faced by pharmaceutical scientists is solubility and bioavailability issues. The nanoemulsions are the best suitable formulations which can upsurge the bioavailability of the insoluble drugs. In the past three years, many research activities have been conducted due to the pandemic situation. Almost all nations have concentrated on scientific and medical research during this process. Materials and Methods: In recent days, quercetin hydrate has been found to have anti-malarial activity for which the bioavailability can be uplifted by using Nanoemulsion formulations. The authors used the high-energy process for formulating the nanoemulsions with the support of design expert software, where it was easy to find the number of trials to be performed. Various tools are used for the optimization of formulations for novel drug delivery systems. These tools have been found advantageous as they lead to a reduction in the number of experiments and less wastage of costly reagents. The purpose of the selection of a Central Composite Design (CCD) was that it required fewer runs over various other designs. Results: According to the design expert, CCD software was accessible for 17 runs, which corresponded to 17 groupings or formulations. Batches produced by the experimental design were formulated and assessed for globule size and dispersibility. Conclusion: Even though quercetin hydrate has been approved as a remedy for the treatment of various disorders, its poor oral bioavailability due to poor aqueous solubility and variable absorption is still a challenge in its clinical applications. Quercetin hydrate-loaded nanoemulsion fabricated with Opuntia ficus indica seed oil, PEG400, tween 80, and ethanol resulted in getting nano-sized particles that help in drug solubility and bioavailability. This work illustrated the importance of nanoemulsion to enhance the bioavailability of Quercetin hydrate. Keywords: Quercetin hydrate, Bioavailability, Design expert, Globule size, Nanoemulsion.","PeriodicalId":13407,"journal":{"name":"Indian Journal of Pharmaceutical Education and Research","volume":"38 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135645444","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}
Abstract: Background: Cyclophosphamide (CTX) is widely used in tumor treatment, but its clinical therapeutic effect is not ideal due to many side effects. Materials and Methods: In the present study, we researched the synergistic and attenuating effects of CⅡ-3 combined with CTX and their underlying mechanism in H22 tumor-bearing mice. Firstly, we established an H22 tumor-bearing mice model, and the body weight, tumor weight, and survival time were recorded. Secondly, HE staining of tumor tissue was performed, and the related organ index, NK cell killing activity, peripheral blood cells, and bone marrow nucleated cells were measured. Moreover, the changes in IL-6 and IFN-1β in serum were detected by ELISA. Finally, RT-qPCR and Western Blot were performed to detect the expressions of TLR4, TLR9 and NF-κB in tumor tissue. Results: The treatment of CⅡ-3 combined with CTX could increase life extension rate of H22 tumor-bearing mice, reduce tumor weight. Additionally, it could inhibit tumor cell proliferation, increase thymus and spleen index, enhance the activity of T cells in spleen, promote the killing activity of NK cells, and had a certain ameliorate effect on the reduction of WBC, Neut, LYM and bone marrow nucleated cells caused by CTX. And the expression of mRNA and the protein of TLR4, TLR9 and NF-κB in tumor mass of H22 tumor-bearing mice were down-regulated. Conclusion: There were synergistic and attenuating effects of CTX combined with CⅡ-3 in the treatment of tumor and the effects might be mediated by the TLR4/NF-κB and TLR9/NF-κB signaling pathways. Keywords Anti-tumor, Cyclophosphamide, Immune depression, Periplaneta americana, Synergism and attenuation.
{"title":"Synergistic and Toxicity-reducing Effects of Periplaneta americana Extract CⅡ-3 Combined with CTX on H22 Tumor Bearing Mice","authors":"Rui Yuan, Guangming Liu, Meixian Guo, Xiaobo Liu","doi":"10.5530/ijper.57.4.135","DOIUrl":"https://doi.org/10.5530/ijper.57.4.135","url":null,"abstract":"Abstract: Background: Cyclophosphamide (CTX) is widely used in tumor treatment, but its clinical therapeutic effect is not ideal due to many side effects. Materials and Methods: In the present study, we researched the synergistic and attenuating effects of CⅡ-3 combined with CTX and their underlying mechanism in H22 tumor-bearing mice. Firstly, we established an H22 tumor-bearing mice model, and the body weight, tumor weight, and survival time were recorded. Secondly, HE staining of tumor tissue was performed, and the related organ index, NK cell killing activity, peripheral blood cells, and bone marrow nucleated cells were measured. Moreover, the changes in IL-6 and IFN-1β in serum were detected by ELISA. Finally, RT-qPCR and Western Blot were performed to detect the expressions of TLR4, TLR9 and NF-κB in tumor tissue. Results: The treatment of CⅡ-3 combined with CTX could increase life extension rate of H22 tumor-bearing mice, reduce tumor weight. Additionally, it could inhibit tumor cell proliferation, increase thymus and spleen index, enhance the activity of T cells in spleen, promote the killing activity of NK cells, and had a certain ameliorate effect on the reduction of WBC, Neut, LYM and bone marrow nucleated cells caused by CTX. And the expression of mRNA and the protein of TLR4, TLR9 and NF-κB in tumor mass of H22 tumor-bearing mice were down-regulated. Conclusion: There were synergistic and attenuating effects of CTX combined with CⅡ-3 in the treatment of tumor and the effects might be mediated by the TLR4/NF-κB and TLR9/NF-κB signaling pathways. Keywords Anti-tumor, Cyclophosphamide, Immune depression, Periplaneta americana, Synergism and attenuation.","PeriodicalId":13407,"journal":{"name":"Indian Journal of Pharmaceutical Education and Research","volume":"210 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135646294","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}
Background: For the estimation of cabotegravir and rilpivirine in the bulk and pharmaceutical dosage form, a stability-indicating reverse-phase high-performance liquid chromatography method was developed and validated using an inertsil C 18 (150 x 4.6 mm, 5 µm) column. At a flow rate of 1.0 ml/min, a mobile phase containing a mixture of 0.01N ammonium acetate buffer (pH 3) and acetonitrile (65:35, v/v) was passed over the column. The column temperature was set at 30°C. A photodiode array detector was used at the wavelength of 257 nm. Results: Retention times of cabotegravir and rilpivirine were found to be 2.250 min and 2.823 min, respectively. The calibration curves were linear over the concentration range of 10-60 µg/ml and 15-90 µg/ml for cabotegravir and rilpivirine, respectively with a correlation coefficient ( R 2 ) of 0.999. The percent relative standard deviation (% RSD) for precision and robustness studies was found to be < 2%. The mean % recovery was obtained as 100.71 % and 100.01 % for cabotegravir and rilpivirine, respectively. The degradation during stability studies was more in the presence of oxidative conditions. Conclusion: The developed method was found to be simple, rapid, and economical and can be applied successfully for simultaneous estimation of cabotegravir and
背景:为了估计散装和药用剂型中的卡波特韦和利匹韦林，建立了一种稳定性指示的反相高效液相色谱法，并使用inertsil c18 (150 x 4.6 mm, 5µm)柱进行了验证。以1.0 ml/min的流速，将含有0.01N醋酸铵缓冲液(pH 3)和乙腈(65:35,v/v)混合物的流动相通过色谱柱。柱温设定为30℃。采用波长为257 nm的光电二极管阵列探测器。结果:卡波特韦和利匹韦林的滞留时间分别为2.250 min和2.823 min。cabotegravir和rilpivirine在10 ~ 60µg/ml和15 ~ 90µg/ml浓度范围内均呈线性，相关系数(r2)为0.999。发现精确度和稳健性研究的相对标准偏差(% RSD)百分比< 2%。卡波特韦和利匹韦林的平均回收率分别为100.71%和100.01%。在稳定性研究中，氧化条件下的降解更多。结论:所建立的方法简便、快速、经济，可成功地用于头孢替他韦和头孢替他韦的同时测定
{"title":"Stability Indicating Reverse Phase-High Performance Liquid Chromatography Method for Simultaneous Estimation of Cabotegravir and Rilpivirine","authors":"Padmabhushana Chary Vemuluri, S. Dodda","doi":"10.5530/ijper.57.3s.87","DOIUrl":"https://doi.org/10.5530/ijper.57.3s.87","url":null,"abstract":"Background: For the estimation of cabotegravir and rilpivirine in the bulk and pharmaceutical dosage form, a stability-indicating reverse-phase high-performance liquid chromatography method was developed and validated using an inertsil C 18 (150 x 4.6 mm, 5 µm) column. At a flow rate of 1.0 ml/min, a mobile phase containing a mixture of 0.01N ammonium acetate buffer (pH 3) and acetonitrile (65:35, v/v) was passed over the column. The column temperature was set at 30°C. A photodiode array detector was used at the wavelength of 257 nm. Results: Retention times of cabotegravir and rilpivirine were found to be 2.250 min and 2.823 min, respectively. The calibration curves were linear over the concentration range of 10-60 µg/ml and 15-90 µg/ml for cabotegravir and rilpivirine, respectively with a correlation coefficient ( R 2 ) of 0.999. The percent relative standard deviation (% RSD) for precision and robustness studies was found to be < 2%. The mean % recovery was obtained as 100.71 % and 100.01 % for cabotegravir and rilpivirine, respectively. The degradation during stability studies was more in the presence of oxidative conditions. Conclusion: The developed method was found to be simple, rapid, and economical and can be applied successfully for simultaneous estimation of cabotegravir and","PeriodicalId":13407,"journal":{"name":"Indian Journal of Pharmaceutical Education and Research","volume":" ","pages":""},"PeriodicalIF":0.8,"publicationDate":"2023-08-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44150336","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}
Madhu Subramanian, Komala Munuswamy, P. Pitchaimuthu
Background: Alzheimer's Disease (AD) suffers from dementia more often in 65-year or older patients. Symptoms of AD's are linked to disease-causing neurons, and current pharmacological therapies inadequately regulate deadly outcomes. Withania somnifera (L ) , has been contributing as a traditional multifunctional herb with a wide variety of health benefits. Materials and Methods: This research examined the importance of Withaferin A nanoparticles against scopolamine induced neuron loss (Impair on memory). Five groups of 6 rats weighing 150-200 g were randomly split. Negative and positive control animals received 2mL/kg saline solution in groups 1 and 2. 3 rd and 4 th group received 5mg/kg of pure Withaferin-A and Withaferin-A nanoformulation. Group 5 received 10 mg/kg of tacrine as a normal medication. Except for group 1, all other groups were induced 30 min after drug administration with 1mg/kg scopolamine. EPM was used to understand the behavioral parameters. Results: Inflexion ratios of 1.1 and 1.3 were seen in groups treated with Withaferin-A nanoparticles and the conventional medication. AchE, MDA, GSH reductase were also measured. Compared to the pure drug, Withaferin-A nanoparticles exhibited substantial activity. Withaferin-A exhibits an anti-amnesic effect similar to tacrine at a specific level. Conclusion: Withaferin-A nanoparticles may help neurodegenerative disease. To establish the formulation as a standard AD's treatment, pharmacokinetic aspects should be explored.
{"title":"Neuroprotective Effects of Withaferin-A Nanoparticles on Scopolamine Rat Model of Alzheimer’s Disease","authors":"Madhu Subramanian, Komala Munuswamy, P. Pitchaimuthu","doi":"10.5530/ijper.57.3s.70","DOIUrl":"https://doi.org/10.5530/ijper.57.3s.70","url":null,"abstract":"Background: Alzheimer's Disease (AD) suffers from dementia more often in 65-year or older patients. Symptoms of AD's are linked to disease-causing neurons, and current pharmacological therapies inadequately regulate deadly outcomes. Withania somnifera (L ) , has been contributing as a traditional multifunctional herb with a wide variety of health benefits. Materials and Methods: This research examined the importance of Withaferin A nanoparticles against scopolamine induced neuron loss (Impair on memory). Five groups of 6 rats weighing 150-200 g were randomly split. Negative and positive control animals received 2mL/kg saline solution in groups 1 and 2. 3 rd and 4 th group received 5mg/kg of pure Withaferin-A and Withaferin-A nanoformulation. Group 5 received 10 mg/kg of tacrine as a normal medication. Except for group 1, all other groups were induced 30 min after drug administration with 1mg/kg scopolamine. EPM was used to understand the behavioral parameters. Results: Inflexion ratios of 1.1 and 1.3 were seen in groups treated with Withaferin-A nanoparticles and the conventional medication. AchE, MDA, GSH reductase were also measured. Compared to the pure drug, Withaferin-A nanoparticles exhibited substantial activity. Withaferin-A exhibits an anti-amnesic effect similar to tacrine at a specific level. Conclusion: Withaferin-A nanoparticles may help neurodegenerative disease. To establish the formulation as a standard AD's treatment, pharmacokinetic aspects should be explored.","PeriodicalId":13407,"journal":{"name":"Indian Journal of Pharmaceutical Education and Research","volume":" ","pages":""},"PeriodicalIF":0.8,"publicationDate":"2023-08-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46743049","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}
The largest nation in South America, Brazil, is now the world's second-largest market for pharmaceuticals thanks to the country's economic growth. The Brazilian Health Surveillance Agency, also known as the National Agency for Health Surveillance (Agencia Nacional de Vigilancia Sanitaria - ANVISA), was founded in 1999 with the primary objective of protecting and strengthening public health surveillance over Brazilian products and services. Biological products, also known as biopharmaceuticals, are medications that are derived from biological systems and then created utilizing contemporary biotechnological techniques. These biological products are very different from traditional synthetic drugs in a number of important respects. Biosimilars are required to satisfy a variety of regulatory requirements before being given permission to enter the market in various regions. Other issues that are related to this need to be established by national authorities. These issues include interchangeability, labelling, and prescription information. The Brazilian health monitoring agency follows the fundamental criteria established by the World Health Organization for evaluating bio-similarity; nevertheless, it does not make use of the name "biosimilar." The objective of this article is to present the Brazilian biosimilar law.
{"title":"Analyzing Biosimilars in Brazil: Comprehensive Specifications of the Regulatory System","authors":"Kethareshwara Sujatha Deeksha, Balamuralidhara Veeranna, Gowthami Kodlahalli Ravindra","doi":"10.5530/ijper.57.3s.57","DOIUrl":"https://doi.org/10.5530/ijper.57.3s.57","url":null,"abstract":"The largest nation in South America, Brazil, is now the world's second-largest market for pharmaceuticals thanks to the country's economic growth. The Brazilian Health Surveillance Agency, also known as the National Agency for Health Surveillance (Agencia Nacional de Vigilancia Sanitaria - ANVISA), was founded in 1999 with the primary objective of protecting and strengthening public health surveillance over Brazilian products and services. Biological products, also known as biopharmaceuticals, are medications that are derived from biological systems and then created utilizing contemporary biotechnological techniques. These biological products are very different from traditional synthetic drugs in a number of important respects. Biosimilars are required to satisfy a variety of regulatory requirements before being given permission to enter the market in various regions. Other issues that are related to this need to be established by national authorities. These issues include interchangeability, labelling, and prescription information. The Brazilian health monitoring agency follows the fundamental criteria established by the World Health Organization for evaluating bio-similarity; nevertheless, it does not make use of the name \"biosimilar.\" The objective of this article is to present the Brazilian biosimilar law.","PeriodicalId":13407,"journal":{"name":"Indian Journal of Pharmaceutical Education and Research","volume":" ","pages":""},"PeriodicalIF":0.8,"publicationDate":"2023-08-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47218285","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}
In the last few decades, researchers have put a lot of time and effort into making new pharmaceuticals. As a result, there are now a huge number of pharmacological chemicals that can be used to treat a wide range of diseases that are a problem for the healthcare system. More than 50% of these medications are classed as BCS (Biopharmaceutical Classification System) class II/IV, indicating that they have limited therapeutic value and are not further studied. In this way, it has been shown that lipoidal manufacturing is a good way to distribute these kinds of medicines. This suggests that a method based on nanotechnology has a lot of potential. Nanoemulgel, a gel composed of diverse nano-lipoidal compositions, has been shown to be an effective method for applying topical drugs. Nanoemulgel is an emulsion-based topical gel product. The correct gelling ingredient is added to emulsion globules made using high energy or low energy processes to form nanoemulgel. Nanoemulgels can be made from all kinds of polymeric polymers, surfactants, and fats that range in size from 5 nm to 500 nm. Nanoemulgel has several topical treatments for both short-term and long-term problems. The widespread use of nanoemulgel formulations of recently patented drugs in a variety of healthcare settings has once again shown that topical administration is better than other methods. Toxicological studies of the chemicals used in these formulations must, however, take into account how safe they are, since the way they are given has changed a lot.
{"title":"Nanoemulgel: A Smarter Topical Lipidic Emulsion-based Nanocarrier","authors":"Suraj Mandal, Prabhakar Vishvakarma","doi":"10.5530/ijper.57.3s.56","DOIUrl":"https://doi.org/10.5530/ijper.57.3s.56","url":null,"abstract":"In the last few decades, researchers have put a lot of time and effort into making new pharmaceuticals. As a result, there are now a huge number of pharmacological chemicals that can be used to treat a wide range of diseases that are a problem for the healthcare system. More than 50% of these medications are classed as BCS (Biopharmaceutical Classification System) class II/IV, indicating that they have limited therapeutic value and are not further studied. In this way, it has been shown that lipoidal manufacturing is a good way to distribute these kinds of medicines. This suggests that a method based on nanotechnology has a lot of potential. Nanoemulgel, a gel composed of diverse nano-lipoidal compositions, has been shown to be an effective method for applying topical drugs. Nanoemulgel is an emulsion-based topical gel product. The correct gelling ingredient is added to emulsion globules made using high energy or low energy processes to form nanoemulgel. Nanoemulgels can be made from all kinds of polymeric polymers, surfactants, and fats that range in size from 5 nm to 500 nm. Nanoemulgel has several topical treatments for both short-term and long-term problems. The widespread use of nanoemulgel formulations of recently patented drugs in a variety of healthcare settings has once again shown that topical administration is better than other methods. Toxicological studies of the chemicals used in these formulations must, however, take into account how safe they are, since the way they are given has changed a lot.","PeriodicalId":13407,"journal":{"name":"Indian Journal of Pharmaceutical Education and Research","volume":" ","pages":""},"PeriodicalIF":0.8,"publicationDate":"2023-08-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49440892","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}
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