Iranian Journal of Pharmaceutical Research : IJPR最新文献_第10页

Development of 1,2,4-Triazole-5-Thione Derivatives as Potential Inhibitors of Enoyl Acyl Carrier Protein Reductase (InhA) in Tuberculosis. 1,2,4-三唑-5-硫酮衍生物作为结核病中烯丙酰基载体蛋白还原酶(InhA)潜在抑制剂的研究进展。

IF 1.6

Iranian Journal of Pharmaceutical Research : IJPR Pub Date : 2019-01-01 DOI: 10.22037/ijpr.2019.112039.13495

Dhagash Vora, Neha Upadhyay, Kalpana Tilekar, Viral Jain, C S Ramaa

引用次数: 4

Main Elements of National Model of Electronic Prescription System from Physicians' Point of View: A Case Study in a Developing Country. 从医师角度看国家电子处方系统模式的要素:以发展中国家为例。

IF 1.6

Iranian Journal of Pharmaceutical Research : IJPR Pub Date : 2019-01-01 DOI: 10.22037/ijpr.2019.1100801

Mahnaz Samadbeik, Maryam Ahmadi, Farahnaz Sadoughi, Ali Garavand

{"title":"Main Elements of National Model of Electronic Prescription System from Physicians' Point of View: A Case Study in a Developing Country.","authors":"Mahnaz Samadbeik, Maryam Ahmadi, Farahnaz Sadoughi, Ali Garavand","doi":"10.22037/ijpr.2019.1100801","DOIUrl":"https://doi.org/10.22037/ijpr.2019.1100801","url":null,"abstract":"Identifying the factors and components of an electronic prescription system is of utmost importance in effective designing and implementation of this system. In this regard, the current study was conducted to determine the main factors affecting the national model of electronic prescription from the physicians' point of view. This is a cross-sectional, descriptive-analytical research carried out in 2015. Based on the census sampling method, 104 members of the board of directors of the Iranian general practitioners' associations, general practitioners' alumni association of Iran, and physicians owner of a website or weblog were selected as samples for this study. Data were collected using a valid and reliable questionnaire. After analyzing the data with SPSS software (v.16), a model was proposed using a regression algorithm. The findings indicated that accessing the current medication data and medication history of patients during prescription, and also creating the electronic patient medication record (ePMR) are the most important selective components for physicians with frequency percent of 92.1%. Moreover, from the physicians' viewpoint, the method of \"transmission of prescriptions to the central national database and retrieving prescriptions information from the selected pharmacy of the patient\" had the highest priority (weight coefficient) in the model of the national electronic prescription system. Therefore, the Iranian prescription system is required to be developed based on the centralized architecture and national electronic prescription database.","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"2204-2215"},"PeriodicalIF":1.6,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7059044/pdf/ijpr-18-2204.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37747096","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 1

Synthesis of 4-Methoxy-1, 3-Benzenediolylhydrazones and Evaluation of Their Anti-Platelet Aggregation Activity. 4-甲氧基- 1,3 -苯二醇腙的合成及其抗血小板聚集活性评价。

IF 1.6

Iranian Journal of Pharmaceutical Research : IJPR Pub Date : 2019-01-01 DOI: 10.22037/ijpr.2019.1100856

Chaoqing Wang, Yan Wang, Qingsong Deng, Xiujie Liu

{"title":"Synthesis of 4-Methoxy-1, 3-Benzenediolylhydrazones and Evaluation of Their Anti-Platelet Aggregation Activity.","authors":"Chaoqing Wang, Yan Wang, Qingsong Deng, Xiujie Liu","doi":"10.22037/ijpr.2019.1100856","DOIUrl":"https://doi.org/10.22037/ijpr.2019.1100856","url":null,"abstract":"In our present investigation, a series of novel 4-methoxy-1,3-benzenediolyl-hydrazones were designed and synthesized, and their ability to inhibit platelet aggregation was evaluated by adenosine diphosphate (ADP) and arachidonic acid (AA). The structures of the synthesized compounds were conﬁrmed by spectral data. Results demonstrated that the activities of all compounds excelled the positive drug Picotamide (25.1% inhibition rate) and seven compounds (PNN01, PNN03, PNN05, PNN07, PNN09, PNN12, and PNN14) have efficiently inhibited platelet aggregation even higher than Clopidogrel (37.6% inhibition rate) induced by AA. Among them, PNN07 (39.8% inhibition rate) was considered as the most potent analogue. Evaluation of cytotoxic activity of the compounds against L929 cell line revealed that none of the compounds have signiﬁcant cytotoxicity. Thus, diolylhydrazones derives are potential to be antiplatelet aggregation inhibitors and maybe working in AA-induced selectively.","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"1803-1815"},"PeriodicalIF":1.6,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7059039/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37747271","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Efficacy of Alpha-lipoic Acid in The Management of Diabetes Mellitus: A Systematic Review and Meta-analysis. α -硫辛酸治疗糖尿病的疗效:系统回顾和荟萃分析。

IF 1.6

Iranian Journal of Pharmaceutical Research : IJPR Pub Date : 2019-01-01 DOI: 10.22037/ijpr.2019.1100842

Mahmoud Ahmed Ebada, Notila Fayed, Laila Fayed, Souad Alkanj, Ahmed Abdelkarim, Haya Farwati, Aya Hanafy, Ahmed Negida, Mohamed Ebada, Yousef Noser

{"title":"Efficacy of Alpha-lipoic Acid in The Management of Diabetes Mellitus: A Systematic Review and Meta-analysis.","authors":"Mahmoud Ahmed Ebada, Notila Fayed, Laila Fayed, Souad Alkanj, Ahmed Abdelkarim, Haya Farwati, Aya Hanafy, Ahmed Negida, Mohamed Ebada, Yousef Noser","doi":"10.22037/ijpr.2019.1100842","DOIUrl":"https://doi.org/10.22037/ijpr.2019.1100842","url":null,"abstract":"Alpha-lipoic acid (ALA) is a naturally-occurring compound that has shown promising antioxidant and anti-inflammatory effects in experimental and human studies. The aim of this study was to assess the efficacy of ALA in the management of patients with diabetes mellitus (DM). We searched Medline (via PubMed), EBSCO, Scopus, and Web of Science for relevant randomized controlled trials. Data on glycated hemoglobin (HbA1c), blood glucose levels, lipid profile components, HOMA, and glutathione peroxidase (GPx) were extracted and pooled as the standardized mean difference (SMD) in a random effect model meta-analysis using RevMan version 5.3. Ten studies (n = 553 patients) were included. In the term of HBA1C, the overall SMD did not favor either of the two groups (SMD = 0.01, 95% CI [-0.32,0.35]; p = 0.94) in uncomplicated T2DM patients. Moreover, there was no statistically significant difference between the two groups in terms of FBG (SMD = -0.06, 95% CI [-0.44,0.33]; p = 0.78), PPBG (SMD = 0.04, 95% CI [-0.27,0.34]; p = 0.82), HDL (SMD = -0.05, 95% CI [-0.35,0.25]; p = 0.75), LDL (SMD = -0.05, 95% CI [-0.33,0.23]; p = 0.75). In terms of GPx, ALA was superior to placebo (SMD = 0.43, 95% CI [0.07,0.8]; p = 0.02). Our analysis showed that ALA was not superior to placebo in terms of HBA1C, LDL, HDL, TC, TG reduction in uncomplicated T2DM. However, in terms of GPx, ALA was significantly superior to the placebo. Further studies with larger sample sizes should investigate different doses of ALA in DM patients.","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"2144-2156"},"PeriodicalIF":1.6,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7059057/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37747090","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 15

MDMA Abuse in Relation to MicroRNA Variation in Human Brain Ventral Tegmental Area and Nucleus Accumbens. MDMA滥用与人脑腹侧被盖区和伏隔核MicroRNA变异的关系。

IF 1.6

Iranian Journal of Pharmaceutical Research : IJPR Pub Date : 2019-01-01 DOI: 10.22037/ijpr.2019.15097.12874

Goksun Demirel, Esra Guzel, Chad J Creighton, Yeter Erol Ozturk, Ceyhun Kucuk, Hızır Asliyuksek, Türkan Yurdun

{"title":"MDMA Abuse in Relation to MicroRNA Variation in Human Brain Ventral Tegmental Area and Nucleus Accumbens.","authors":"Goksun Demirel, Esra Guzel, Chad J Creighton, Yeter Erol Ozturk, Ceyhun Kucuk, Hızır Asliyuksek, Türkan Yurdun","doi":"10.22037/ijpr.2019.15097.12874","DOIUrl":"https://doi.org/10.22037/ijpr.2019.15097.12874","url":null,"abstract":"3,4-methylenedioxymethamphetamine (MDMA) is one of the most widespread illegal drugs, that have been used particularly by young people in the 15-34 age group. MicroRNAs (miRNAs) are endogenously synthesized, non-coding, and small RNAs that post-transcriptionally regulate their target genes' expression by inhibiting protein translation or degradation. miRNAs are increasingly implicated in drug-related gene expressions and functions. Notably, there are no reports of miRNA variation in the human brain in MDMA abuse. We here present a miRNA profiling study - the first such study, to the best of our knowledge - into the post-mortem human brains of a sample of people with MDMA abuse, along with non-drug dependent controls. The miRNA profiling of nucleus accumbens (NAc) and ventral tegmental areas (VTA) was performed by microarray analysis. Subsequently, two candidate miRNA putative biomarkers were selected according to significant regional differential expression (miR-1202 and miR-7975), using quantitative reverse-transcription PCR (qRT-PCR). We showed that the expression level of miR-7975 was significantly lower in the VTA regions of the 30 MDMA users, as compared with the 30 control samples. Another significantly deregulated miR-1202 was down-regulated in the NAc regions of 30 MDMA samples in comparison to the control samples. Alteration of these miRNAs can potentially serve as novel biomarkers for MDMA abuse, and warrant further research in independent and larger samples of patients.","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"1989-1999"},"PeriodicalIF":1.6,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7059052/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37747741","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 4

Effect of Topiramate on Morphine-induced Conditioned Place Preference (CPP) in Rats: Role of ERK and CREB Proteins in Hippocampus and Cerebral Cortex. 托吡酯对吗啡诱导的大鼠条件位置偏好(CPP)的影响:海马和大脑皮层ERK和CREB蛋白的作用。

IF 1.6

Iranian Journal of Pharmaceutical Research : IJPR Pub Date : 2019-01-01 DOI: 10.22037/ijpr.2019.1100873

Nima Bagherpasand, Soghra Mehri, Mahdieh Jafari Shahroudi, Seyed Meghdad Tabatabai, Ali Khezri, Mohammad Fathi, Khalil Abnous, Mohsen Imenshahidi, Hossein Hosseinzadeh

{"title":"Effect of Topiramate on Morphine-induced Conditioned Place Preference (CPP) in Rats: Role of ERK and CREB Proteins in Hippocampus and Cerebral Cortex.","authors":"Nima Bagherpasand, Soghra Mehri, Mahdieh Jafari Shahroudi, Seyed Meghdad Tabatabai, Ali Khezri, Mohammad Fathi, Khalil Abnous, Mohsen Imenshahidi, Hossein Hosseinzadeh","doi":"10.22037/ijpr.2019.1100873","DOIUrl":"https://doi.org/10.22037/ijpr.2019.1100873","url":null,"abstract":"In this study, the effect of topiramate, as an antiepileptic drug, was evaluated on morphine craving in rats. The conditioned place preference (CPP) test was used for this purpose. Repeated administration of morphine (10 mg/kg, i.p. for 4 days) induced significant CPP. Administration of topiramate (50 and 100 mg/kg, i.p. for 4 days) with each morphine administration decreased the acquisition of morphine-induced CPP. At the next step, the levels of extracellular signal-regulated kinase (ERK), p-ERK, cAMP responsive element binding (CREB), and p-CREB proteins were evaluated in hippocampus and cerebral cortex using western blot analysis. Following the repeated administration of morphine, the level of p-ERK protein markedly enhanced in both tissues, while topiramate could significantly reduce the phosphorylation of ERK in these brain regions. Additionally, the level of CREB and p-CREB proteins did not change in different groups. Memantine as a positive control reduced the acquisition of morphine-induced CPP. Also, memantine significantly decreased the level of p-ERK protein in hippocampus and cerebral cortex. These results demonstrated that topiramate can attenuate the acquisition of morphine-induced CPP in rats. This effect in part can be mediated through down regulation of p-ERK protein in hippocampus and cerebral cortex.","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"2000-2010"},"PeriodicalIF":1.6,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7059042/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37747742","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 4

Effects of Baneh (Pistacia atlantica) Gum on Human Breast Cancer Cell Line (MCF-7) and Its Interaction with Anticancer Drug Doxorubicin. 桐树树胶对人乳腺癌细胞系MCF-7的影响及其与抗癌药物阿霉素的相互作用。

IF 1.6

Iranian Journal of Pharmaceutical Research : IJPR Pub Date : 2019-01-01 DOI: 10.22037/ijpr.2019.1100853

Hamzeh Pasban-Aliabadi, Vahid Sobhani, Saeed Esmaeili-Mahani, Hamid Najafipour, Alireza Askari, Hamidreza Jalalian

{"title":"Effects of Baneh (Pistacia atlantica) Gum on Human Breast Cancer Cell Line (MCF-7) and Its Interaction with Anticancer Drug Doxorubicin.","authors":"Hamzeh Pasban-Aliabadi, Vahid Sobhani, Saeed Esmaeili-Mahani, Hamid Najafipour, Alireza Askari, Hamidreza Jalalian","doi":"10.22037/ijpr.2019.1100853","DOIUrl":"https://doi.org/10.22037/ijpr.2019.1100853","url":null,"abstract":"Pistacia atlantica is one of the species of Anacardiaceae that grows in the wild in different regions of Iran. Traditionally, anacardiaceae family has antibacterial, fungicidal, and cytotoxic properties. Therefore, the present study was designed to investigate the possible cytotoxic and anti-proliferative properties of Baneh gum. Cytotoxicity of the plant gum was determined using MTT assay on MCF-7 human breast cancer cells. The cellular makers of apoptosis (caspase3 and P53) and cell proliferation (Cyclin-D1) were evaluated by western blotting. Doxorubicin was used as anticancer control drug in combination treatment. The result showed that Baneh gum (100 µg/mL) significantly induced cell damage, activated caspase3, and increased P53 protein level. In addition, Cyclin-D1 was significantly decreased in gum-incubated cells. Furthermore, combination treatment of cells with Baneh gum (25 µg/mL) and doxorubicin (200 nM) produced a significant cytotoxic effect as compared to each drug alone. In conclusion, Baneh gum (100 µg/mL) has a potential pro-apoptotic/anti-proliferative property against human breast cancer cells and its combination with doxorubicin in low doses may induce cell death effectively and be a potent modality to treat this type of cancer.","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"1959-1966"},"PeriodicalIF":1.6,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7059076/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37747284","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 6

Dynamic Thinking Approach of Non-medical Use of Pharmaceutical Opioids. 阿片类药物非医疗使用的动态思维方法。

IF 1.6

Iranian Journal of Pharmaceutical Research : IJPR Pub Date : 2019-01-01 DOI: 10.22037/ijpr.2019.1100886

Farahnaz Zeinali, Ali Rajabzadeh Ghatari, Mehdi Mohammadzadeh, Fatemeh Mojibian

{"title":"Dynamic Thinking Approach of Non-medical Use of Pharmaceutical Opioids.","authors":"Farahnaz Zeinali, Ali Rajabzadeh Ghatari, Mehdi Mohammadzadeh, Fatemeh Mojibian","doi":"10.22037/ijpr.2019.1100886","DOIUrl":"https://doi.org/10.22037/ijpr.2019.1100886","url":null,"abstract":"Unsteady increase in using pharmaceutical opioids is a phenomenon that has existed in human societies for a long time. Furthermore, the ever-growing trend of addiction to opioids affects communities in various economic, social, and cultural aspects. Since abusing pharmaceutical opioids is a complex dynamic problem, it is extremely difficult to recognize the factors influencing this abuse. Thus, applying such dynamic models as system dynamics (SD) plays an important role in addressing these complex dynamic problems. System dynamics model falls in two categories of qualitative and quantitative system dynamics. In this paper, causal loop diagrams (CLDs), which are conceptual qualitative stages were applied, and variables were elicited from literatures; then, the initial CLDs were generated, and afterward, some experts were interviewed in order for the CLDs model to be evaluated. Ultimately, a meeting was held for discussing the variables and validating the diagrams. In this study, variables are connected by causal relationships called reinforcing and balancing. Then, the CLD model clearly depicted how the variables interact with one another indifferent stages of the process. The CLDs model is a fundamental issue in developing quantitative system dynamic, assisting policymakers in forecasting the process of non-medical use of pharmaceutical opioids and finding some measures to reduce their usage.","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"2216-2225"},"PeriodicalIF":1.6,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7059054/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37747543","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Myelin Protection by Ursolic Acid in Cuprizone-Induced Demyelination in Mice. 熊果酸对铜酮诱导小鼠脱髓鞘的保护作用。

IF 1.6

Iranian Journal of Pharmaceutical Research : IJPR Pub Date : 2019-01-01 DOI: 10.22037/ijpr.2019.112181.13582

Fatemeh Honarvar, Vida Hojati, Nuredin Bakhtiari, Gholamhassan Vaezi, Mohammad Javan

{"title":"Myelin Protection by Ursolic Acid in Cuprizone-Induced Demyelination in Mice.","authors":"Fatemeh Honarvar, Vida Hojati, Nuredin Bakhtiari, Gholamhassan Vaezi, Mohammad Javan","doi":"10.22037/ijpr.2019.112181.13582","DOIUrl":"https://doi.org/10.22037/ijpr.2019.112181.13582","url":null,"abstract":"Neuronal survival in multiple sclerosis (MS) and other demyelinating diseases depends on the preservation of myelin and remyelination of axons. Myelin protection is the main purpose to decrease myelin damage in the central nervous system (CNS). Ursolic acid (UA) as a natural product in apple is suggested to protect neural cells. This study is the first to demonstrate an effect for UA on CNS myelin loss induced by cuprizone toxin. In the current study, we hypothesized that daily treatment with UA in drinking water (1 mg/mL) prevents myelin damage by 6 weeks administration of CPZ in mice pellet which lead to corpus callosum axonal demyelination. We assessed the myelin content and the number of myelinating cells in corpus callosum by FluoroMyelin and luxol fast blue staining as well as by immunostaining against MBP and Olig2. Our finding indicated that UA could decrease the extent of demyelination area and enhanced myelin stain intensity within CC and protected oligodendrocyte lineage cells against cuprizone toxin. We could conclude that myelinated structures could be protected by UA in corpus callosum, which provide favorable evidence for the possibility of application of UA in demyelinating diseases and traumatic injuries.","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"1978-1988"},"PeriodicalIF":1.6,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7059067/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37747740","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 9

Lipid Nanocapsules for Imatinib Delivery: Design, Optimization and Evaluation of Anticancer Activity Against Melanoma Cell Line. 用于伊马替尼输送的脂质纳米胶囊:设计、优化和对黑色素瘤细胞系抗癌活性的评估。

IF 1.6

Iranian Journal of Pharmaceutical Research : IJPR Pub Date : 2019-01-01 DOI: 10.22037/ijpr.2019.1100870

Mohammad Reza Molaahmadi, Jaleh Varshosaz, Somayeh Taymouri, Vajihe Akbari

{"title":"Lipid Nanocapsules for Imatinib Delivery: Design, Optimization and Evaluation of Anticancer Activity Against Melanoma Cell Line.","authors":"Mohammad Reza Molaahmadi, Jaleh Varshosaz, Somayeh Taymouri, Vajihe Akbari","doi":"10.22037/ijpr.2019.1100870","DOIUrl":"https://doi.org/10.22037/ijpr.2019.1100870","url":null,"abstract":"Lipid nanocapsules (LNCs) represent a stable, biocompatible and worthwhile drug delivery system, demonstrating significant potential as gene/drug delivery platforms for cancer therapy. Imatinib, a potent tyrosine kinase inhibitor, has revolutionized the therapy of malignancies resulting from abnormal tyrosine kinase activity. However, its Clinical effectiveness in cancer treatment is hampered by its off-target side effects. In this study, we have investigated the potential benefits of LNCs as a novel drug delivery vehicle for imatinib with a view to improve drug efficacy. LNC formulations were prepared by phase-inversion temperature method and the effects of various formulation variables were assessed using full factorial design. The cytotoxicity and cellular uptake of optimized formulation were investigated against B16F10 melanoma cell line. Analysis of result by Design-Expert® software indicated that Solutol HS15 percent was the most effective parameter on the encapsulation efficiency, particle size, zeta potential, and release efficiency of LNCs. The optimized formulation revealed a particle size of 38.96 ± 0.84 nm, encapsulation efficiency of 99.17 ± 0.086%, zeta potential of -21.5 ± 0.61 mV, release efficiency of 60.03 ± 4.29, and polydispersity index of 0.24 ± 0.02. The imatinib loaded LNCs showed no hemolysis activity. Fluorescent microscopy test showed that the cellular uptake of LNCs was time dependent and density of fluorescent signals increased with time in cells. The in-vitro cytotoxicity study indicated that imatinib kept its pharmacological activity when loaded into LNCs. These results introduced imatinib loaded LNCs as a promising candidate for further investigation in cancer therapy.","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"1676-1693"},"PeriodicalIF":1.6,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7059069/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37748369","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 6