The Turkish Journal of Pharmaceutical Sciences最新文献

{"title":"Anti-Angiogenic activity of flunarizine by in ovo, in vitro and in vivo assays.","authors":"Chandana Kamili, Ravishankar Kakaraparthy, U. M. Vattikuti","doi":"10.4274/tjps.29981","DOIUrl":"https://doi.org/10.4274/tjps.29981","url":null,"abstract":"Background and Objective: The involvement of T-type calcium channels in cell proliferation and the role of sodium channels in cell migration have been extensively studied in angiogenesis. In the present study Flunarizine, a dual sodium /calcium channel blocker; was selected to evaluate its anti-angiogenic potential. This can be therapeutically beneficial in the diseases caused due to pathologically excess angiogenesis. Methods: The anti-angiogenic activity of ion channel blocker was screened by chick chorioallantoic membrane assay (in ovo), rat aortic ring assay,endothelial cell proliferation assay,transwell migration assay, matrigel cord-like morphogenesis assay (in vitro) and sponge implantation method (in vivo). The anti-angiogenic activity of the test drug was compared with the standard anti-angiogenic drug Bevacizumab and in addition, the test responses were compared with the angiogenic factor VEGF, at a maximal concentration of 500pM. Results: All the groups were compared with the control group using one-way ANOVA, followed by post hoc test, the Dunnett’s test to compare the mean of all the groups with the control mean.In the chick chorioallantoic membrane assay, number of branching points and angiogenic score were evaluated and significant results were observed at 10-5M and 10-4M. In the aortic ring assay reduction in the area of sprouts were observed with 5-10μM and a significant reduction in weight of sponges, number of blood vessels formed and hemoglobin content were observed at all the three tested concentrations of Flunarizine in the sponge implantation method. In the studies on human umbilical vein endothelial cellsthe test drug (1-100nM) showed significant inhibition of proliferation, migration and decrease in network length of cord like tubes in a dose dependent manner. Conclusions: Flunarizine has significant anti-angiogenic action byinhibiting the cell proliferation, migration and cord like tube formation, which have resulted by blocking the T-type u co rre cte d p r o f calcium and sodium channels. Further studies on the structural modifications of Flunarizinefor repurposing this ion channel modulator will be able to treat the diseases due to excess angiogenesis from the root cause.","PeriodicalId":193717,"journal":{"name":"The Turkish Journal of Pharmaceutical Sciences","volume":"5 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2018-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"127294449","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}

{"title":"Palmitic Acid-Pluronic F127-Palmitic Acid Penta-Block Copolymer as a Novel Nanocarrier for Oral Delivery of Glipizide","authors":"Vipan Kumar Kamboj, Prabhakar Kumar Verma","doi":"10.4274/tjps.20082","DOIUrl":"https://doi.org/10.4274/tjps.20082","url":null,"abstract":"Objective: The aim of the present study is to develop nanotechnology-based oral formulations of Glipizide to enhance bioavailability and to eliminate the frequent oral administration of the conventional dosage form. Glipizide is an antidiabetic drug with short biological half-life with limited oral bioavailability. Noval Palmitic acid-Pluronic F127-Palmitic acid (PAF127) pentablock copolymer based prolonged release glipizide nanoparticles (GN) were prepared and screened for in vitro and in vivo studies. Methods: GN was prepared using novel PA-F127 pentablock copolymer by solvent evaporation technique. The prepared nanoparticles were evaluated for particle size, polydispersity index (PDI), zeta potential, entrapment efficiency, percentage yield, drug excipient compatibility using FTIR and DSC analysis, XRD, SEM, In vitro drug release studies, stability studies and in vivo pharmacokinetic studies. Results: The results of FTIR and DSC analysis revealed the absence of drug-excipient interactions. The optimized GN1 has particle size 242.60 ± 4.20 nm, PDI 0.171 ± 0.014 and zeta potential -21.41 ± 0.462 mV. Prepared nanoparticles were spherical in shape and showed semi-amorphous characteristics. In vitro release studies showed 34.43 ± 4.8 % drug was released in first 8 h, 56.11 ± 4.12 % glipizide were released further for 24 h. The GN1 was found to be stable at 5 ± 3 oC up to three months. Pharmacokinetic studies showed that the orally administered GN1 were superior with Cmax 2.35 fold, tmax 1.6 fold, area under the curve (AUC0→∞) 3.3 fold and mean residence time (MRT) 1.2 fold as compared to pure glipizide (p < 0.05). Conclusion: The study concluded that the bioavailability of newly developed GN1 was successfully prolonged and frequent oral administration problem with conventional dosage form can be defeated for diabetes treatment.","PeriodicalId":193717,"journal":{"name":"The Turkish Journal of Pharmaceutical Sciences","volume":"4 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2018-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"114864288","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}

{"title":"Electroanalytical Determination of Antiinflammatory Drug Tenoxicam in Pharmaceutical Dosage Forms","authors":"F. Ağın, Sena Atal","doi":"10.4274/tjps.60783","DOIUrl":"https://doi.org/10.4274/tjps.60783","url":null,"abstract":"","PeriodicalId":193717,"journal":{"name":"The Turkish Journal of Pharmaceutical Sciences","volume":"5 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2018-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"130349036","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}

{"title":"Evaluation of the Anti-inflammatory and Antioxidant Parameters of Aqueous and Ethanolic Extracts of Roman chamomile in mice","authors":"H. Erjaee, H. Rajaian, S. Nazifi","doi":"10.4274/tjps.51423","DOIUrl":"https://doi.org/10.4274/tjps.51423","url":null,"abstract":"","PeriodicalId":193717,"journal":{"name":"The Turkish Journal of Pharmaceutical Sciences","volume":"11 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2018-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"131058730","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}

{"title":"Optimization Of Thiazolidone Scaffolds Using Pocket Modelling For Development Of Potential Secretary System Inhibitors of Mycobacterium Tuberculosis","authors":"P. Choudhari, Shivaratna V Khare, S. P. Phalle, Santosh S. Kumbhar, Sambhaji R Masal, Rakesh P. Dhavale, D. Bhagwat, Atual M Kadam, Sujata P Choudahri","doi":"10.4274/tjps.12599","DOIUrl":"https://doi.org/10.4274/tjps.12599","url":null,"abstract":"","PeriodicalId":193717,"journal":{"name":"The Turkish Journal of Pharmaceutical Sciences","volume":"1 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2018-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"131749303","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}

{"title":"Investigation of antioxidant, α-glucosidase inhibitory, anti-inflammatory and DNA protective properties of Vaccinium arctostaphylos L.","authors":"Burak Barut, Elif Nur Barut, Seçkin Engin, Arzu Özel, Feride Sena Sezen","doi":"10.4274/tjps.28247","DOIUrl":"https://doi.org/10.4274/tjps.28247","url":null,"abstract":"","PeriodicalId":193717,"journal":{"name":"The Turkish Journal of Pharmaceutical Sciences","volume":"19 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2018-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"133028734","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}

{"title":"Simultaneous estimation of saxagliptin and dapagliflozin in human plasma by validated HPLC-UV method","authors":"Sharmila Donepudi, S. Achanta","doi":"10.4274/tjps.46547","DOIUrl":"https://doi.org/10.4274/tjps.46547","url":null,"abstract":"Objective: The fixed dose combination of saxagliptin and dapagliflozin, recently approved antidiabetic medication. It is marketed with a brand name Qtern. The intend method aim to develop a simple, rapid, sensitive and validated isocratic reversed phase high performance liquid chromatography (RP-HPLC) method for the simultaneous estimation of saxagliptin and dapagliflozin in human plasma by using linagliptin as internal standard as per US-FDA guidelines. Materials and methods: The method was performed on Waters 2695 HPLC equipped with quaternary pump. The analyte separation was achieved using Eclipse XDB C18 (150×4.6μ×5mm) column with a mobile phase consisting of 0.1% ortho phosphoric acid and acetonitrile (50:50) with pH adjusted to 5.0 at1ml/min flow rate. Results: The analyte was detected at 254nm. Retention time of the internal standard, saxagliptin and dapagliflozin was found at 2.746, 5.173 and 7.218minutes, respectively. The peaks were found to be free of interference. The method is validated over a dynamic linear range of 0.01 to 0.5μg/ml and 0.05 to 2μg/ml for saxagliptin and dapagliflozin, respectively, with a correlation coefficient of 0.998. The precision and accuracy of samples of six replicate measurements at LLOQ level was within limit. The analytes were found to be stable in human plasma at -28°C for 37 days. Conclusion: The stability, sensitivity, specificity and reproducibility of this method make it appropriate for the determination of saxagliptin and dapagliflozin in human plasma.","PeriodicalId":193717,"journal":{"name":"The Turkish Journal of Pharmaceutical Sciences","volume":"14 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2018-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"127965489","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}