首页 > 最新文献

International Journal of Drug Delivery最新文献

英文 中文
Formulation And In Vitro/In Vivo Evaluation Of Olmesartan Medoxomil Solid Dispersions Incorporated E/R Trilayer Matrix Tablets By Geomatrix 奥美沙坦美多沙米固体分散体含E/R三层基质片的制备及体外/体内评价
Pub Date : 2017-02-28 DOI: 10.5138/09750215.1948
M. Balakrishnaiah, V. Gupta
An attempt has been made to develop and optimize an novel anti hypertensive trilayered controlled release matrix tablets incorporated with Olmesartan medoxomil solid dispersion prepared by direct compression and consisted of middle active layer with different grades of hydroxypropylmethylcellulose (HPMC), guar gum, ethyl cellulose. Upper and lower layers are prepared with Carnauba wax, guar gum and sodium CMC. The developed drug delivery system provided prolonged drug release rates over a period of 24 h. The release profile of the optimized formulation (HF14) was described by the Zero-order and Higuchi model. In-vivo bioavailability studies were carried out with the optimized formulation (HF14) and reference standard A fair correlation between the dissolution profile and bioavailability for the optimized formulation was observed. The results indicate that the approach used could lead to a successful development of a trilayer extended release formulation up to 24h. These results also demonstrated that the Olmesartan solid dispersion incorporated trilayer tablets shown more bioavailability because of its conversion from crystalline to amorphous form.
采用直接压缩法制备了由不同等级羟丙基甲基纤维素(HPMC)、瓜尔胶、乙基纤维素组成中间活性层的奥美沙坦-美多索米固体分散体,制备并优化了新型抗高血压三层控释片。上下两层由巴西棕榈蜡、瓜尔胶和CMC钠配制而成。该给药系统具有24 h的缓释时间。优化后的配方(HF14)的释放曲线采用零阶和Higuchi模型描述。采用优化后的配方(HF14)和参比标准进行体内生物利用度研究,发现其溶出度与生物利用度之间存在良好的相关性。结果表明,所采用的方法可以成功地开发出长达24小时的三层缓释制剂。这些结果还表明,奥美沙坦固体分散体含有三层片剂,由于其从晶体到无定形的转化,具有更高的生物利用度。
{"title":"Formulation And In Vitro/In Vivo Evaluation Of Olmesartan Medoxomil Solid Dispersions Incorporated E/R Trilayer Matrix Tablets By Geomatrix","authors":"M. Balakrishnaiah, V. Gupta","doi":"10.5138/09750215.1948","DOIUrl":"https://doi.org/10.5138/09750215.1948","url":null,"abstract":"An attempt has been made to develop and optimize an novel anti hypertensive trilayered controlled release matrix tablets incorporated with Olmesartan medoxomil solid dispersion prepared by direct compression and consisted of middle active layer with different grades of hydroxypropylmethylcellulose (HPMC), guar gum, ethyl cellulose. Upper and lower layers are prepared with Carnauba wax, guar gum and sodium CMC. The developed drug delivery system provided prolonged drug release rates over a period of 24 h. The release profile of the optimized formulation (HF14) was described by the Zero-order and Higuchi model. In-vivo bioavailability studies were carried out with the optimized formulation (HF14) and reference standard A fair correlation between the dissolution profile and bioavailability for the optimized formulation was observed. The results indicate that the approach used could lead to a successful development of a trilayer extended release formulation up to 24h. These results also demonstrated that the Olmesartan solid dispersion incorporated trilayer tablets shown more bioavailability because of its conversion from crystalline to amorphous form.","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-02-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87221854","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Structural designing of suppressors for autisms spectrum diseases using molecular dynamics sketch 基于分子动力学草图的自闭症谱系疾病抑制因子结构设计
Pub Date : 2017-02-28 DOI: 10.5138/09750215.1973
Bipin Nair, V. Bhaskaran, K. Arunjit
In this paper we are sketching the chemical structure of suppressor drug for autism spectrum disorder using a computational tool. Here we are designing three molecular compounds like Fluoxetine, Risperidone, Melatonin. Structuring the suppressors, sketching the aromatization and bonding of the functional groups with the elements like Oxygen, Nitrogen, halogens. In our work we are using computational algorithm for drawing the structure of suppressor drug. In this paper we are mentioning the autism spectrum suppressor’s molecular formula as well as structural formula.
在本文中,我们使用计算工具绘制了自闭症谱系障碍抑制药物的化学结构。我们正在设计三种分子化合物,比如氟西汀,利培酮,褪黑素。构造抑素,勾勒出官能团与氧、氮、卤素等元素的芳构化和成键。在我们的工作中,我们使用计算算法来绘制抑制药物的结构。本文介绍了自闭症谱系抑制因子的分子式和结构式。
{"title":"Structural designing of suppressors for autisms spectrum diseases using molecular dynamics sketch","authors":"Bipin Nair, V. Bhaskaran, K. Arunjit","doi":"10.5138/09750215.1973","DOIUrl":"https://doi.org/10.5138/09750215.1973","url":null,"abstract":"In this paper we are sketching the chemical structure of suppressor drug for autism spectrum disorder using a computational tool. Here we are designing three molecular compounds like Fluoxetine, Risperidone, Melatonin. Structuring the suppressors, sketching the aromatization and bonding of the functional groups with the elements like Oxygen, Nitrogen, halogens. In our work we are using computational algorithm for drawing the structure of suppressor drug. In this paper we are mentioning the autism spectrum suppressor’s molecular formula as well as structural formula.","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-02-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82022112","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 2
EPR effect based nanocarriers targeting for treatment of cancer 基于EPR效应的纳米载体靶向治疗癌症
Pub Date : 2017-02-28 DOI: 10.5138/09750215.1974
K. R. Gajbhiye, J. Gajbhiye
The enhanced permeability and retention (EPR) effect is a unique phenomenon of solid tumors related to their anatomical and pathophysiological differences from normal tissues. In solid tumors, angiogenesis leads to high vascular density. Large gaps exist between endothelial cells in tumor blood vessels, which lead to selective extravasations and retention of macromolecular drugs. This EPR effect served as a basis for development of macromolecular anticancer therapy. There are various factors, which lead to a significantly increased EPR effect and enhanced antitumor drug effects as well. This review discusses the unique anatomy of tumor vessels, molecular mechanisms of factors related to the EPR effect and the role of the EPR effect in the intratumoral delivery of protein and peptide drugs, macromolecular drugs and drug-loaded long-circulating nanocarriers.
增强渗透性和滞留性(EPR)效应是实体瘤的独特现象,与实体瘤与正常组织的解剖和病理生理差异有关。在实体瘤中,血管生成导致高血管密度。肿瘤血管内皮细胞之间存在较大间隙,导致大分子药物选择性外渗和滞留。这种EPR效应为大分子抗癌治疗的发展奠定了基础。多种因素导致EPR效应显著增强,抗肿瘤药物作用增强。本文综述了肿瘤血管的独特解剖结构、EPR效应相关因素的分子机制以及EPR效应在肿瘤内传递蛋白质和多肽药物、大分子药物和载药长循环纳米载体中的作用。
{"title":"EPR effect based nanocarriers targeting for treatment of cancer","authors":"K. R. Gajbhiye, J. Gajbhiye","doi":"10.5138/09750215.1974","DOIUrl":"https://doi.org/10.5138/09750215.1974","url":null,"abstract":"The enhanced permeability and retention (EPR) effect is a unique phenomenon of solid tumors related to their anatomical and pathophysiological differences from normal tissues. In solid tumors, angiogenesis leads to high vascular density. Large gaps exist between endothelial cells in tumor blood vessels, which lead to selective extravasations and retention of macromolecular drugs. This EPR effect served as a basis for development of macromolecular anticancer therapy. There are various factors, which lead to a significantly increased EPR effect and enhanced antitumor drug effects as well. This review discusses the unique anatomy of tumor vessels, molecular mechanisms of factors related to the EPR effect and the role of the EPR effect in the intratumoral delivery of protein and peptide drugs, macromolecular drugs and drug-loaded long-circulating nanocarriers.","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-02-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90393504","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 5
Development and validation of analytical methods for the simultaneous estimation of Nimorazole and Ofloxacin in tablet dosage form 片剂中尼莫唑和氧氟沙星含量同时测定方法的建立与验证
Pub Date : 2016-12-08 DOI: 10.5138/09750215.1792
A. Ghugare, L. Devhare, B. Hatwar
Two simple, rapid, accurate and precise spectrophotometric methods have been developed for simultaneous estimation of Nimorazole and Ofloxacin from tablet dosage form. Method І involves formation of ‘simultaneous equations’ at 304 nm (λ max of Nimorazole) and 287.5 nm (λ max of Ofloxacin); while Method ІІ involves, formation of ‘Absorbance ratio equation’ at 301(isoabsorptive point) and 287.5 nm (λ max of Ofloxacin) using distilled water as a solvent. The linearity was observed in the concentration range of 5 - 25 μg/ml for Nimorazole and 2 - 10 μg/ml for Ofloxacin. The results of analysis have been validated statistically and by recovery studies and were found satisfactory.
建立了两种简便、快速、准确、精密的分光光度法同时测定片剂剂型中尼莫唑和氧氟沙星含量的方法。І方法涉及在304 nm(尼莫唑λ max)和287.5 nm(氧氟沙星λ max)处形成“联立方程”;方法ІІ使用蒸馏水作为溶剂,在301(等吸收点)和287.5 nm(氧氟沙星λ max)处形成“吸光度比方程”。尼莫唑在5 ~ 25 μg/ml、氧氟沙星在2 ~ 10 μg/ml浓度范围内呈线性关系。分析结果经统计和回收率研究验证,结果令人满意。
{"title":"Development and validation of analytical methods for the simultaneous estimation of Nimorazole and Ofloxacin in tablet dosage form","authors":"A. Ghugare, L. Devhare, B. Hatwar","doi":"10.5138/09750215.1792","DOIUrl":"https://doi.org/10.5138/09750215.1792","url":null,"abstract":"Two simple, rapid, accurate and precise spectrophotometric methods have been developed for simultaneous estimation of Nimorazole and Ofloxacin from tablet dosage form. Method І involves formation of ‘simultaneous equations’ at 304 nm (λ max of Nimorazole) and 287.5 nm (λ max of Ofloxacin); while Method ІІ involves, formation of ‘Absorbance ratio equation’ at 301(isoabsorptive point) and 287.5 nm (λ max of Ofloxacin) using distilled water as a solvent. The linearity was observed in the concentration range of 5 - 25 μg/ml for Nimorazole and 2 - 10 μg/ml for Ofloxacin. The results of analysis have been validated statistically and by recovery studies and were found satisfactory.","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2016-12-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78762623","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
Enhancement of Solubility of Artemisinin and Curcumin by Co-Solvency Approach for Application in Parenteral Drug Delivery System 用共溶度法提高青蒿素和姜黄素在静脉给药系统中的溶解度
Pub Date : 2016-12-08 DOI: 10.5138/09750215.1868
V. Thakkar, R. Dhankecha, M. Gohel, P. Shah, T. Pandya, T. Gandhi
The aim of present study was to enhance solubility of poorly soluble antimalarial drugs, Artemisinin and Curcumin by adopting  Co-solvency approach and to develop parenteral aqueous injectable solution. Solubility enhancement of both drugs was achieved using co-solvency approach. The parenteral injection was prepared by using a ternary co-solvent system which comprised of benzyl alcohol, PEG 400 and tween 80 (as surfactant). Solubility of Artemisinin and Curcumin was found to be higher in benzyl alcohol and PEG 400. Co-solvent system comprising of  benzyl alcohol, PEG 400 and tween 80 in volume fraction of 0.3, 0.9 and 0.2 respectively showed the minimum required solubility of Artemisinin (90 mg per ml) and Curcumin (180 mg per ml). The parenteral injectable formulation was characterized for pH, clarity, viscosity, osmolarity and sterility and the stated parameters were found in acceptable range.  In-vitro erythrocyte toxicity study showed that intravenous administration of optimized formulation will be safe. In-vitro antimalarial assay indicated that efficacy of artemisinin and curcumin parenteral formulation was greater than quinine and combination of Artemether and Lumefantrine. Stability study of the optimized batch showed no change in physical and chemical characteristics. Based on study, one can conclude that Artemisinin and Curcumin can be successfully formulated as parenteral injectable formulation by co-solvency approach for the effective treatment of malarial infection
本研究旨在采用共溶性方法提高难溶性抗疟药物青蒿素和姜黄素的溶解度,并开发非肠外注射水溶液。两种药物的溶解度增强是通过共溶性方法实现的。采用以苯甲醇、peg400和吐温80为表面活性剂的三元共溶剂体系制备了肠外注射剂。青蒿素和姜黄素在苯甲醇和peg400中的溶解度较高。由苯甲醇、peg400和吐温80组成的共溶剂体系,其体积分数分别为0.3、0.9和0.2,表明青蒿素(90 mg / ml)和姜黄素(180 mg / ml)的最小溶解度要求。对该制剂的pH值、清晰度、粘度、渗透压和无菌性进行了表征,所述参数在可接受范围内。体外红细胞毒性研究表明,优化后的配方静脉给药是安全的。体外抗疟试验表明,青蒿素姜黄素肠外制剂的抗疟效果优于奎宁和蒿甲醚与甲苯胺联合用药。稳定性研究表明,优化后的批料的理化特性没有变化。研究表明,青蒿素和姜黄素可通过共偿付方法配制成有效治疗疟疾感染的肠外注射制剂
{"title":"Enhancement of Solubility of Artemisinin and Curcumin by Co-Solvency Approach for Application in Parenteral Drug Delivery System","authors":"V. Thakkar, R. Dhankecha, M. Gohel, P. Shah, T. Pandya, T. Gandhi","doi":"10.5138/09750215.1868","DOIUrl":"https://doi.org/10.5138/09750215.1868","url":null,"abstract":"The aim of present study was to enhance solubility of poorly soluble antimalarial drugs, Artemisinin and Curcumin by adopting  Co-solvency approach and to develop parenteral aqueous injectable solution. Solubility enhancement of both drugs was achieved using co-solvency approach. The parenteral injection was prepared by using a ternary co-solvent system which comprised of benzyl alcohol, PEG 400 and tween 80 (as surfactant). Solubility of Artemisinin and Curcumin was found to be higher in benzyl alcohol and PEG 400. Co-solvent system comprising of  benzyl alcohol, PEG 400 and tween 80 in volume fraction of 0.3, 0.9 and 0.2 respectively showed the minimum required solubility of Artemisinin (90 mg per ml) and Curcumin (180 mg per ml). The parenteral injectable formulation was characterized for pH, clarity, viscosity, osmolarity and sterility and the stated parameters were found in acceptable range.  In-vitro erythrocyte toxicity study showed that intravenous administration of optimized formulation will be safe. In-vitro antimalarial assay indicated that efficacy of artemisinin and curcumin parenteral formulation was greater than quinine and combination of Artemether and Lumefantrine. Stability study of the optimized batch showed no change in physical and chemical characteristics. Based on study, one can conclude that Artemisinin and Curcumin can be successfully formulated as parenteral injectable formulation by co-solvency approach for the effective treatment of malarial infection","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2016-12-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82128641","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 4
In Vitro - In Vivo Evaluation Of E/R Trilayer Matrix Tablets Containing Solid Dispersion Of Atorvastatin 含阿托伐他汀固体分散体的E/R三层基质片的体内外评价
Pub Date : 2016-12-08 DOI: 10.5138/09750215.1947
A. Thirupathaiah, R. Sunder
Investigation of  in vitro/in vivo  behaviour of extended release tablets containing solid dispersions of Atorvastatin is the focus of the present research work. Atorvastatin trilayer matrix tablets were prepared by direct compression method and consisted of middle active layer with different grades of hydroxypropylmethylcellulose (HPMC), ethyl cellulose and Carbopol 934P. Barrier layers are prepared with hydrophobic polymers carnauba wax and xanthan gum. Based on the evaluation parameters, drug dissolution profile and release order kinetics HF16 was found to be optimized formulation. The developed drug delivery system provided prolonged drug release rates over a period of 24 h. The release profile of the optimized formulation (HF16) was described by the Zero-order and best fitted to Higuchi model. FTIR confirmed that there was no chemical interaction between drug and excipients used in the formulation. . In vivo bioavailability studies were conducted for optimized formulation HF16 and reference standard. The optimized formulation of Atorvastatin trilayer matrix tablet was shown significant plasma concentration with extended release and maintained for 24 hrs with patient compliance by reducing the dosage frequency, when compared with reference standard.
研究阿托伐他汀固体分散体缓释片的体内外行为是本研究的重点。采用直接压缩法制备阿托伐他汀三层基质片,中间活性层由不同等级羟丙基甲基纤维素(HPMC)、乙基纤维素和卡波波尔934P组成。屏障层由疏水聚合物巴西棕榈蜡和黄原胶制备。根据评价参数,确定了最佳处方HF16的药物溶出曲线和释放顺序动力学。该给药体系在24 h内具有较长的释药速度。优化后的配方(HF16)的释药曲线为零阶,最符合Higuchi模型。FTIR证实制剂中所用辅料与药物之间无化学相互作用。对优化配方HF16和标准品进行体内生物利用度研究。与参比标准相比,优化后的阿托伐他汀三层基质片血药浓度显著,缓释时间延长,维持24小时,且患者依从性良好,降低给药频率。
{"title":"In Vitro - In Vivo Evaluation Of E/R Trilayer Matrix Tablets Containing Solid Dispersion Of Atorvastatin","authors":"A. Thirupathaiah, R. Sunder","doi":"10.5138/09750215.1947","DOIUrl":"https://doi.org/10.5138/09750215.1947","url":null,"abstract":"Investigation of  in vitro/in vivo  behaviour of extended release tablets containing solid dispersions of Atorvastatin is the focus of the present research work. Atorvastatin trilayer matrix tablets were prepared by direct compression method and consisted of middle active layer with different grades of hydroxypropylmethylcellulose (HPMC), ethyl cellulose and Carbopol 934P. Barrier layers are prepared with hydrophobic polymers carnauba wax and xanthan gum. Based on the evaluation parameters, drug dissolution profile and release order kinetics HF16 was found to be optimized formulation. The developed drug delivery system provided prolonged drug release rates over a period of 24 h. The release profile of the optimized formulation (HF16) was described by the Zero-order and best fitted to Higuchi model. FTIR confirmed that there was no chemical interaction between drug and excipients used in the formulation. . In vivo bioavailability studies were conducted for optimized formulation HF16 and reference standard. The optimized formulation of Atorvastatin trilayer matrix tablet was shown significant plasma concentration with extended release and maintained for 24 hrs with patient compliance by reducing the dosage frequency, when compared with reference standard.","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2016-12-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82353541","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Limonene and BEZ 235 inhibits growth of COLO-320 and HCT-116 colon cancer cells 柠檬烯和BEZ 235抑制结肠癌细胞COLO-320和HCT-116的生长
Pub Date : 2016-12-08 DOI: 10.5138/09750215.1919
Raja Ratna Reddy Yakkanti, P. C. Sekhar, K. Reddy, S. Ramamoorthy, S. Suresh, T. Lakshmi, M. Rajesh, C. Reddy
D-Limonene is a dietary monoterpene with significant anticancer activity against many cancer types in preclinical and clinical studies. The study is designed to investigate synergistic anticancer effects of limonene and BEZ235 combination in COLO-320 and HCT-116 colon cancer cells. Cells were treated with both the drugs alone and in combination and the effects on cell viability; cell migration and clonogenic potential were examined. Results show that both drugs exhibited dose and time dependant cytotoxicity on the cell lines tested. CompuSyn analysis of the drug combination effects revealed the strong synergistic interaction of the combination. Our results also indicate that COLO-320 cells were more sensitive for anticancer effects of the drugs than HCT-116 cells. The presence of Ras and PI3K mutations in HCT-116 cells could possibly be one of the main reasons for the observed outcome as compared to the wild type expressions of them in COLO-320 cells.
d -柠檬烯是一种膳食单萜,在临床前和临床研究中对多种癌症具有显著的抗癌活性。本研究旨在探讨柠檬烯和BEZ235联合使用对COLO-320和HCT-116结肠癌细胞的协同抗癌作用。观察单药和联合用药对细胞活力的影响;检测细胞迁移和克隆潜能。结果表明,两种药物均表现出剂量和时间依赖性的细胞毒性。药物联合效应的CompuSyn分析显示该组合具有较强的协同作用。结果还表明,COLO-320细胞对药物的抗癌作用比HCT-116细胞更敏感。与COLO-320细胞中的野生型表达相比,HCT-116细胞中Ras和PI3K突变的存在可能是观察到结果的主要原因之一。
{"title":"Limonene and BEZ 235 inhibits growth of COLO-320 and HCT-116 colon cancer cells","authors":"Raja Ratna Reddy Yakkanti, P. C. Sekhar, K. Reddy, S. Ramamoorthy, S. Suresh, T. Lakshmi, M. Rajesh, C. Reddy","doi":"10.5138/09750215.1919","DOIUrl":"https://doi.org/10.5138/09750215.1919","url":null,"abstract":"D-Limonene is a dietary monoterpene with significant anticancer activity against many cancer types in preclinical and clinical studies. The study is designed to investigate synergistic anticancer effects of limonene and BEZ235 combination in COLO-320 and HCT-116 colon cancer cells. Cells were treated with both the drugs alone and in combination and the effects on cell viability; cell migration and clonogenic potential were examined. Results show that both drugs exhibited dose and time dependant cytotoxicity on the cell lines tested. CompuSyn analysis of the drug combination effects revealed the strong synergistic interaction of the combination. Our results also indicate that COLO-320 cells were more sensitive for anticancer effects of the drugs than HCT-116 cells. The presence of Ras and PI3K mutations in HCT-116 cells could possibly be one of the main reasons for the observed outcome as compared to the wild type expressions of them in COLO-320 cells.","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2016-12-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81813817","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 5
Effect of Sunlight, Moisture, Temperature and Ultraviolet Radiation on the Quality Control Parameters of Ciprofloxacin Tablet Formulation 光照、湿度、温度和紫外线辐射对环丙沙星片制剂质量控制参数的影响
Pub Date : 2016-12-08 DOI: 10.5138/09750215.1928
K. M. Ezealisiji, Angenlina Pepple, C. Stanley
This work assesses the stability and quality of Ciprofloxacin hydrochloride tablets after subjection to accelerated stability conditions of sunlight, temperature of 40±1 0 C, 75% relative humidity, and UV light of 365 nm for 4 hours each day. This study was performed at time zero and at 4-day intervals for a period of 45 days (that is, days 0, 4, 8, 12…40, 44) according to the International Conference on Harmonization (ICH) accelerated aging conditions and the results obtained were subjected to statistical analysis. The results showed that with increasing time there was a gradual reduction in the dissolution rate with the tablets exposed to all four storage conditions failing the test on day 44 where they had less than 80 % release of the label claim. For content of Ciprofloxacin Hydrochloride, only those tablets exposed to UV light passed the test for all 44 days as they had a minimum of 96.83 % content on the 44 th day. At day 0, all the tablets assayed passed this test, having a ciprofloxacin content of 99.43 %. For those tablets subjected to the other storage conditions including temperature of 40±1 0 C, 75 % relative humidity and sunlight, they had ciprofloxacin content of 70.22 %, 71.50 %, and 78.36 % respectively. The results further, indicated that the storage conditions used in the study had a greater impact on the dissolution behavior and content of the Ciprofloxacin tablets than they did on the physical stability (hardness, uniformity of weight, disintegration).
本研究对盐酸环丙沙星片在光照、温度40±10℃、相对湿度75%、365 nm紫外光每天照射4小时的加速稳定条件下的稳定性和质量进行了评价。根据国际协调会议(ICH)的加速老化条件,本研究在时间0和间隔4天进行,为期45天(即0、4、8、12、40、44天),所得结果进行统计分析。结果表明,随着时间的增加,溶出率逐渐降低,暴露于所有四种储存条件下的片剂在第44天未能通过测试,因为它们的标签声明释放量低于80%。对于盐酸环丙沙星含量,只有在紫外光照射下44天均通过检测,第44天含量最低为96.83%。第0天,所有样品均通过本试验,环丙沙星含量为99.43%。在温度为40±10℃、相对湿度为75%、光照条件下,环丙沙星含量分别为70.22%、71.50%、78.36%。研究结果进一步表明,贮藏条件对环丙沙星片的溶出行为和含量的影响大于对其物理稳定性(硬度、重量均匀性、崩解性)的影响。
{"title":"Effect of Sunlight, Moisture, Temperature and Ultraviolet Radiation on the Quality Control Parameters of Ciprofloxacin Tablet Formulation","authors":"K. M. Ezealisiji, Angenlina Pepple, C. Stanley","doi":"10.5138/09750215.1928","DOIUrl":"https://doi.org/10.5138/09750215.1928","url":null,"abstract":"This work assesses the stability and quality of Ciprofloxacin hydrochloride tablets after subjection to accelerated stability conditions of sunlight, temperature of 40±1 0 C, 75% relative humidity, and UV light of 365 nm for 4 hours each day. This study was performed at time zero and at 4-day intervals for a period of 45 days (that is, days 0, 4, 8, 12…40, 44) according to the International Conference on Harmonization (ICH) accelerated aging conditions and the results obtained were subjected to statistical analysis. The results showed that with increasing time there was a gradual reduction in the dissolution rate with the tablets exposed to all four storage conditions failing the test on day 44 where they had less than 80 % release of the label claim. For content of Ciprofloxacin Hydrochloride, only those tablets exposed to UV light passed the test for all 44 days as they had a minimum of 96.83 % content on the 44 th day. At day 0, all the tablets assayed passed this test, having a ciprofloxacin content of 99.43 %. For those tablets subjected to the other storage conditions including temperature of 40±1 0 C, 75 % relative humidity and sunlight, they had ciprofloxacin content of 70.22 %, 71.50 %, and 78.36 % respectively. The results further, indicated that the storage conditions used in the study had a greater impact on the dissolution behavior and content of the Ciprofloxacin tablets than they did on the physical stability (hardness, uniformity of weight, disintegration).","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2016-12-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75617457","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 4
Deep Percutaneous Penetration into Muscles and Joints: Update 深层经皮渗透到肌肉和关节:更新
Pub Date : 2014-01-01 DOI: 10.1007/978-1-4939-1289-6_13
Vladyslava Doktor, Christine M. Lee, H. Maibach
{"title":"Deep Percutaneous Penetration into Muscles and Joints: Update","authors":"Vladyslava Doktor, Christine M. Lee, H. Maibach","doi":"10.1007/978-1-4939-1289-6_13","DOIUrl":"https://doi.org/10.1007/978-1-4939-1289-6_13","url":null,"abstract":"","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2014-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84701607","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 2
The emitted dose of drug from a valved holding chamber using five pressurized metered dose inhalers 使用5个加压计量吸入器从带阀的容纳室释放出的药物剂量
Pub Date : 2012-12-19 DOI: 10.5138/IJDD.V4I3.745
F. Berardino, A. Cesarani, Agostina Moles, O. Brenna
Background. The dose available at the mouth from a pressurised metered-dose inhaler (pMDI) cannot stay the same if it is used with a valved holding chamber (VHC). A different aerosol drug delivery system is created when the pMDI is used with the VHC and therefore the dose delivered to the patients is no longer that released from the pMDI alone, but the one emitted by the new system. This study aims to verify the emitted dose of five pMDI drugs when used with a VHC. Methods. The emitted dose was expressed as the amount of drug within the respirable fraction available at the end of the VHC, i.e. the drug output (measured by high performance liquid chromatography) multiplied by the percentage of FDF determined using a laser diffraction analyser. Results. the emitted doses were drastically reduced in comparison with the nominal doses (Beclomethasone from 250 to 90.5 µg, Budesonide from 200 to 100 µg, Ciclesonide from 160 to 102 µg Fluticasone from 250 to 116 µg, Salbutamol from 100 to 54 µg). Conclusions. When pMDIs are employed with a VHC, the emitted dose drastically changes; it is more or less halved. In order to facilitate prescription by the physician, both the nominal and the emitted doses should be reported in the VHC package.
背景。如果与带阀保持室(VHC)一起使用,从加压计量吸入器(pMDI)获得的口服剂量就不能保持不变。当pMDI与VHC一起使用时,产生了一种不同的气溶胶给药系统,因此给患者的剂量不再是pMDI单独释放的剂量,而是由新系统释放的剂量。本研究旨在验证五种pMDI药物与VHC一起使用时的释放剂量。方法。发射剂量表示为VHC结束时可用的可吸入部分内的药物量,即药物输出(通过高效液相色谱测量)乘以使用激光衍射分析仪确定的FDF百分比。结果。与标称剂量相比,放射剂量大幅减少(倍氯米松从250µg降至90.5µg,布地奈德从200µg降至100µg,环来奈德从160µg降至102µg,氟替卡松从250µg降至116µg,沙丁胺醇从100µg降至54µg)。结论。当pmdi与VHC一起使用时,发射剂量急剧变化;差不多减半了。为了方便医生开具处方,VHC包装中应同时报告名义剂量和放射剂量。
{"title":"The emitted dose of drug from a valved holding chamber using five pressurized metered dose inhalers","authors":"F. Berardino, A. Cesarani, Agostina Moles, O. Brenna","doi":"10.5138/IJDD.V4I3.745","DOIUrl":"https://doi.org/10.5138/IJDD.V4I3.745","url":null,"abstract":"Background. The dose available at the mouth from a pressurised metered-dose inhaler (pMDI) cannot stay the same if it is used with a valved holding chamber (VHC). A different aerosol drug delivery system is created when the pMDI is used with the VHC and therefore the dose delivered to the patients is no longer that released from the pMDI alone, but the one emitted by the new system. This study aims to verify the emitted dose of five pMDI drugs when used with a VHC. Methods. The emitted dose was expressed as the amount of drug within the respirable fraction available at the end of the VHC, i.e. the drug output (measured by high performance liquid chromatography) multiplied by the percentage of FDF determined using a laser diffraction analyser. Results. the emitted doses were drastically reduced in comparison with the nominal doses (Beclomethasone from 250 to 90.5 µg, Budesonide from 200 to 100 µg, Ciclesonide from 160 to 102 µg Fluticasone from 250 to 116 µg, Salbutamol from 100 to 54 µg). Conclusions. When pMDIs are employed with a VHC, the emitted dose drastically changes; it is more or less halved. In order to facilitate prescription by the physician, both the nominal and the emitted doses should be reported in the VHC package.","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2012-12-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81124368","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
期刊
International Journal of Drug Delivery
全部 Acc. Chem. Res. ACS Applied Bio Materials ACS Appl. Electron. Mater. ACS Appl. Energy Mater. ACS Appl. Mater. Interfaces ACS Appl. Nano Mater. ACS Appl. Polym. Mater. ACS BIOMATER-SCI ENG ACS Catal. ACS Cent. Sci. ACS Chem. Biol. ACS Chemical Health & Safety ACS Chem. Neurosci. ACS Comb. Sci. ACS Earth Space Chem. ACS Energy Lett. ACS Infect. Dis. ACS Macro Lett. ACS Mater. Lett. ACS Med. Chem. Lett. ACS Nano ACS Omega ACS Photonics ACS Sens. ACS Sustainable Chem. Eng. ACS Synth. Biol. Anal. Chem. BIOCHEMISTRY-US Bioconjugate Chem. BIOMACROMOLECULES Chem. Res. Toxicol. Chem. Rev. Chem. Mater. CRYST GROWTH DES ENERG FUEL Environ. Sci. Technol. Environ. Sci. Technol. Lett. Eur. J. Inorg. Chem. IND ENG CHEM RES Inorg. Chem. J. Agric. Food. Chem. J. Chem. Eng. Data J. Chem. Educ. J. Chem. Inf. Model. J. Chem. Theory Comput. J. Med. Chem. J. Nat. Prod. J PROTEOME RES J. Am. Chem. Soc. LANGMUIR MACROMOLECULES Mol. Pharmaceutics Nano Lett. Org. Lett. ORG PROCESS RES DEV ORGANOMETALLICS J. Org. Chem. J. Phys. Chem. J. Phys. Chem. A J. Phys. Chem. B J. Phys. Chem. C J. Phys. Chem. Lett. Analyst Anal. Methods Biomater. Sci. Catal. Sci. Technol. Chem. Commun. Chem. Soc. Rev. CHEM EDUC RES PRACT CRYSTENGCOMM Dalton Trans. Energy Environ. Sci. ENVIRON SCI-NANO ENVIRON SCI-PROC IMP ENVIRON SCI-WAT RES Faraday Discuss. Food Funct. Green Chem. Inorg. Chem. Front. Integr. Biol. J. Anal. At. Spectrom. J. Mater. Chem. A J. Mater. Chem. B J. Mater. Chem. C Lab Chip Mater. Chem. Front. Mater. Horiz. MEDCHEMCOMM Metallomics Mol. Biosyst. Mol. Syst. Des. Eng. Nanoscale Nanoscale Horiz. Nat. Prod. Rep. New J. Chem. Org. Biomol. Chem. Org. Chem. Front. PHOTOCH PHOTOBIO SCI PCCP Polym. Chem.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
0
微信
客服QQ
Book学术公众号 扫码关注我们
反馈
×
意见反馈
请填写您的意见或建议
请填写您的手机或邮箱
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
现在去查看 取消
×
提示
确定
Book学术官方微信
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术
文献互助 智能选刊 最新文献 互助须知 联系我们:info@booksci.cn
Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。
Copyright © 2023 Book学术 All rights reserved.
ghs 京公网安备 11010802042870号 京ICP备2023020795号-1