首页 > 最新文献

British Journal of Pharmacy最新文献

英文 中文
Physicochemical characterisation of spray dried ternary solid dispersions of simvastatin. Processability, tableting and dissolution. 辛伐他汀喷雾干燥三元固体分散体的物理化学性质。加工性、压片性和溶解性。
Pub Date : 2019-04-17 DOI: 10.5920/BJPHARM.605
Hanan Abdalmaula, A. Paradkar, K. Paluch
Simvastatin(SMV) is poorly soluble drug classified as belonging to Class II of BiopharmaceuticsClassification System. Common approach to improve apparent solubility of drugsis production of amorphous solid dispersions (ASD) by means of spray drying(SD) or hot-melt extrusion. Spray drying of low-glass transition temperature(Tg) ASDs is challenging due to the risk of material being exposed to SD outlettemperatures close to its Tg which may result in melting of ASD and subsequentcrystallisation of amorphous drug. It was hypothesised that addition ofeasily-crystallising material to ASD will improve its SD processability. Inaddition, it was hypothesised that produced ternary solid dispersions (TSD)composed of amorphous composite of drug and the polymer (PVP K17, 55 and 150) andcrystalline, soluble nanoparticles (NaCl) will improve dissolution of TSDtablets.  The dissolution of SMV fromTSDs was faster compared with that of binary solid dispersion in case of SMV-TSDsproduced with PVP K55 and 150. The tabletabilityassessment showed increase in compression led to increase in tensile strengthand decrease in porosities of SDs tablets.
辛伐他汀(SMV)是一种难溶性药物,属于生物药品分类系统第二类。提高药物表观溶解度的常用方法是采用喷雾干燥或热熔挤压法制备非晶固体分散体。低玻璃化转变温度(Tg) ASD的喷雾干燥是具有挑战性的,因为材料暴露在接近其Tg的SD出口温度下,可能导致ASD熔化和随后的非晶态药物结晶。假设在ASD中加入易结晶材料可以提高其SD加工性能。此外,假设制备由药物与聚合物(PVP K17、55和150)的非晶态复合材料和结晶性可溶纳米颗粒(NaCl)组成的三元固体分散体(TSD)将改善TSD片的溶出度。以PVP K55和PVP 150为原料制备的SMV- tsds中SMV的溶解速度比二元固体分散更快。抗压性评价表明,SDs片的抗拉强度增加,孔隙率降低。
{"title":"Physicochemical characterisation of spray dried ternary solid dispersions of simvastatin. Processability, tableting and dissolution.","authors":"Hanan Abdalmaula, A. Paradkar, K. Paluch","doi":"10.5920/BJPHARM.605","DOIUrl":"https://doi.org/10.5920/BJPHARM.605","url":null,"abstract":"Simvastatin(SMV) is poorly soluble drug classified as belonging to Class II of BiopharmaceuticsClassification System. Common approach to improve apparent solubility of drugsis production of amorphous solid dispersions (ASD) by means of spray drying(SD) or hot-melt extrusion. Spray drying of low-glass transition temperature(Tg) ASDs is challenging due to the risk of material being exposed to SD outlettemperatures close to its Tg which may result in melting of ASD and subsequentcrystallisation of amorphous drug. It was hypothesised that addition ofeasily-crystallising material to ASD will improve its SD processability. Inaddition, it was hypothesised that produced ternary solid dispersions (TSD)composed of amorphous composite of drug and the polymer (PVP K17, 55 and 150) andcrystalline, soluble nanoparticles (NaCl) will improve dissolution of TSDtablets.  The dissolution of SMV fromTSDs was faster compared with that of binary solid dispersion in case of SMV-TSDsproduced with PVP K55 and 150. The tabletabilityassessment showed increase in compression led to increase in tensile strengthand decrease in porosities of SDs tablets.","PeriodicalId":9253,"journal":{"name":"British Journal of Pharmacy","volume":"243 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-04-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77587690","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
Impact of solid state miscibility on quantitive nano-precipitation of budesonide and PVP-VA. 固相混相对布地奈德和PVP-VA定量纳米沉淀的影响。
Pub Date : 2019-04-03 DOI: 10.5920/BJPHARM.606
Hanan Abdalmaula, A. Paradkar, K. Paluch
In the present study, the drug–polymer miscibility and molecular interaction of budesonide in polymers (PVP/VA E 735, 635 and 535) systems were studied, by using three techniques including, calculation of Hansen solubility parameters, analysis of melting points depression, and measurement of glass transition temperature (Tg). Budesonide nanoparticles were prepared by sonication technique.  The combined effect of four significant formulation variables, namely, polymer and surfactant concentrations, time and amplitude of sonication on particle size, polydispersity, drug loading and entrapment efficiency of drug was investigated by apply 24 factorial design. The drug/ polymer blend was considered miscible depending on the results of three approaches. The results of calculated values of miscibility parameter (χ) for each pair were negative ranging from - 2.012to -1.948. Single Tg and positive deviation from Gordon-Taylor model for all ratios of drug–polymer binary mixtures. Produced amorphous budesonide nanoparticles, depending on choice of polymer and process parameters contained from 97% to 99% drug, with particle size diameter varying in size from 641-357 nm. It was found that clear evidence on effect VA ratio on percent entrapment efficiency and particle size of budesonide.
本文采用Hansen溶解度参数计算、熔点下降分析和玻璃化转变温度(Tg)测定三种方法,研究了布地奈德在PVP/VA E 735、635和535聚合物体系中的混相及分子相互作用。采用超声技术制备布地奈德纳米颗粒。采用24因子设计,考察了聚合物和表面活性剂浓度、超声时间和超声振幅对药物粒径、多分散性、载药量和包封效率的综合影响。根据三种方法的结果,药物/聚合物混合物被认为是可混溶的。各配对的混相参数(χ)计算值均为负值,范围为- 2.012 ~ -1.948。单Tg和正偏离戈登-泰勒模型对所有比例的药物-聚合物二元混合物。所制得的非晶布地奈德纳米颗粒,根据所选择的聚合物和工艺参数,药物含量在97% ~ 99%之间,粒径直径在641 ~ 357 nm之间。结果表明,VA比对布地奈德的捕集率和粒径有明显的影响。
{"title":"Impact of solid state miscibility on quantitive nano-precipitation of budesonide and PVP-VA.","authors":"Hanan Abdalmaula, A. Paradkar, K. Paluch","doi":"10.5920/BJPHARM.606","DOIUrl":"https://doi.org/10.5920/BJPHARM.606","url":null,"abstract":"In the present study, the drug–polymer miscibility and molecular interaction of budesonide in polymers (PVP/VA E 735, 635 and 535) systems were studied, by using three techniques including, calculation of Hansen solubility parameters, analysis of melting points depression, and measurement of glass transition temperature (Tg). Budesonide nanoparticles were prepared by sonication technique.  The combined effect of four significant formulation variables, namely, polymer and surfactant concentrations, time and amplitude of sonication on particle size, polydispersity, drug loading and entrapment efficiency of drug was investigated by apply 24 factorial design. The drug/ polymer blend was considered miscible depending on the results of three approaches. The results of calculated values of miscibility parameter (χ) for each pair were negative ranging from - 2.012to -1.948. Single Tg and positive deviation from Gordon-Taylor model for all ratios of drug–polymer binary mixtures. Produced amorphous budesonide nanoparticles, depending on choice of polymer and process parameters contained from 97% to 99% drug, with particle size diameter varying in size from 641-357 nm. It was found that clear evidence on effect VA ratio on percent entrapment efficiency and particle size of budesonide.","PeriodicalId":9253,"journal":{"name":"British Journal of Pharmacy","volume":"3 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-04-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88014986","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
A Novel Microfluidic Assembly of a Biodegradable Nanostructures Designed for Site Specific Delivery of Anticancer Peptide Site Specific Delivery of Anticancer Peptide 一种新型的可生物降解纳米结构微流控组件,用于抗癌肽的位点特异性传递
Pub Date : 2019-04-03 DOI: 10.5920/BJPHARM.601
A. Faheem, A. Elkordy, Mohamed El-Tanani, Samuel Girgis
Ran is a small RAS-related GTPase and is overexpressed in breast carcinoma to induce malignant transformation and metastatic growth. A novel series of antiRan-GTPase peptide (CK-10), which inhibits Ran hydrolysis and activation, have suboptimal activity in vitro due to low bioavailability and poor delivery. To overcome these disadvantages, we delivered the CK-10 peptide by encapsulating it in PLGA-based nanoparticles (NP). The successful delivery of CK-10 can prevent Ran activation by blocking a regulator of chromosome condensation 1 (RCC1) following peptide release directly in the cytoplasm after endocytosis of the novel NP(s). A novel hydrodynamic flow technique is designed to avoid the drawbacks with a double emulsion solvent evaporation technique. Loading efficiency and in vitro release were measured by modified Lowry assay, size was characterized by dynamic light scattering, tuneable pore resistive sensing and laser obscuration time, zeta potential was measured by laser anemometry, morphology was scanned by electron microscopes and laser obscuration time. Water absorption and its associated changes in the physicochemical properties were measured by various color indicator and potentiometric titration techniques tounderstand the fundamental biodegradation process. PLGA/β-cyclodextrin nanoparticles showed the highest peptide loading (53.92%m/m) for the novel microfluidic technique with the highest cumulative release of 91.38%.
Ran是一种小的ras相关GTPase,在乳腺癌中过表达,诱导恶性转化和转移生长。一种新型的抗Ran- gtpase肽(CK-10),可以抑制Ran的水解和激活,但由于生物利用度低和递送不良,其体外活性不理想。为了克服这些缺点,我们将CK-10肽包封在基于plga的纳米颗粒(NP)中。成功递送CK-10可以通过阻断新NP胞吞后在细胞质中直接释放肽后的染色体凝聚1 (RCC1)调节因子来阻止Ran激活。设计了一种新的流体动力流动技术,以避免双乳液溶剂蒸发技术的缺点。采用改进的Lowry法测定载药效率和体外释放度,采用动态光散射、可调孔电阻传感和激光遮蔽时间表征尺寸,采用激光风速法测定zeta电位,采用电子显微镜和激光遮蔽时间扫描形貌。通过各种显色指示剂和电位滴定技术测量了吸水率及其相关的物理化学性质变化,以了解基本的生物降解过程。新型微流控技术的PLGA/β-环糊精纳米颗粒多肽负载最高(53.92%m/m),累积释放量最高为91.38%。
{"title":"A Novel Microfluidic Assembly of a Biodegradable Nanostructures Designed for Site Specific Delivery of Anticancer Peptide Site Specific Delivery of Anticancer Peptide","authors":"A. Faheem, A. Elkordy, Mohamed El-Tanani, Samuel Girgis","doi":"10.5920/BJPHARM.601","DOIUrl":"https://doi.org/10.5920/BJPHARM.601","url":null,"abstract":"Ran is a small RAS-related GTPase and is overexpressed in breast carcinoma to induce malignant transformation and metastatic growth. A novel series of antiRan-GTPase peptide (CK-10), which inhibits Ran hydrolysis and activation, have suboptimal activity in vitro due to low bioavailability and poor delivery. To overcome these disadvantages, we delivered the CK-10 peptide by encapsulating it in PLGA-based nanoparticles (NP). The successful delivery of CK-10 can prevent Ran activation by blocking a regulator of chromosome condensation 1 (RCC1) following peptide release directly in the cytoplasm after endocytosis of the novel NP(s). A novel hydrodynamic flow technique is designed to avoid the drawbacks with a double emulsion solvent evaporation technique. Loading efficiency and in vitro release were measured by modified Lowry assay, size was characterized by dynamic light scattering, tuneable pore resistive sensing and laser obscuration time, zeta potential was measured by laser anemometry, morphology was scanned by electron microscopes and laser obscuration time. Water absorption and its associated changes in the physicochemical properties were measured by various color indicator and potentiometric titration techniques tounderstand the fundamental biodegradation process. PLGA/β-cyclodextrin nanoparticles showed the highest peptide loading (53.92%m/m) for the novel microfluidic technique with the highest cumulative release of 91.38%.","PeriodicalId":9253,"journal":{"name":"British Journal of Pharmacy","volume":"7 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-04-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85803263","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
A Novel biodegradable system based on poly (lactic‐co‐glycolic acid) nanoparticles for delivery of a novel anticancer peptide delivery of a novel anticancer peptide 一种新型的基于聚乳酸- co -乙醇酸纳米颗粒的可生物降解体系,用于递送一种新型抗癌肽
Pub Date : 2019-04-03 DOI: 10.5920/BJPHARM.599
A. Faheem, A. Elkordy, Mohamed El-Tanani, Samuel Girgis
The main objective of this work was to formulate novel amphiphilic PLGA nanoparticles with improved physicochemical properties for the delivery of the novel peptide (CK-10) to be used for targeting of the cancerous/tumour tissue. This was achieved by blending of various amphiphilic polymers with PLGA, especially by using a novel microfluidic technique which can overcome several problems of the conventional techniques like the double emulsion technique e.g. low peptide loading efficiencies, large sizes, and high PDI. Loading efficiency was measured by modified Lowry assay; size and zeta potential were characterized by dynamic light scattering and tuneable pore resistive sensing techniques; images were scanned by scanning and transmission electron microscopes; stability and interaction were confirmed by HPLC-MS, FTIR, DSC and CZE. PLGA/Poloxamer nanoparticles exhibited higher peptide loading than the other types of PLGA nanoparticles [56.13 %m/m for the novel microfluidic technique]. PLGA/Poloxamer prepared by the microfluidics technique had the smallest size with the lowest PDI (208.90 nm, 0.11) which is a vital parameter for targeting. The successful development of better physicochemical properties for the CK-10 loaded PLGA nanoparticles can improve the RAN blocking by CK-10.
这项工作的主要目的是制备具有改进的物理化学性质的新型两亲性PLGA纳米颗粒,用于递送用于靶向癌/肿瘤组织的新型肽(CK-10)。这是通过将各种两亲性聚合物与PLGA共混而实现的,特别是通过使用一种新的微流控技术,该技术可以克服双乳液技术等传统技术的几个问题,例如肽装载效率低,尺寸大,PDI高。采用改良Lowry法测定负载效率;采用动态光散射和可调孔电阻传感技术表征了尺寸和zeta电位;用扫描电镜和透射电镜对图像进行扫描;通过HPLC-MS、FTIR、DSC和CZE等方法证实了其稳定性和相互作用。PLGA/Poloxamer纳米颗粒比其他类型的PLGA纳米颗粒具有更高的肽负载[56.13% m/m的新型微流控技术]。微流控技术制备的PLGA/Poloxamer具有最小的尺寸和最低的PDI (208.90 nm, 0.11),这是靶向的重要参数。成功开发出了具有较好理化性质的负载CK-10的PLGA纳米颗粒,可以改善CK-10对RAN的阻断作用。
{"title":"A Novel biodegradable system based on poly (lactic‐co‐glycolic acid) nanoparticles for delivery of a novel anticancer peptide delivery of a novel anticancer peptide","authors":"A. Faheem, A. Elkordy, Mohamed El-Tanani, Samuel Girgis","doi":"10.5920/BJPHARM.599","DOIUrl":"https://doi.org/10.5920/BJPHARM.599","url":null,"abstract":"The main objective of this work was to formulate novel amphiphilic PLGA nanoparticles with improved physicochemical properties for the delivery of the novel peptide (CK-10) to be used for targeting of the cancerous/tumour tissue. This was achieved by blending of various amphiphilic polymers with PLGA, especially by using a novel microfluidic technique which can overcome several problems of the conventional techniques like the double emulsion technique e.g. low peptide loading efficiencies, large sizes, and high PDI. Loading efficiency was measured by modified Lowry assay; size and zeta potential were characterized by dynamic light scattering and tuneable pore resistive sensing techniques; images were scanned by scanning and transmission electron microscopes; stability and interaction were confirmed by HPLC-MS, FTIR, DSC and CZE. PLGA/Poloxamer nanoparticles exhibited higher peptide loading than the other types of PLGA nanoparticles [56.13 %m/m for the novel microfluidic technique]. PLGA/Poloxamer prepared by the microfluidics technique had the smallest size with the lowest PDI (208.90 nm, 0.11) which is a vital parameter for targeting. The successful development of better physicochemical properties for the CK-10 loaded PLGA nanoparticles can improve the RAN blocking by CK-10.","PeriodicalId":9253,"journal":{"name":"British Journal of Pharmacy","volume":"30 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-04-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85334127","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
Bilayer Dissolving Microneedles Incorporating Hypericin-Loaded Nanocapsules For Improved Localised Photodynamic Therapy 含有金丝桃素负载纳米胶囊的双层溶解微针用于改善局部光动力治疗
Pub Date : 2019-04-03 DOI: 10.5920/BJPHARM.593
A. Ramadan, Heba M. Abd-El-Azim, I. Tekko, N. Khalafallah, N. Nafee, R. Donnelly
Hypericin (Hy) is a potent lipid-soluble photosensitizerhaving broad pharmacological spectrum. Nevertheless, its poor water solubilityleads to its aggregation in the biological systems that consequently diminishesits photodynamic activity (PDA) and its therapeutic applications. Therefore,this study presents novel hydro-solving bilayer microneedle (MN) arraysincorporating Hy-loaded lipid nanocapsules (LNC) to prevent drug aggregation,enhance its delivery and local PDA. The Hy-LNC were prepared by phase inversiontechnique and showed homogenous particle size distribution and highencapsulation efficiency (88.42 ± 0.11%). The bilayer MNs consist of a hydrogelcross-linked, drug-free base plate and a Hy-loaded MN for a one-stepapplication. The dissolving MNs were fabricated from aqueous blends of 10% w/wpolyvinyl alcohol and 30% w/w polyvinyl pyrrolidone by casting and pressure.The MN arrays were characterized for mechanical strength and insertion depth.The bilayer arrays showed good mechanical strength under a compression force of32 N, with a height reduction of 10.14 ± 0.55% and sufficient insertion depthin both Parafilm M® and the excised porcine skin. After 2h of application toexcised pig skin, the MNs were completely dissolved ensuring the delivery ofits payload and the base plate was removed intact free from MN residuals. Inconclusion, the incorporation of Hy-LNC into this novel bilayer MNs overcomeits aggregation and ensured the complete insertion of the drug-loaded MNs. ThisLNC-MN system is promising for improving Hy local availability and thusenhancing its photodynamic application.
金丝桃素(Hy)是一种有效的脂溶性光敏剂,具有广泛的药谱。然而,其水溶性差导致其在生物系统中聚集,从而降低其光动力活性(PDA)及其治疗应用。因此,本研究提出了一种新型的水溶性双层微针(MN)阵列,结合负载高脂纳米胶囊(LNC)来防止药物聚集,增强其递送和局部PDA。采用相转化法制备的Hy-LNC粒径分布均匀,包封效率高(88.42±0.11%)。双层MN由水凝胶交联的无药物基板和氢负载MN组成,用于一步应用。以10% w/w的聚乙烯醇和30% w/w的聚乙烯醇为溶剂,通过浇铸和加压法制备了可溶解的纳米颗粒。对MN阵列的机械强度和插入深度进行了表征。该双层阵列在32 N的压缩力下表现出良好的机械强度,高度降低10.14±0.55%,在Parafilm®和切除的猪皮中都有足够的插入深度。在切除的猪皮上应用2h后,MN被完全溶解,以确保其有效载荷的传递,并且基底板被完整地去除MN残留物。综上所述,将Hy-LNC整合到这种新型双层MNs中克服了其聚集性,并确保了载药MNs的完全插入。该系统有望提高Hy的局部可用性,从而增强其光动力学应用。
{"title":"Bilayer Dissolving Microneedles Incorporating Hypericin-Loaded Nanocapsules For Improved Localised Photodynamic Therapy","authors":"A. Ramadan, Heba M. Abd-El-Azim, I. Tekko, N. Khalafallah, N. Nafee, R. Donnelly","doi":"10.5920/BJPHARM.593","DOIUrl":"https://doi.org/10.5920/BJPHARM.593","url":null,"abstract":"Hypericin (Hy) is a potent lipid-soluble photosensitizerhaving broad pharmacological spectrum. Nevertheless, its poor water solubilityleads to its aggregation in the biological systems that consequently diminishesits photodynamic activity (PDA) and its therapeutic applications. Therefore,this study presents novel hydro-solving bilayer microneedle (MN) arraysincorporating Hy-loaded lipid nanocapsules (LNC) to prevent drug aggregation,enhance its delivery and local PDA. The Hy-LNC were prepared by phase inversiontechnique and showed homogenous particle size distribution and highencapsulation efficiency (88.42 ± 0.11%). The bilayer MNs consist of a hydrogelcross-linked, drug-free base plate and a Hy-loaded MN for a one-stepapplication. The dissolving MNs were fabricated from aqueous blends of 10% w/wpolyvinyl alcohol and 30% w/w polyvinyl pyrrolidone by casting and pressure.The MN arrays were characterized for mechanical strength and insertion depth.The bilayer arrays showed good mechanical strength under a compression force of32 N, with a height reduction of 10.14 ± 0.55% and sufficient insertion depthin both Parafilm M® and the excised porcine skin. After 2h of application toexcised pig skin, the MNs were completely dissolved ensuring the delivery ofits payload and the base plate was removed intact free from MN residuals. Inconclusion, the incorporation of Hy-LNC into this novel bilayer MNs overcomeits aggregation and ensured the complete insertion of the drug-loaded MNs. ThisLNC-MN system is promising for improving Hy local availability and thusenhancing its photodynamic application.","PeriodicalId":9253,"journal":{"name":"British Journal of Pharmacy","volume":"46 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-04-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85832058","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
Oral Insulin Delivery in Diabetic Rats by PLGA Nanoparticles Combined with a Protease Inhibitor (N-Ethylmaleimide) PLGA纳米颗粒联合蛋白酶抑制剂(n -乙基马来酰亚胺)给药糖尿病大鼠口服胰岛素
Pub Date : 2019-04-02 DOI: 10.5920/BJPHARM.588
A. Faheem, D. Abdelkader, M. Osman, P. McCarron, S. El-Gizawy
Nanoparticles have shown a certain potential to overcome thedrawbacks of oral peptide delivery in the gastrointestinal tract such as lowpeptide stability and permeability. Insulin PLGA NP were prepared using amodified double emulsion solvent evaporation technique. Insulin PLGA NP were composedfrom human insulin (5 mg) encapsulated in PLGA 2.5% (w/v) mixed with PEG (2kDa, 5% w/w) and the external aqueous phase contained 1.25% of PVA. Theresulting nanoparticles of 202.6 nm diameter and loaded with 33.86 μg insulinper mg of polymer were utilised in this study to examine the hypoglycaemiceffect after combination with a protease inhibitor, N-Ethylmaleimide.
纳米颗粒已经显示出一定的潜力来克服口服肽在胃肠道中递送的缺点,如肽的低稳定性和渗透性。采用改进的双乳溶剂蒸发技术制备胰岛素PLGA NP。胰岛素PLGA NP由人胰岛素(5mg)包封在PLGA 2.5% (w/v)中,与PEG (2kDa, 5% w/w)混合,外水相含有1.25%的PVA组成。该纳米颗粒直径为202.6 nm,负载33.86 μg / mg的聚合物,在本研究中研究了与蛋白酶抑制剂n -乙基马来酰亚胺联合使用后的降糖效果。
{"title":"Oral Insulin Delivery in Diabetic Rats by PLGA Nanoparticles Combined with a Protease Inhibitor (N-Ethylmaleimide)","authors":"A. Faheem, D. Abdelkader, M. Osman, P. McCarron, S. El-Gizawy","doi":"10.5920/BJPHARM.588","DOIUrl":"https://doi.org/10.5920/BJPHARM.588","url":null,"abstract":"Nanoparticles have shown a certain potential to overcome thedrawbacks of oral peptide delivery in the gastrointestinal tract such as lowpeptide stability and permeability. Insulin PLGA NP were prepared using amodified double emulsion solvent evaporation technique. Insulin PLGA NP were composedfrom human insulin (5 mg) encapsulated in PLGA 2.5% (w/v) mixed with PEG (2kDa, 5% w/w) and the external aqueous phase contained 1.25% of PVA. Theresulting nanoparticles of 202.6 nm diameter and loaded with 33.86 μg insulinper mg of polymer were utilised in this study to examine the hypoglycaemiceffect after combination with a protease inhibitor, N-Ethylmaleimide.","PeriodicalId":9253,"journal":{"name":"British Journal of Pharmacy","volume":"83 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-04-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78799575","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 influence of oxygen and pressure on keratinocytes 氧和压力对角质形成细胞的影响
Pub Date : 2019-04-02 DOI: 10.5920/BJPHARM.598
Adrian C Williams, K. A. Obeid, K. W. Ng, W. Lau
Thisstudy aims to elucidate the respective effects of normobaric hyperoxygenationand hyperbaric pressurisation on key re-epithelialisation processes in woundhealing. Cultured human keratinocytes exposed to intermittent normobaric hyperoxygenationexhibited enhanced cellularmigration marked by a significant decline in E-cadherin expression. Keratinocyteproliferation, cellular metabolic activity, as well as IL-6 and IL-8 releasewere also significantly reduced. These changes were not observed with hyperbaricpressurisation alone. Moreover, cellular differentiation was not altered undernormobaric hyperoxygenation or hyperbaric pressurisation. Thus, we concludethat hyperoxygenation differentially modulates key cellular processes in re-epithelialisation.Oxygenation, but not pressurisation, appears to be the predominant factor modulatingkeratinocyte migration and proliferation. These findings argue for an alternativetreatment modality to hyperbaric oxygenation for wound healing, focused on enhancingtissue oxygenation without administering hyperbaric pressures.
本研究旨在阐明常压高氧和高压分别对伤口愈合中关键的再上皮化过程的影响。培养的人角质形成细胞暴露于间歇性常压高氧环境下,表现出细胞迁移增强,其特征是e -钙粘蛋白表达显著下降。角质细胞增殖、细胞代谢活性以及IL-6和IL-8的释放也显著降低。单独使用高压加压时没有观察到这些变化。此外,在常压高氧或高压加压下,细胞分化没有改变。因此,我们得出结论,高氧对再上皮化的关键细胞过程有差异调节。氧合作用,而不是加压作用,似乎是角化细胞迁移和增殖的主要调节因素。这些发现为伤口愈合提供了一种替代高压氧合的治疗方式,重点是在不施加高压的情况下增强组织氧合。
{"title":"The influence of oxygen and pressure on keratinocytes","authors":"Adrian C Williams, K. A. Obeid, K. W. Ng, W. Lau","doi":"10.5920/BJPHARM.598","DOIUrl":"https://doi.org/10.5920/BJPHARM.598","url":null,"abstract":"Thisstudy aims to elucidate the respective effects of normobaric hyperoxygenationand hyperbaric pressurisation on key re-epithelialisation processes in woundhealing. Cultured human keratinocytes exposed to intermittent normobaric hyperoxygenationexhibited enhanced cellularmigration marked by a significant decline in E-cadherin expression. Keratinocyteproliferation, cellular metabolic activity, as well as IL-6 and IL-8 releasewere also significantly reduced. These changes were not observed with hyperbaricpressurisation alone. Moreover, cellular differentiation was not altered undernormobaric hyperoxygenation or hyperbaric pressurisation. Thus, we concludethat hyperoxygenation differentially modulates key cellular processes in re-epithelialisation.Oxygenation, but not pressurisation, appears to be the predominant factor modulatingkeratinocyte migration and proliferation. These findings argue for an alternativetreatment modality to hyperbaric oxygenation for wound healing, focused on enhancingtissue oxygenation without administering hyperbaric pressures.","PeriodicalId":9253,"journal":{"name":"British Journal of Pharmacy","volume":"257 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-04-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76782045","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
Effect of pregelatinization and carboxymethylation on starches from African rice and Fonio: Influence on release of low melting-point drug Starch modifications for drug release 预糊化和羧甲基化对非洲大米和木薯淀粉的影响:对低熔点药物释放的影响
Pub Date : 2019-03-29 DOI: 10.5920/BJPHARM.645
A. Adeola, K. Asare-Addo, Michael A. Odeniyi, O. A. Omoteso, W. Kaialy
The study investigated theeffect of modification on the physicochemical and drug release properties ofstarches extracted from African rice (Oryzaglaberrima Steud) (AR) and Fonio (Digitariaexilis Stapf) (FR). The starches were modified by pregelatinization andcarboxymethylation.  The morphology andphysicochemical properties of the produced grades of starches were analysedusing SEM, RVA, FTIR, P-XRD and DSC. Dissolution was also conducted using amodel poorly-soluble drug with low melting point (Ibuprofen). SEM images showeda distinct change in the morphology of the modified starches. Native starchforms had the highest solubility while the carboxymethylated starch forms hadthe highest water absorbing capacity and swelling index. FTIR and P-XRDconfirmed the characteristic functional groups of the starches with theirthermal properties demonstrated by DSC. Ibuprofen release from the starch tabletsin phosphate buffer (pH 6.8) showed that native AR starch demonstrated similarrelease profiles with its carboxymethylated form (f2 = 57.5), however, different from the pregelatinisedform (f2 = 32.8). Native FRstarch demonstrated a different release profile to the carboxymethylated (f2 = 8.6) and the pregelatinisedstarch forms (f2 = 35.3). Fickiandiffusion was the main kinetics of drug release. Modification of these starchescan generate polysaccharides with different properties and improvedfunctionalities with a potential for use as alternative pharmaceuticalexcipients.
研究了改性对非洲稻(Oryzaglaberrima Steud) (AR)和丰io (Digitariaexilis Stapf) (FR)淀粉提取物理化性质和药物释放特性的影响。通过预糊化和羧甲基化对淀粉进行改性。采用扫描电镜(SEM)、红外光谱(RVA)、红外光谱(FTIR)、x射线衍射(P-XRD)和差热分析(DSC)对所制淀粉的形貌和理化性质进行了分析。用低熔点难溶性药物(布洛芬)进行溶出。SEM图像显示,改性淀粉的形貌发生了明显的变化。原生淀粉的溶解度最高,羧甲基化淀粉的吸水能力和溶胀指数最高。FTIR和p - x射线衍射证实了淀粉的特征官能团,DSC表征了淀粉的热性质。磷酸缓冲液(pH 6.8)中淀粉片的布洛芬释放表明,原生AR淀粉与其羧甲基化形式表现出相似的释放谱(f2 = 57.5),但与预糊化形式不同(f2 = 32.8)。原生fr淀粉与羧甲基化淀粉(f2 = 8.6)和预糊化淀粉(f2 = 35.3)表现出不同的释放特征。黏性扩散是药物释放的主要动力学过程。这些淀粉的改性可以产生具有不同性质和改进功能的多糖,具有作为替代药物解毒剂的潜力。
{"title":"Effect of pregelatinization and carboxymethylation on starches from African rice and Fonio: Influence on release of low melting-point drug Starch modifications for drug release","authors":"A. Adeola, K. Asare-Addo, Michael A. Odeniyi, O. A. Omoteso, W. Kaialy","doi":"10.5920/BJPHARM.645","DOIUrl":"https://doi.org/10.5920/BJPHARM.645","url":null,"abstract":"The study investigated theeffect of modification on the physicochemical and drug release properties ofstarches extracted from African rice (Oryzaglaberrima Steud) (AR) and Fonio (Digitariaexilis Stapf) (FR). The starches were modified by pregelatinization andcarboxymethylation.  The morphology andphysicochemical properties of the produced grades of starches were analysedusing SEM, RVA, FTIR, P-XRD and DSC. Dissolution was also conducted using amodel poorly-soluble drug with low melting point (Ibuprofen). SEM images showeda distinct change in the morphology of the modified starches. Native starchforms had the highest solubility while the carboxymethylated starch forms hadthe highest water absorbing capacity and swelling index. FTIR and P-XRDconfirmed the characteristic functional groups of the starches with theirthermal properties demonstrated by DSC. Ibuprofen release from the starch tabletsin phosphate buffer (pH 6.8) showed that native AR starch demonstrated similarrelease profiles with its carboxymethylated form (f2 = 57.5), however, different from the pregelatinisedform (f2 = 32.8). Native FRstarch demonstrated a different release profile to the carboxymethylated (f2 = 8.6) and the pregelatinisedstarch forms (f2 = 35.3). Fickiandiffusion was the main kinetics of drug release. Modification of these starchescan generate polysaccharides with different properties and improvedfunctionalities with a potential for use as alternative pharmaceuticalexcipients.","PeriodicalId":9253,"journal":{"name":"British Journal of Pharmacy","volume":"1 2 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-03-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82225973","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
Osteoporosis therapy initiation post-minimal trauma fracture 骨质疏松治疗开始后,最小创伤骨折
Pub Date : 2019-02-06 DOI: 10.5920/BJPHARM.567
Mary G. Etty-Leal, V. Tran, Lara Kusmanoff, D. Pearce, A. Politis, Loren A. Reynolds, D. Sepe, V. Chan
Aim: To determine the proportion of patients admitted to a major tertiary teaching hospital in Australia aged 50 years and older with a confirmed neck of femur or vertebral minimal trauma fracture, who are commenced on specific antiosteoporosis therapy by discharge, and to describe the agents prescribed. Methods: A retrospective analysis was conducted using patients’ electronic medical files of patients admitted with a minimal trauma fracture of the hip or vertebra during a 6 month period. Results: A total of 407 patients were audited and 64 patients were included in the study; 37 were admitted for a fractured hip and 27 were admitted for a vertebral fracture. Of these 64 patients, a total of 14 (21.9%) patients were commenced on specific anti-osteoporosis therapy. Denosumab (71%) was the most commonly initiated treatment, followed by risedronate (21%) then alendronate (7%). Conclusion: Majority of patients presenting to hospital with a minimal trauma fracture were not commenced on anti-osteoporosis therapy in hospital. This is a missed opportunity for intervention that may place patients at a higher risk of subsequent fracture; therefore effective strategies should be implemented to address this treatment gap in the future.
目的:确定澳大利亚一家大型三级教学医院收治的50岁及以上确诊股骨颈或椎体轻度创伤性骨折的患者出院时开始接受特定抗骨质疏松治疗的比例,并描述所开药物。方法:回顾性分析6个月内髋部或椎体轻度创伤性骨折患者的电子病历。结果:共审核407例患者,64例患者纳入研究;37人因髋部骨折入院,27人因椎体骨折入院。在这64例患者中,共有14例(21.9%)患者开始接受特异性抗骨质疏松治疗。Denosumab(71%)是最常见的初始治疗,其次是利塞膦酸钠(21%),然后是阿仑膦酸钠(7%)。结论:大多数轻度创伤性骨折患者未在医院开始抗骨质疏松治疗。这是一个错失的干预机会,可能会使患者面临更高的骨折风险;因此,未来应该实施有效的策略来解决这一治疗差距。
{"title":"Osteoporosis therapy initiation post-minimal trauma fracture","authors":"Mary G. Etty-Leal, V. Tran, Lara Kusmanoff, D. Pearce, A. Politis, Loren A. Reynolds, D. Sepe, V. Chan","doi":"10.5920/BJPHARM.567","DOIUrl":"https://doi.org/10.5920/BJPHARM.567","url":null,"abstract":"Aim: To determine the proportion of patients admitted to a major tertiary teaching hospital in Australia aged 50 years and older with a confirmed neck of femur or vertebral minimal trauma fracture, who are commenced on specific antiosteoporosis therapy by discharge, and to describe the agents prescribed. Methods: A retrospective analysis was conducted using patients’ electronic medical files of patients admitted with a minimal trauma fracture of the hip or vertebra during a 6 month period. Results: A total of 407 patients were audited and 64 patients were included in the study; 37 were admitted for a fractured hip and 27 were admitted for a vertebral fracture. Of these 64 patients, a total of 14 (21.9%) patients were commenced on specific anti-osteoporosis therapy. Denosumab (71%) was the most commonly initiated treatment, followed by risedronate (21%) then alendronate (7%). Conclusion: Majority of patients presenting to hospital with a minimal trauma fracture were not commenced on anti-osteoporosis therapy in hospital. This is a missed opportunity for intervention that may place patients at a higher risk of subsequent fracture; therefore effective strategies should be implemented to address this treatment gap in the future.","PeriodicalId":9253,"journal":{"name":"British Journal of Pharmacy","volume":"116 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-02-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87675369","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
Surface texture analysis of 3D printed matrices: before and after dissolution 3DP tablet surface imaging 3D打印基质表面纹理分析:溶出前后的3DP片剂表面成像
Pub Date : 2019-01-14 DOI: 10.5920/BJPHARM.554
B. Conway, M. U. Ghori, Z. Khizer
{"title":"Surface texture analysis of 3D printed matrices: before and after dissolution 3DP tablet surface imaging","authors":"B. Conway, M. U. Ghori, Z. Khizer","doi":"10.5920/BJPHARM.554","DOIUrl":"https://doi.org/10.5920/BJPHARM.554","url":null,"abstract":"","PeriodicalId":9253,"journal":{"name":"British Journal of Pharmacy","volume":"60 5 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86800341","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
期刊
British Journal of Pharmacy
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