Binder effectiveness for beads with high drug levels

Previous reports from these laboratories showed that microcrystalline cellulose (Avicel^R MCC, PH-101) formulations with low and medium drug levels (10 and 50%) produced very uniform beads whereas formulations containing MCC with high drug levels (80%) were difficult to process without special treatment or required the incorporation of alternate excipients. In this study, several binders, at a 2% level, specifically: Carbomer (Carbopol^R 934-P), Sodium carboxymethylcellulose (CMC 7MF), Hydroxypropylcellulose (Klucel^R HXF), Methylcellulose (Methocel^R K-15). Povidone, USP (PVP K29-32) and Pregelatinized starch NF (Starch 1500^R), were evaluated to determine whether they might impart advantages in processing and whether any differences in dissolution behavior would result. Spheres containing 80% anhydrous theophylline, the binders and MCC were manufactured by the extrusion/marumerization technique. In general, beads containing high drug levels produced with these binders are suitable for further processing (coating). Processing ease, bead shape, and bead hardness (friability) varied with the choice of binder. Beads with carbomer, hydroxypropylcellulose, and methylcellulose remained intact during dissolution testing; beads with starch, carboxymethylcellulose, PVP, and the control did not.     

Effluent from drug manufactures contains extremely high levels of pharmaceuticals

It is generally accepted that the main route for human pharmaceuticals to the aquatic environment is via sewage treatment plants receiving wastewater from households and hospitals. We have analysed pharmaceuticals in the effluent from a wastewater treatment plant serving about 90 bulk drug manufacturers in Patancheru, near Hyderabad, India--a major production site of generic drugs for the world market. The samples contained by far the highest levels of pharmaceuticals reported in any effluent. The high levels of several broad-spectrum antibiotics raise concerns about resistance development. The concentration of the most abundant drug, ciprofloxacin (up to 31,000 microg/L) exceeds levels toxic to some bacteria by over 1000-fold. The results from the present study call for an increased focus on the potential release of active pharmaceutical ingredients from production facilities in different regions.     

改性PVDF或替代PVDF粘结剂在锂电池中的应用研究进展

在锂电池中,粘结剂主要用来稳定电极结构,虽然含量较少,但是对电池性能影响较大.聚偏氟乙烯(PVDF)是目前主要使用的粘结剂,但其在不同活性物质中的应用存在不同的缺陷.因此对于不同活性物质应选用不同的粘结剂.在正极中,磷酸铁锂和三元材料(NCM)由于本身晶型限制,表现出较差的导电性和离子电导率,具有更高离子扩散系数的粘结剂对电池性能的提高作用更明显.硫正极在充放电过程中,"飞梭效应"是导致电池性能变差的主要因素之一,而具有含氧官能团的粘结剂捕获多硫化锂能力极强,对电池性能的提高作用明显.对于锂电池负极活性材料,传统PVDF粘结剂易与碳基材料反应导致锂盐沉积在负极,影响电池性能.因此在电池循环中,能产生更均一且稳定的SEI膜的粘结剂可阻止活性物质脱落和促进锂离子传导,提高电池性能.硅基负极材料在脱嵌锂过程中,材料体积变化较大,易使活性物质从集流体上脱落,而粘弹性适中且具有立体网状结构的粘结剂可以使硅负极发生可逆膨胀,减少活性物质损失,提升电池性能.此外,尖晶石结构的LTO负极材料导电性较差,人们对导电聚合物粘结剂关注较多,未来其也将会是主要研究方向之一.本文将近几年关于粘结剂的文献基于活性材料进行分类综述,探究粘结剂对锂电池的影响,并对未来正负极粘结剂的发展趋势进行展望.     

Investigation on sulphonated PEEK beads for drug delivery,bioactivity and tissue engineering applications

Poly ether ether ketone (PEEK) has wide applications in the field of medicine as a prosthetic material and can be sulphonated using sulphuric acid. This study focuses on the fabrication of water soluble SPEEK beads using infusion pump and the obtained beads were characterised using Fourier Transform Infra Red (FTIR) spectroscopy to confirm the sulphonation, while their surface morphology was studied using scanning electron microscope (SEM). In order to study the bioactivity of the prepared beads, hydroxyapatite was dispersed within them followed by their immersion in SBF. In order to study the drug release kinetics of the beads, they were loaded with amoxicillin in different concentrations. Cytotoxicity studies were performed by MTT method and ALP activity was measured using mouse osteoblast cells (MC3T3-E1). The SEM and FTIR of the prepared beads confirmed the morphology and the sulphonation of the prepared beads. Also, the apatite formation on the SPEEK beads, subsequent to their immersion in SBF, proved that the beads possessed excellent bioactivity. Moreover, the beads developed exhibited low cytotoxicity, implying good biocompatibility and safety. Thus, the results of the study indicated that the novel SPEEK beads could potentially be used as a drug carrying vehicle with low toxicity.     

Comparison of DC Bead-irinotecan and DC Bead-topotecan drug eluting beads for use in locoregional drug delivery to treat pancreatic cancer

DC Bead^® is a drug delivery embolisation system that can be loaded with doxorubicin or irinotecan for the treatment of a variety of liver cancers. In this study we demonstrate that the topoisomerase I inhibitor topotecan hydrochloride can be successfully loaded into the DC Bead sulfonate-modified polyvinyl alcohol hydrogel matrix, resulting in a sustained-release drug eluting bead (DEBTOP) useful for therapeutic purposes. The in vitro drug loading capacity, elution characteristics and the effects on mechanical properties of the beads are described with reference to our previous work with irinotecan hydrochloride (DEBIRI). Results showed that drug loading was faster when the solution was agitated compared to static loading and a maximum loading of ca. 40–45 mg topotecan in 1 ml hydrated beads was achievable. Loading the drug into the beads altered the size, compressibility moduli and colour of the bead. Elution was shown to be reliant on the presence of ions to perform the necessary exchange with the electrostatically bound topotecan molecules. Topotecan was shown by MTS assay to have an IC₅₀ for human pancreatic adenocarcinoma cells (PSN-1) of 0.22 and 0.27 μM compared to 28.1 and 19.2 μM for irinotecan at 48 and 72 h, respectively. The cytotoxic efficacy of DEBTOP on PSN-1 was compared to DEBIRI. DEPTOP loaded at 6 &; 30 mg ml^?1, like its free drug form, was shown to be more potent than DEBIRI of comparable doses at 24, 48 &; 72 h using a slightly modified MTS assay. Using a PSN-1 mouse xenograft model, DEBIRI doses of 3.3–6.6 mg were shown to be well-tolerated (even with repeat administration) and effective in reducing the tumour size. DEBTOP however, was lethal after 6 days at doses of 0.83–1.2 mg but demonstrated reasonable efficacy and tolerability (again with repeat injection possible) at 0.2–0.4 mg doses. Care must therefore be taken when selecting the dose of topotecan to be loaded into DC Bead given its greater potency and potential toxicity.     

Chiral nanoporous metal-organic frameworks with high porosity as materials for drug delivery

A chiral nanoporous metal-organic framework (MOF) with high porosity is obtained based on nontoxic zinc and achiral hexadentate ligand. It shows high drug loading and slow release of the proportion of the loaded drug with a complete delivery time of about one week when used as a material for adsorption and delivery of anticancer 5-fluorouracil.     

Quantum dot-encoded mesoporous beads with high brightness and uniformity: rapid readout using flow cytometry

A new generation of optically encoded beads has been prepared by using mesoporous polystyrene beads and surfactant-coated semiconductor quantum dots. In comparison with nonporous beads of similar sizes and chemical compositions, the encoded porous beads are approximately 1000 times brighter and 5 times more uniform in fluorescence intensities. Using both absolute intensity and ratiometric fluorescence coding, we show that the beads can be identified with a standard flow cytometer at 1000 beads/s. This result indicates that the multiple excited-state lifetimes and relaxation pathways of quantum dots do not limit their applications in high-speed optical detection and imaging.     

Development of novel gastroretentive drug delivery system of gliclazide: hollow beads

Aim: The current communication deals with the development of hollow floating beads of gliclazide. The primary effect of this drug is to potentiate glucose-stimulated insulin release from pancreatic islet-β-cells by induction of a decrease in potassium efflux from these cells. Because of the poor aqueous solubility, its absorption is limited. Thus, an attempt was made to improve its release profile.

Methods: The hollow drug-loaded alginate beads in combination with low methoxyl pectin and hydroxypropylmethylcellulose (HPMC) were prepared by a simple ionotropic gelation method. The beads were evaluated for particle size and morphology using optical microscopy and scanning electron microscopy (SEM), respectively. Mucoadhesion test was done using goat stomach mucosal membrane. Release characteristics of the gliclazide-loaded hollow beads were studied in 0.1?N HCl (pH 1.2) and phosphate buffer (pH 5.8).

Results: The developed beads were spherical in shape with hollow internal structure and had a particle size in the range of 0.730?±?0.05 to 0.890?±?0.03?mm. The incorporation efficiency of alginate -pectin beads was higher than alginate -HPMC beads. The Fourier transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC) and X-ray diffraction analysis showed stable character of drug in the drug-loaded hollow beads and revealed the absence of any drug -polymer interactions. The beads remained buoyant for more than 12?h. The drug release from beads followed Fickian diffusion with swelling.

Conclusion: The preliminary results of this study suggest that the developed beads containing gliclazide could enhance drug entrapment efficiency, reduce the initial burst release and modulate the drug release.     

Encoded beads for electrochemical identification

Encoded redox beads, based on the encapsulation of different quantum dots (QD) within polystyrene microspheres, have been developed for electrochemical identification. Encoded redox rods, prepared by sequential plating of different metal tracers into the pores of a host membrane, have also been designed. By incorporating different predetermined levels of multiple metal markers, such redox-encoded particles lead to a large number of recognizable voltammetric signatures and, hence, offer great promise for covert tagging of commercial products. The resulting voltammetric signatures correlate well with the predetermined loading ratio, indicating a reproducible encapsulation process. As desired for effective authenticity testing, QD-based "identification layers" were reproducibly cast and removed from packages of commercial products to display their distinct voltammetric profiles. Factors affecting the preparation of such identification layers were optimized.     

A New Binder for Pharmaceutical Dosage Forms

Gellan gum is a biodegradable polysaccharide recently approved by the U.S. Food and Drug Administration (FDA) for industrial use as a food additive. The objective of the present investigation was to evaluate its potential use as a binder for pharmaceutical dosage forms. Tablets were prepared with gellan gum and evaluated for tablet characteristics. Efficiency of gellan gum and its effects on various disintegrants were also studied.     

An effectiveness analysis of altmetrics indices for different levels of artificial intelligence publications

Scientometrics - Altmetrics indices are increasingly applied to measure scholarly influence in recent years because they can reflect the influence of research outputs more timely comparing with...     

Solidification of Boron-Containing Ion-Exchange Resins with Aluminosilicate Binder

Radiochemistry - Solidification of a mixture of ion-exchanger resins (IERs), consisting of a cation exchanger in the sodium form and an anion exchanger in the tetraborate form, using a binder based...     

Low-Dose Electroradiographic Multilayer System with PbO Binder Layers

An advantage of electrophotographic multilayer systems is that both for the generation and for the storage of pictorial electric charges. layers can be used with optimum properties for each function. Large-area and highly sensitive PbO binder layers which are marked by an excellent absorption of X-rays. and with adielectric foil which is directly glued to the binder layer without any additional adhesive penetrating into the layer, are used. Since the time taken to irradiate the whole picture area has to be short, a liquid electrode is used to increase the sensitivity. Essential steps in the performance of this process are shorting ofthe electrodes after taking the picture and subsequently the fast removal of the liquid electrode. All conditions are described with the aid of examples.     

Fabrication of photo-encoded beads for bioanalysis

Encoding large libraries of biomolecules is important to the applications such as immunoassay, drug screening and so on. By now a number of encoding schemes have been proposed and developed. In this paper, a new encoding approach was proposed based on the photonic crystal beads and an apparatus was developed for the fabrication. Encoded beads, with diameters in the range between 0.2 mm and 3 mm, were prepared using polymer and pearl dye. Pearl dye is a kind of photonic crystal, the color of which is from the ordered nanostructure. Such a colorizing mechanism makes the color of pearl dye much stable to high temperature, UV irradiation or longtime storage comparing with the conventional dyes.     

粘结剂对高电阻率各向异性粘结NdFeB磁体性能的影响

用于高频场下的永磁材料不仅要具有高的磁性能,还需要具备高电阻率,避免高频交变场在磁体表面产生涡流而导致致命温升.本文即通过分析几种粘接剂的起始粘度、不同温度下的粘度曲线等性能参数优选粘接剂,并采用正交试验的方法得到了最优的高电阻率各向异性粘结NdFeB成型工艺,所成型磁体在高频场的应用得到了验证.     

Partially Carbonized Polymer Binder with Polymer Dots for Silicon Anodes in Lithium-Ion Batteries

Large-scale applications of conventional conductive binders for silicon (Si) anodes are challenging to accomplish due to their complex synthesis steps and high cost. Herein, a carbonized polymer dots-assisted polyvinyl alcohol-chitosan (PVA-CS-CPDs) binder is developed through a simple and low-cost hydrothermal method. Through rational design, the PVA-CS-CPDs binder retains rich polar groups while forming conjugated structures. The conjugated structure endows the PVA-CS-CPDs with high electronic conductivity, and the retained polar groups maintain strong binding strength. The proposed water-soluble binding system acts as both a binder and conductive additive, enabling stable cycling for high-Si-content (90 wt.%) anodes without any other conductive additives.     

MIM粘结剂中聚合物性质的估算

介绍了金属注射成形中一些聚合物性质的估算方法，并探讨了一些粘结剂的表面性能。     

Facile one-pot synthesis of iron oxide nanoparticles cross-linked magnetic poly(vinyl alcohol) gel beads for drug delivery

In this paper, a facile one-pot strategy for scalable synthesis of robust magnetic poly(vinyl alcohol) (mPVA) gel beads is developed. Through dropwise addition of mixed aqueous solution of iron salts and PVA solution into alkaline (e.g., ammonia, NaOH, and KOH) solution, mPVA gel beads with uniform size and excellent superparamagnetic property can be fabricated based on the simultaneous formation of magnetic iron oxide nanoparticles (MIONs) and cross-link of PVA chains. Moreover, this approach can be extended to prepare dual- or multiresponsive gel beads through simply adding functional fillers into PVA solution (e.g., mPVA-PNIPAM gel beads that possess both magnetic and temperature responsibilities can be readily prepared by adding temperature responsive poly(N-isopropylacrylamide) (PNIPAM) into PVA solution). It is found that that the obtained mPVA gel beads exhibit high drug loading level (e.g., above 70%) after the treatment of freezing-thawing. Drug release experiments reveal that the drug release rate and amount of the mPVA gel beads can be tuned by operating the external magnetic field and adjusting the concentration of iron oxide nanoparticles and temperature (for mPVA-PNIPAM gel beads). The present work is of interest for opening up enormous opportunities to make full use of magnetic gel beads in drug delivery and other applications, because of their facile availability, cost-effective productivity, and tunable drug release performance.