Borosilicate nanoparticles prepared by exothermic phase separation

Nanoparticles play an important role in chemical and biological sciences due to their ability to bind and concentrate many molecules on their surface. Polymers and silica are widely used to make nanoparticles, but efforts to make nanoparticles from borosilicate glass--which exhibits high tolerance to chemicals and solvents, combined with excellent mechanical and thermal stability--have proved unsuccessful. Here we show that borosilicate nanoparticles (100-500 nm in size) can be synthesized by simply mixing a silicon-boron binary oxide solution, prepared using non-aqueous organic solvents, with water. This induces a vigorous exothermic phase separation in which borosilicate nanoparticles burst out of a silica phase. In addition to potential applications in the life sciences, monodisperse borosilicate particles could also have applications in the production of photonic bandgap devices with high optical contrast, contrast agents for ultrasonic microscopy or chemical filtration membranes.     

Injectable sustained release PLA microparticles prepared by solvent evaporation-media milling technology

The objective of this study was to develop agomelatine (AGM) intramuscular sustained release PLA microparticles by using solvent evaporation combined with wet milling technology. The final preparation had a regular and homogeneous particle size of approximately 35?µm, as measured by laser diffraction particle size analysis and scanning electron microscopy (SEM). The drug was confirmed to be within the carrier in an amorphous state through differential scanning calorimetry (DSC) and power X-ray diffraction (PXRD) experiments. Additionally, Fourier transform infrared spectroscopy (FT-IR) analysis was applied to confirm that there was hydrogen bonding between the drug and polymer at the molecular level. In vitro release experiments indicated that the drug could achieve long-term sustained release over the period of one month, with only a 3.07% burst release, due to the involvement of the polymer and removal of drug adsorbed on the surface during the wet grinding process. The dominant release mechanism was considered to be diffusion of the drugs in the initial period. Following this, with the hydrolysis of PLA to form a colloidal viscous layer, drug release is due to the combined effect of diffusion and erosion of the polymer matrix. Additionally, drug release behavior is closely related to the degradation mechanism of the polymer carrier. The results suggest that AGM could be developed as a potential delivery system for long-acting intramuscular administration with extensive application prospects.     

Direct encapsulation of water-soluble drug into silica microcapsules for sustained release applications

Direct encapsulation of water-soluble drug into silica microcapsules was facilely achieved by a sol-gel process of tetraethoxysilane (TEOS) in W/O emulsion with hydrochloric acid (HCl) aqueous solution containing Tween 80 and drug as well as cyclohexane solution containing Span 80. Two water-soluble drugs of gentamicin sulphate (GS) and salbutamol sulphate (SS) were chosen as model drugs. The characterization of drug encapsulated silica microcapsules by scanning electronic microscopy (SEM), FTIR, thermogravimetry (TG) and N₂ adsorption-desorption analyses indicated that drug was successfully entrapped into silica microcapsules. The as-prepared silica microcapsules were uniform spherical particles with hollow structure, good dispersion and a size of 5-10 μm, and had a specific surface area of about 306 m²/g. UV-vis and thermogravimetry (TG) analyses were performed to determine the amount of drug encapsulated in the microcapsules. The BJH pore size distribution (PSD) of silica microcapsules before and after removing drug was examined. In vitro release behavior of drug in simulated body fluid (SBF) revealed that such system exhibited excellent sustained release properties.     

Characteristics and release property of polylactic acid/sodium monofluorophosphate microcapsules prepared by spray drying

Microcapsules composed of polylactic acid (PLA)/corrosion inhibitor sodium monofluorophosphate (MFP) were prepared by spray drying, and the effects of processing parameters on the morphology and encapsulation efficiency of the microcapsules were investigated. The results showed that low viscous PLA solution only resulted in porous microcapsules with low encapsulation efficiency, whereas filamentous substances were produced instead of microcapsules once PLA solution content exceeded 5%. When spray pressure exceeded 0.4 MPa, the microcapsule surface was wrinkled due to high evaporation rate of the atomized droplets. The spray pressure less than 0.3 MPa created larger atomized droplets and yielded the adhesive microcapsules with lower encapsulation efficiency. The optimal emulsion parameters were as follows: PLA concentration, 5%; water-oil ratio, 1:9; inlet air temperature, 50 °C; and spray pressure, 0.4 MPa. The resulting microcapsules exhibited a good sustained-release behavior in a simulated concrete pore solution.     

湿相分离制备可生物降解壳聚糖膜的研究

采用湿相分离法制备壳聚糖膜.主要研究成型条件对壳聚糖膜力学性能和膜形态结构的影响.结果表明:用氢氧化钠和无水硫酸钠的双组分凝固浴和适当的热处理可获得具有良好力学性能和内部结构的壳聚糖膜.当双组分凝固浴浓度为6%NaOH-1.2%Na2SO4,凝固时间为6h时,制得的壳聚糖膜的拉伸强度可达到12.44MPa.     

Kinetics of drug release from isonicotinic acid hydrazide microcapsules

Abstract

Isonicotinic acid hydrazide is encapsulated by emulsification - solvent evaporation technique using Eudragit RS 100 as coating polymer.An empirical relationship between drug loading and drug diffusibility through the polymer matrix was developed.     

Kinetics of drug release from isonicotinic acid hydrazide microcapsules

Isonicotinic acid hydrazide is encapsulated by emulsification - solvent evaporation technique using Eudragit RS 100 as coating polymer.An empirical relationship between drug loading and drug diffusibility through the polymer matrix was developed.     

Polyelectrolyte microcapsules for sustained delivery of water-soluble drugs

Polyelectrolyte capsules composed of weak polyelectrolytes are introduced as a simple and efficient system for spontaneous encapsulation of low molecular weight water-soluble drugs. Polyelectrolyte capsules were prepared by layer-by-layer (LbL) assembling of weak polyelectrolytes, poly(allylamine hydrochloride) (PAH) and poly(methacrylic acid) (PMA) on polystyrene sulfonate (PSS) doped CaCO₃ particles followed by core removal with ethylene-diaminetetraacetic acid (EDTA). The loading process was observed by confocal laser scanning microscopy (CLSM) using tetramethylrhodamineisothiocyanate labeled dextran (TRITC-dextran) as a fluorescent probe. The intensity of fluorescent probe inside the capsule decreased with increase in cross-linking time. Ciprofloxacin hydrochloride (a model water-soluble drug) was spontaneously deposited into PAH/PMA capsules and their morphological changes were investigated by scanning electron microscopy (SEM) and atomic force microscopy (AFM). The quantitative study of drug loading was also elucidated which showed that drug loading increased with initial drug concentration, but decreased with increase in pH. The loaded drug was released in a sustained manner for 6 h, which could be further extended by cross-linking the capsule wall. The released drug showed significant antibacterial activity against E. coli. These findings indicate that such capsules can be potential carriers for water-soluble drugs in sustained/controlled drug delivery applications.     

Morphologies and release behavior of polyurea microcapsules from different polyisocyanates

Polyurea microcapsules were prepared by emulsion polymerization after adding an aqueous solution with poly(vinyl alcohol) as protective colloid into an organic solution with migrin oil as core material, 1,4-diamino anthraquinone (DAA) as penetrator, and different molar ratios of isophorone diisocyanates (IPDI) and toluene diisocyanates (TDI) as wall materials. The effects of diisocyanate types on the morphologies and release behavior of the resultant microcapsules were investigated. The transmittance (%) of the completely dissolved microcapsule in dimethyl acetamide (DMAc) by UV/visible spectrophotometer decreased with the content of aliphatic IPDI in the wall by increasing the wall thickness due to its inferior reactivity compared to aromatic TDI. Also in SEM images, these polyurea microcapsules from higher TDI content had rougher surfaces. In conclusion, the release profiles of the microcapsules in extraction solution showed that release rate of DAA depended on the roughness of the microcapsules.     

原位聚合法制备相变储热微胶囊

以三聚氰胺-甲醛为壁材,十二醇为囊芯,采用原位聚合法制备了相变储热微胶囊。采用SEM、DSC、FTIR、激光粒径分布仪等测试仪器分别测定微胶囊形态、热性能、化学成分以及粒径分布;采用光学显微镜二次聚焦法测定微胶囊的壁厚,并讨论微胶囊壁厚的影响因素。实验结果表明,当壁材／芯材用量比为1：2时,在3000r／min的乳化转速下乳化10min,80℃时固化1h制备的微胶囊粒径分布均匀,平均粒径〈10μm,且表面光洁;微胶囊壁厚随乳化转数增加而减小,而囊芯比对壁厚影响并不显著;DSC显示相变材料微胶囊化后并不影响其相变点,相变储热效果明显。     

Sustained release of doxorubicin from zeolite-magnetite nanocomposites prepared by mechanical activation

Nanocomposites consisting of magnetite and FAU zeolite with a high surface area and adsorption capacity have been prepared by mechanical activation using high-energy milling at room temperature. FTIR results, as well as HRTEM, EFTEM, and XPS measurements, show that the resulting magnetic nanoparticles are covered by a thin aluminosilicate coating. A saturation magnetization as high as 16?emu?g(-1) and 94.2?Oe of coercivity were observed for the obtained composites. The main advantages of this synthesis procedure are (i) simplicity of the preparation procedure, (ii) prevention of agglomeration of the magnetite nanoparticles to a large extent, and (iii)?absence of free magnetite outside the zeolitic matrix. In addition, in vitro experiments revealed that the nanoparticles prepared were able to store and release substantial amounts of doxorubicin. In view of these advantages, these magnetic nanoparticles can be considered as potential candidates for drug-delivery applications.     

Molecularly imprinted nanoparticles prepared by miniemulsion polymerization as selective receptors and new carriers for the sustained release of carbamazepine

Water-compatible imprinted nanoparticles were prepared for carbamazepine as a template and used for the selective extraction and controlled release of carbamazepine. Assay materials and drug delivery carriers were typically used in aqueous environments, so it is generally preferable to prepare solvent-free molecularly imprinted nanoparticles in water using the miniemulsion polymerization method. The present work investigates a bio-analytical strategy generically applicable to imprinted materials for molecular recognition studies, including equilibrium and non-equilibrium binding, and release experiments, increasing the knowledge of the molecular interactions between the template molecules and imprinted nanoparticles. The results showed that the imprinted nanoparticles exhibited a higher binding level and slower release rate than non-imprinted nanoparticles. The selectivity of imprinted nanoparticles for carbamazepine studied in comparison with an analogue compound, oxcarbazepine, the main metabolite of carbamazepine. The recovery and selectivity of carbamazepine in human serum was determined to be 100%, 1.7 times that of oxcarbazepine. The results indicated that carbamazepine-imprinted nanoparticles are appropriate for serum level determination of the drug in therapeutic range. The template to functional monomer ratio as a key factor controlling the recognition and release kinetic mechanism of imprinted nanoparticles is discussed. The imprinted nanoparticles prepared at the appropriate template to functional monomer mole ratio (2:8) exhibited the best drug affinity (5.1 times higher) and a slower drug release rate due to the interaction of carbamazepine with the imprinted cavities within the nanoparticles. Loaded imprinted nanoparticles as drug reservoirs were able to prolong carbamazepine release, in 1% wt sodium dodecyl sulfate aqueous solution, for more than 8 days.     

Dual cross-linked chitosan microspheres formulated with spray-drying technique for the sustained release of levofloxacin

Objective: This study was aimed to develop sustained drug release from levofloxacin (LF)-loaded chitosan (CS) microspheres for treating ophthalmic infections.

Significance: Dual cross-linked CS microspheres developed by the spray-drying technique displays significantly higher level of sustained drug release compared with non-cross-linked CS microspheres.

Methods: LF-loaded CS microspheres were prepared using the spray-drying technique, and then solidified with tripolyphosphate and glutaraldehyde as dual cross-linking agents. The microspheres were characterized by surface morphology, size distribution, zeta potential, encapsulation efficiency, and drug release profiles in vitro. The drug quantification was verified and analyzed by high-performance liquid chromatography (HPLC). The structural interactions of the CS with LF were studied with Fourier transform infrared spectroscopy. The effect of various influencing excipients in the formulation of the dual cross-linked CS microspheres on drug encapsulation efficiency and the drug release profiles were extensively investigated.

Result: The microspheres demonstrated high encapsulation efficiency (72.4?～?98.55%) and were uniformly spherical with wrinkled surface. The mean particle size was between 1020.7?±?101.9 and 2381.2?±?101.6?nm. All microspheres were positively charged (zeta potential ranged from 31.1?±?1.32 to 42.81?±?1.55?mV). The in vitro release profiles showed a sustained release of the drug and it was remarkably influenced by the cross-linking process.

Conclusion: This novel spray-drying technique we have developed is suitable for manufacturing LF-loaded CS microspheres, and thus could serve as a potential platform for sustained drug release for effective therapeutic application in ocular infections.     

超滤法分离丹皮多糖的研究

采用超滤法分离丹皮多糖,研究了超滤膜的选择、预处理方法以及温度、压力各因素对超滤分离结果的影响,优化了超滤分离丹皮多糖的工艺参数.采用本实验工艺,对丹皮多糖的截留率达到92.91%,多糖制品的纯度达到84.2%,说明超滤是分离浓缩丹皮多糖的有效手段之一.     

液相电沉积类金刚石薄膜的组成及结构分析

利用液相电沉积的方法，从乙腈中在硅片上沉积非晶碳薄膜，首次发现了电流密度随反应时间呈波动变化的规律。红外光谱和拉曼光谱分析表明所得薄膜是一种典型的含氢类金刚石薄膜(a-C：H薄膜)，并用高斯分解的方法对非晶碳薄膜的拉曼光谱和X射线光电子能谱进行定量分析，从而确定这种a-C：H薄膜中sp^3的相对含量为30％～35％。     

Ibuprofen agglomerates preparation by phase separation

The compression ability and dissolution rate of ibuprofen are poor. There are many processes to optimize these properties through adapted formulations. However, it would be more satisfactory to obtain directly during the crystallization step crystalline particles that can be directly compressed and quickly dissolved. This was the aim of this work. Ibuprofen spherical agglomerates were obtained using a very simple method based on the difference of solubility of ibuprofen in ethanol and in water. By cooling down an ibuprofen-saturated solution in an ethanol/water 50/50 mixture from 60°C to room temperature under stirring, a phase separation occurs. Ibuprofen crystallizes in separated water droplets. After separation by sieving and drying, spherical agglomerates were obtained. A study of the physical properties of ibuprofen agglomerates was carried out using electron scanning microscopy and X-ray powder diffraction. The compression ability was tested using an instrumented tablet machine, and the dissolution rate was measured using continuous flow cells. An improvement in compression and dissolution properties of the spherical agglomerates produced was observed. The process of crystallization in a separated dispersed phase could be envisaged each time a drug exhibits opposite solubilities in two miscible solvents.     

Investigation of hypromellose particle size effects on drug release from sustained release hydrophilic matrix tablets

Selected combinations of six model drugs and four hypromellose (USP 2208) viscosity grades were studied utilizing direct compression and in vitro dissolution testing. Experimental HPMC samples with differing particle size distributions (coarse, fine, narrow, bimodal) were generated by sieving. For some formulations, the impact of HPMC particle size changes was characterized by faster drug release and an apparent shift in drug release mechanism when less than 50% of the HPMC passed through a 230 mesh (63 μm) screen. Within the ranges studied, drug release from other formulations appeared to be unaffected by HPMC particle size changes.