Efficient loading and entrapment of tamoxifen in human serum albumin based nanoparticulate delivery system by a modified desolvation technique

Herein, the poorly water-soluble drug, Tamoxifen (Tmx), was loaded in the amphipathic matrix of human serum albumin (HSA) nanoparticles by a modified desolvation method. In order to enhance the drug loading (DL) and drug entrapment efficiency (DEE) (<2% and 10%, respectively), ultrasonication of Tmx-HSA mixture was performed prior to desolvation process. Tmx loading and entrapment efficiency were optimized by employment of the response surface methodology (RSM)-central composite design (CCD) of experiments. Under the optimum conditions of 1.59 mg Tmx/ml concentration, 7.76 pH and 5 h incubation of HSA-Tmx, the DL of 6.7% and DEE of 74% are achievable. Particles with the average size of 195 nm, zeta potential of −21 mV and polydispersity index of 0.09 were produced under these conditions. A more sustained Tmx release behavior was observed from polyethylene glycol (PEG) conjugated nanoparticles in comparison to the non-PEGylated ones. The short-term stability investigation showed no alteration in physicochemical properties of nanoparticles at 4 and 37 °C, but small increase in nanoparticles size was observed after three months of storage at room temperature. This is the first report for efficient production of a Tmx delivery system based on HSA nanoparticles.     

Structural and magnetic properties of erbium doped nanocrystalline Li–Ni ferrites

A series of nanocrystalline Li_0.25Ni_0.5Fe_2.25−xEr_xO₄ (x=0.00, 0.02, 0.06, 0.08, and 0.10) ferrite powders, having a cubic spinel crystal structure and a low value of coercivity, was synthesized by the sol–gel auto-combustion route. The structure, morphology and magnetic properties of the prepared nanoferrites were characterized by powder X-ray diffraction (XRD), scanning electron microscopy (SEM), transmission electron microscopy (TEM), and the magnetic property measurement system (MPMS). A well-defined single phase spinel structure is confirmed in all the samples by X-ray diffraction analysis. The lattice parameters of the samples increase slightly with increasing the erbium content. The crystallite size of the Er-doped samples is smaller than that of pure Li–Ni ferrite, and decrease regularly in the range of 36.0–14.5 nm. It has been observed that the magnetic properties of these ferrites are strongly influenced by the added erbium content. The magnetic measurements indicate that saturation magnetization (M_s) and coercivity (H_c) decrease gradually with the increase of Er content in the lattice.     

Performance analysis of three advanced controllers for polymerization batch reactor: An experimental investigation

The performances of three advanced non-linear controllers are analyzed for the optimal set point tracking of styrene free radical polymerization (FRP) in batch reactors. The three controllers are the artificial neural network-based MPC (NN-MPC), the artificial fuzzy logic controller (FLC) as well as the generic model controller (GMC). A recently developed hybrid model (Hosen et al., 2011a. Asia-Pac. J. Chem. Eng. 6(2), 274) is utilized in the control study to design and tune the proposed controllers. The optimal minimum temperature profiles are determined using the Hamiltonian maximum principle. Different types of disturbances are introduced and applied to examine the stability of controller performance. The experimental studies revealed that the performance of the NN-MPC is superior to that of FLC and GMC.     

Tepary Bean Starch Part III: In vitro Digestibility

In vitro digestibility of starch from tepary bean, Phaseolus acutifolius var. latifolius, was determined in comparison with tepary bean flour and maize starch. The extent of sample hydrolysis by α-amylase was measured as mg reducing sugar (maltose) released per 100 mg substrate. After 2 h incubation at 37°C, values obtained for tepary starch, tepary flour and maize starch treated in various ways were as follows: raw 8.0, 8.6 and 25.6; freeze dried 2.6, 3.2 and 17.8; autoclaved 7.4, 5.7 and 27.7; cooked (15 min) 81.7, 23.1 and 87.8; resp. Raw tepary starch was more resistant to hydrolysis than maize starch due, perhaps, to differences in granule structure and amylose content. Freeze-drying and autoclaving slightly decreased digestibility of both tepary starch and flour. Cooking greatly increased susceptibility to hydrolysis for each substrate. The rate of increase was reduced after 15 min exposure to enzymes, and no appreciable difference was found between cooked tepary and maize starches.     

pH Responsive Abelmoschus esculentus Mucilage and Administration of Methotrexate: In-Vitro Antitumor and In-Vivo Toxicity Evaluation

The rapid progression in biomaterial nanotechnology apprehends the potential of non-toxic and potent polysaccharide delivery modules to overcome oral chemotherapeutic challenges. The present study is aimed to design, fabricate and characterize polysaccharide nanoparticles for methotrexate (MTX) delivery. The nanoparticles (NPs) were prepared by Abelmoschus esculentus mucilage (AEM) and chitosan (CS) by the modified coacervation method, followed by ultra-sonification. The NPs showed much better pharmaceutical properties with a spherical shape and smooth surface of 213.4–254.2 nm with PDI ranging between 0.279–0.485 size with entrapment efficiency varying from 42.08 ± 1.2 to 72.23 ± 2.0. The results revealed NPs to possess positive zeta potential and a low polydispersity index (PDI). The in-vitro drug release showed a sustained release of the drug up to 32 h with pH-dependence. Blank AEM -CS NPs showed no in-vivo toxicity for a time duration of 14 days, accompanied by high cytotoxic effects of optimized MTX loaded NPs against MCF-7 and MD-MBA231 cells by MTT assay. In conclusion, the findings advocated the therapeutic potential of AEM/CS NPs as an efficacious tool, offering a new perspective for pH-responsive routing of anticancer drugs with tumor cells as a target.     

A collaborative approach for urban underground space development toward sustainable development goals: Critical dimensions and future directions

The utilization of urban underground space (UUS) offers an effective solution to urban problems but may also negatively affect urban development. Therefore, UUS development needs better concerted guidelines to coordinate various urban systems and the multiple components of the underground world. Sustainable Development Goals (SDGs), which should be viewed as important yardsticks for UUS development, do not explicitly mention urban underground space, although many of them are affected by both the positive and negative consequences of its development. To fill this gap, this review lays the foundations of relevant UUS concepts and uses exemplary cases to reveal that 11 out of 17 SDGs can be linked with UUS uses. These linkages also manifest that land administration, integrated planning, architectural design, and construction technology are critical dimensions for increasing the contributions of UUS to the realization of SDGs. To achieve multi-disciplinary synergies among these four critical dimensions, a collaborative approach framework based on spatial data infrastructure is required. Thus, this work provides academics and practitioners with a holistic view of sustainable UUS development.     

Biofilm and Small Colony Variants—An Update on Staphylococcus aureus Strategies toward Drug Resistance

Recently, the drawbacks arising from the overuse of antibiotics have drawn growing public attention. Among them, drug-resistance (DR) and even multidrug-resistance (MDR) pose significant challenges in clinical practice. As a representative of a DR or MDR pathogen, Staphylococcus aureus can cause diversity of infections related to different organs, and can survive or adapt to the diverse hostile environments by switching into other phenotypes, including biofilm and small colony variants (SCVs), with altered physiologic or metabolic characteristics. In this review, we briefly describe the development of the DR/MDR as well as the classical mechanisms (accumulation of the resistant genes). Moreover, we use multidimensional scaling analysis to evaluate the MDR relevant hotspots in the recent published reports. Furthermore, we mainly focus on the possible non-classical resistance mechanisms triggered by the two important alternative phenotypes of the S. aureus, biofilm and SCVs, which are fundamentally caused by the different global regulation of the S. aureus population, such as the main quorum-sensing (QS) and agr system and its coordinated regulated factors, such as the SarA family proteins and the alternative sigma factor σB (SigB). Both the biofilm and the SCVs are able to escape from the host immune response, and resist the therapeutic effects of antibiotics through the physical or the biological barriers, and become less sensitive to some antibiotics by the dormant state with the limited metabolisms.     

New syntheses of pyrazolo[3,4-d]pyrimidine,pyrazolo[3,4-d]pyridazine,isoindolinedione and pyrazole derivatives

Phenacylmalononitriles 2 react with hydrazines, acetic-hydrochloric acid and with diazotised primary aromatic amines to afford phenacylpyrazole ( 5a,b ), aminofurans ( 6a,b ) and aminopyrazole derivatives ( 3a,d ) respectively. The synthesised derivatives ( 3d, 6a ) were the key materials for the synthesis of isoindolinedione, ( 7a – c ) pyrazolopyrimidine ( 9, 10 ), and pyrazolopyridazine derivatives ( 11 ). The structures of the newly synthesised heterocycles were established on the basis of elemental analyses and spectral data besides synthesis via other routes.     

Recent Developments in Predicting Impact and Shock Sensitivities of Energetic Materials （英）

Empirical, quantum mechanical and artificial neural network methods are three usual methods in recent years that were used to predict sensitivity of different classes of high explosives. Some recent developments in predicting sensitivity by various methods are reviewed and discussed for various classes of energetic materials.