Camptothecin in sterically stabilized phospholipid nano-micelles: a novel solvent pH change solubilization method

Camptothecin (CPT) is a topoisomerase I inhibitor that acts against a broad spectrum of cancers. Unfortunately clinical application of CPT is limited by insolubility, instability, and toxicity problems. To circumvent these delivery problems of CPT, we propose biocompatible, targeted sterically stabilized micelles (SSM) as nanocarriers for CPT (CPT-SSM). SSM composed of polyethylene glycol (PEGylated) phospholipids are attractive nanocarriers for CPT delivery because they are sufficiently small to extravasate through the leaky microvasculature of tumor and inflamed tissues for passive targeting. The purpose of this study was to develop a novel method of preparing CPT-SSM based on its pH dependent, reversible carboxylate-lactone conversion chemistry. CPT carboxylate was added to SSM at pH 5 that favored the formation of active but hydrophobic CPT lactone for spontaneous association with SSM. The kinetics of CPT conversion and CPT-SSM formation, and the effect of varying CPT-PEGylated phospholipid molar ratio on CPT-SSM properties and CPT solubilization were evaluated. CPT converted gradually from the carboxylate form to lactone, and CPT-SSM were formed after 12 h incubation. The mean size of CPT-SSM was approximately 14 nm. CPT solubilization (approximately 12 microg/ml) and other CPT-SSM micelle properties did not change significantly with increasing CPT to PEGylated hospholipid molar ratios using this novel method, unlike the coprecipitation/reconstitution technique previously reported. This reproducible CPT solubilization in SSM was attributed to avoidance of drug aggregate formation by this method. The advantages of our solvent pH change method to prepare CPT-SSM support further investigations of this approach to other hydrophobic drugs similar to CPT in chemistry and also CPT molecular solubilization in other nanocarriers.     

GISAXS analysis of 3D nanoparticle assemblies--effect of vertical nanoparticle ordering

We report on grazing-incidence small-angle x-ray scattering (GISAXS) study of 3D nanoparticle arrays prepared by two different methods from colloidal solutions-layer-by-layer Langmuir-Schaefer deposition and spontaneous self-assembling during the solvent evaporation. GISAXS results are evaluated within the distorted wave Born approximation (DWBA) considering the multiple scattering effects and employing a simplified multilayer model to reduce the computing time. In the model, particular layers are represented by nanoparticle chains where the positions of individual nanoparticles are generated following a model of cumulative disorder. The nanoparticle size dispersion is considered as well. Three model cases are distinguished-no shift between the neighboring chains (AA stacking), a shift equal to half of the mean interparticle distance (AB stacking) and random shift between the chains. The first two cases correspond to vertically correlated nanoparticle positions across different chains. A comparison of the experimental GISAXS patterns with the model cases enabled us to distinguish important differences between the 3D arrays prepared by the two methods. In particular, laterally ordered layers without vertical correlation of the nanoparticle positions were found in the nanoparticle multilayers prepared by the Langmuir-Schaefer method. On the other hand, the solvent evaporation under particular conditions produced highly ordered 3D nanoparticle assemblies where both laterally and vertically correlated nanoparticle positions were found.     

Grain velocity distribution in a mixed flow dryer

For corn drying one of the most popular possibilities in Europe is to use a mixed flow dryer. Large differences in the vertical grain particle velocity in this type of dryers are causing differences in the residence time. Hence, uneven drying occurs causing under-drying or over-drying of grain portions. To investigate the influences of the dryer walls and the air ducts on the particle velocity distribution experiments have been carried out in industrial and laboratory sized dryers and the measurements were compared with discrete element models. The particle flow velocity distribution between the air ducts is modelled analytically based on arching hypothesis. Using discrete element models the effects of different possible constructional modifications causing more even vertical grain particle velocity distribution were analyzed.     

Mint and pomegranate extracts/oils as antibacterial agents against Escherichia coli O157:H7 and Listeria monocytogenes on shredded carrots

Among minimally processed vegetables, shredded carrots are particularly popular. The aim of this study was to evaluate the antimicrobial activity of different washing treatments with aqueous solutions of mint essential oil (EO) (1:1000), mint hydrosol (1:10), and pomegranate juice (1:10) against two major foodborne pathogens on shredded carrots as well as their effect on carrot's quality. The results of this study indicate that the tested washing treatments resulted in a small but significant decrease of the microbial load of Escherichia coli and Listeria monocytogenes on the sixth day of storage. Pomegranate juice and mint hydrosol were more effective against L.   monocytogenes, whereas mint EO was more effective against E.   coli. Furthermore, an increase in carrot's total phenolics and antioxidants was observed with the application of mint hydrosol and pomegranate juice, whereas mint EO resulted in a decrease on the sixth day of storage. Additionally, a decreased chroma of the shredded carrots were observed during the application of mint hydrosol on the sixth day. Total carotenoids, ascorbic acid, total soluble solids, and tritratable acidity were not differing after six days of storage of shredded carrots. These washing products can be used for the partial disinfection of shredded carrots.

Practical applications

Pomegranate and mint natural products solution can be used for the partial disinfection of minimally processed fresh produce as an alternative to chlorine, and these products can be a part of the sanitation process.     

Multi-objective optimization of skeletal structures under static and seismic loading conditions

Almost every real world problem involves simultaneous optimization of several incommensurable and often competing objectives which constitutes a multi-objective optimization problem. In multi-objective optimization problems the optimal solution is not unique as in single-objective optimization problems. This paper is concerned with large-scale structural optimization of skeletal structures such as space frames and trusses, under static and/or seismic loading conditions with multiple objectives. Combinatorial optimization methods and in particular algorithms based on evolution strategies are implemented for the solution of this type of problems. In treating seismic loading conditions a number of accelerograms are produced from the elastic design response spectrum of the region. These accelerograms constitute the multiple loading conditions under which the structures are optimally designed. This approach for treating seismic loading is compared with an approximate design approach, based on simplifications adopted by the seismic codes, in the framework of multi-objective optimization.     

Studies on polyethylene oxide and phenolic resin blends

Blends of poly(ethylene oxide) (PEO) and novolac type phenolic resin were prepared by a solution cast method using acetonitrile as a solvent. In this work, we have investigated the PEO/phenolic blends having low phenolic content (0 to 30 wt %) with the objective in mind to design a crystallizable component for a shape memory polymer system having adjustable switching temperature. The blends were characterized by Fourier transform infrared (FTIR) spectroscopy, polarized optical microscopy (POM), and differential scanning calorimetry (DSC). The rate of crystallization and crystallinity (calculated from heat of crystallization value) decrease with increase in novolac content. FTIR analysis indicates the existence of H‐bonding between hydroxyl groups of novolac and ether groups of PEO. POM studies indicate that size of Maltese cross section decreases with increase in novolac content and in the blends containing higher novolac content less regular leaf like texture was obtained. © 2008 Wiley Periodicals, Inc. J Appl Polym Sci, 2008     

Biomimetically synthesized silica-carbon nanofiber architectures for the development of highly stable electrochemical biosensor systems

Biomimetically synthesized silica and conductive activated carbon nanofibers (CNFs) are used in a synergistic manner for the development of a novel electrochemical biosensor system. Poly(L-lysine) templated silica grows and encapsulates the CNF-immobilized enzyme generating a highly stabilizing nanostructured environment for the underlying protein. Concurrently, CNFs provide both the required surface area for the high-capacity enzyme immobilization required in biosensors as well as direct electron transfer to the inner platinum transducer. As a result, this silica/nanofiber superstructure is an ideal architecture for the development of electrochemical biosensor systems that can withstand exposure to extreme operational conditions, such as high temperatures or the presence of proteases. Acetylcholine esterase is used as the model catalyst and with the aid of spectroscopic data it is shown that the observed high operational stability of the biosensor is due to the direct interaction of the protein with the silica backbone, as well as due to the nanostructured enzyme confinement.     

Direct evidence for covalent functionalization of carbon nanohorns by high-resolution electron microscopy imaging of C60 conjugated onto their skeleton

Carbon nanohorns (CNHs) functionalized with aryl units, possessing ethylene glycol chains terminated to amine groups, were condensed with modified C₆₀ carrying a free carboxylic acid group. Direct evidence for the covalent functionalization of CNHs was given by high-resolution transmission electron microscopy (HR-TEM) imaging of C₆₀ present in that CNH hybrid material. In addition, it was found that C₆₀ remained unaffected even after prolonged exposure to the electron beam. Finally, monitoring the wave motion of the connecting ethylene glycol chains, through sequential HR-TEM images, further proved the stability of the covalent bond that links the two carbon nanostructures.     

Structure and properties of amine‐hardened epoxy/benzoxazine hybrids: Effect of epoxy resin functionality

Bifunctional, trifunctional, and tetrafunctional epoxy resins (EP) were hardened with stoichiometric amount of 4,4′‐diaminodiphenyl methane in presence and absence of benzoxazine (BOX). The EP/BOX ratio of the hybrid systems was 100/0, 75/25, 50/50, and 25/75 wt %, respectively. Information on the structure of the hybrid systems was received from differential scanning calorimetry, dynamic‐mechanical thermal analysis, atomic force microscopy, and fractographic studies. The flexural and fracture mechanical properties of the EP/BOX hybrids were determined and compared to those of the reference EPs. The thermal degradation and fire resistance of the hybrids were also studied. It was found that the polymerized BOX was built in the network in from of nanoscale inclusions and acted as antiplasticizer. Incorporation of BOX enhanced the flexural modulus and strength and reduced the glass transition temperature of the parent EP. The fracture toughness and energy were practically not improved by hybridization with BOX. The charring and flame resistance were improved with increasing amount of BOX in the EP/BOX hybrids. The relative improvement in the latter was most prominent for the bifunctional EP/BOX systems. © 2011 Wiley Periodicals, Inc. J Appl Polym Sci, 2012