Dual Thermo‐ and pH‐Responsive Zwitterionic Sulfobataine Copolymers for Oral Delivery System

A novel oral delivery system consisting of thermoresponsive zwitterionic poly(sulfobetaine methacrylate) (PSBMA) and pH‐responsive poly(2‐(diisopropylamino)ethyl methacrylate) (PDPA) is synthesized via free radical polymerization. This copolymer can self‐aggregate into nanoparticles via electrostatic attraction between ammonium cation and sulfo‐anion of PSBMA and successfully encapsulate anticancer drug, curcumin (CUR), with highest loading content of 2.6% in the P(SBMA‐co‐DPA) nanoparticles. The stimuli‐responsive phase transition behaviors of P(SBMA‐co‐DPA) copolymers at different pH buffer solution show pH‐dependent upper critical solution temperature (UCST) attributed to the influence of protonation/deprotonation of the pH‐responsive DPA segments. Through the delicate adjustment of the PSBMA/PDPA molar ratios, the stimuli‐responsive phase transition could be suitable for physiological environment. The kinetic drug release profiles demonstrate that P(SBMA‐co‐DPA) nanoparticles have the potential as oral delivery carriers due to their effective release of entrapped drugs in the stimulated intestinal fluid and preventing the deterioration of drug in stimulated gastric fluid.

     

Modeling and solution of the joint quay crane and truck scheduling problem

This paper addresses the joint quay crane and truck scheduling problem at a container terminal, considering the coordination of the two types of equipment to reduce their idle time between performing two successive tasks. For the unidirectional flow problem with only inbound containers, in which trucks go back to quayside without carrying outbound containers, a mixed-integer linear programming model is formulated to minimize the makespan. Several valid inequalities and a property of the optimal solutions for the problem are derived, and two lower bounds are obtained. An improved Particle Swarm Optimization (PSO) algorithm is then developed to solve this problem, in which a new velocity updating strategy is incorporated to improve the solution quality. For small sized problems, we have compared the solutions of the proposed PSO with the optimal solutions obtained by solving the model using the CPLEX software. The solutions of the proposed PSO for large sized problems are compared to the two lower bounds because CPLEX could not solve the problem optimally in reasonable time. For the more general situation considering both inbound and outbound containers, trucks may go back to quayside with outbound containers. The model is extended to handle this problem with bidirectional flow. Experiment shows that the improved PSO proposed in this paper is efficient to solve the joint quay crane and truck scheduling problem.     

A mathematical model of inter-terminal transportation

We present a novel integer programming model for analyzing inter-terminal transportation (ITT) in new and expanding sea ports. ITT is the movement of containers between terminals (sea, rail or otherwise) within a port. ITT represents a significant source of delay for containers being transshipped, which costs ports money and affects a port’s reputation. Our model assists ports in analyzing the impact of new infrastructure, the placement of terminals, and ITT vehicle investments. We provide analysis of ITT at two ports, the port of Hamburg, Germany and the Maasvlakte 1 & 2 area of the port of Rotterdam, The Netherlands, in which we solve a vehicle flow combined with a multi-commodity container flow on a congestion based time–space graph to optimality. We introduce a two-step solution procedure that computes a relaxation of the overall ITT problem in order to find solutions faster. Our graph contains special structures to model the long term loading and unloading of vehicles, and our model is general enough to model a number of important real-world aspects of ITT, such as traffic congestion, penalized late container delivery, multiple ITT transportation modes, and port infrastructure modifications. We show that our model can scale to real-world sizes and provide ports with important information for their long term decision making.     

Purification,Characterization and N‐terminal Sequence Analysis of Betel Leaf (Piper betle) Invertase

The present study is the first report describing the purification, enzymatic properties and N‐terminal amino acid sequence of a native invertase in betel leaf. The invertase was purified as a monomeric glycoprotein of molecular mass (Mr) 68 kDa. The enzyme was capable to attack β‐fructofuranoside linkages from the fructose end of sucrose, raffinose and stachyose indicating it as an authentic β‐D‐fructofuranosidase with high specificity for sucrose (Km 4.83 mM). The maximum activity was detected at pH 5.2 and 37 °C. Glucose and fructose showed typical inhibitory effect on the enzyme activity where as lectin was found to be effective activators of the enzyme. Significant inhibition by heavy metal ion Hg²⁺ and sulfhydryl group modifying agents suggesting that free sulfhydryl group containing amino acid, cysteine is necessary for the catalytic activity of the invertase. A BLAST search of the N‐terminal amino acid sequence of betel leaf invertase showed significant homology with the homologous invertases in database.     

Threshold voltage for purely flexoelectric deformations of conducting homeotropic nematic layers

Elastic deformations induced by an electric field in homeotropic nematic layers with finite anchoring energy were studied numerically. A nematic material possessing flexoelectric properties and characterized by a positive dielectric anisotropy was considered. The ionic space charge and the ion transport across the layer were taken into account. The director orientation, the electric field strength and the ion concentrations were calculated as functions of the coordinate normal to the layer. The calculations show that the electric field distribution, which determines the form of the deformations, is influenced by the ionic current and therefore depends on the ionic content and on the properties of the electrodes. Several types of deformations were distinguished. When the electrode contacts are well conducting or when the ionic content is low, the threshold voltage is very close to the value U _f valid for an insulating nematic. When the electrodes are poorly conducting or blocking at high ion concentration, the threshold voltage decreases much below U _f. At moderate ion concentrations, i.e. between 10¹⁹ and 10²⁰ m^?3, two different behaviours were found depending on the sign of the sum of flexoelectric coefficients e ₁₁+e ₃₃. In the case of e ₁₁+e ₃₃<0, the threshold voltage decreases with the ionic content; in the case of e ₁₁+e ₃₃>0, the deformations occur in two separate voltage regimes. They arise above a certain threshold voltage, disappear at some higher voltage and reappear at an even higher threshold.     

Synthesis of the Upstream Terminal Disaccharide of the O-Antigenic Polysaccharide of Vibrio cholerae O37

The terminal disaccharide of the O-antigenic polysaccharide of Vibrio cholerae O37, 4-O-methyl-α-D-QuiNAc-(1→4)-α-d-QuiNAc, was synthesized as methyl glycoside involving glycosylation between glycosyl donor ethyl 2-azido-3-O-benzyl-2,6-dideoxy-4-O-methyl-6-iodo-1-thio-α-d-glucopyranoside and glycosyl acceptor methyl 2-azido-3-O-benzyl-2,6-dideoxy-6-iodo-α-d-glucopyranoside. Dehalogenation, global deprotection, and reduction of the azide to amine were effected in one step by catalytic hydrogenation. It was followed by selective N-acetylation to give the desired deprotected disaccharide.     

Graft Polymerization of a Polymer Matrix: Grafting of Tetrafluoroethylene

Graft polymerization of tetrafluoroethylene on polyethylene preirradiated by γ-rays from a cobalt-60 source at ?196°C has been investigated in the region of PE devitrification. A calorimetric technique made it possible to establish that 1.5-2% of monomer dissolves in the amorphous regions of PE at low temperatures. Efficient grafting proceeds in the temperature range directly adjoining the PE devitrification region. The graft copolymer yield amounts to ca. 1200%. The intensification of grafting is apparently caused by the following: (1) because of previous solution of TFE in the PE amorphous regions and filling of the micropores, the reaction in the initial stage is not limited by diffusion; (2) and the initiation efficiency is increased by slow passage through the PE devitrification region. The breaking strength of the graft copolymer is higher than that for the PE copolymer irradiated by the same dose.     

Controlled Release of Covalently Bound Organic Molecules by Slow Hydrolysis for Potential Biocide Applications†

A study of the slow hydrolysis of labile acetal groups by low concentrations of lactic acid to release the active molecules is reported. A prototype molecule containing cyclic acetal groups, dimethyl‐2,3‐O‐benzylidene‐L‐tartrate (DMTAc) and the same molecule incorporated as a pendant group in a polyamide were studied for their hydrolysis by low concentrations of lactic acid. The release of benzaldehyde during slow hydrolysis is monitored by UV‐vis and ¹H‐NMR spectroscopy. This study is very useful to ultimately design and synthesize a polymer with covalently bound insecticidal/anti‐microbial/anti‐fungal materials for the development of controlled release formulations.     

Formulation and Evaluation of 5-FU Loaded Eudragit Microspheres: Effect of Various Eudragit on Micromeretic Properties of Microspheres

The aim of the present study was to prepare and evaluate microspheres of Eudragit (RS, RL and RSPO) containing an anticancer drug 5-FU. Microspheres were prepared by O/O solvent evaporation method using a acetone/liquid paraffin system. Magnesium stearate was used as the droplet stabilizer and n-hexane was added to harden the microspheres. The prepared microspheres were characterized for their micromeretic properties and entrapment efficiency; as well by Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), X-ray powder diffractometry (XRPD), thin layer chromatography (TLC) and scanning electron microscopy (SEM) revealed the crystalline nature of drug in a final state. The in vitro release studies were performed in a Phosphate Buffer Solution (PBS) pH 7.4. The best fit release kinetics was achieved with a Higuchi plot. The yields of preparation and entrapment efficiencies were very high with a larger particle size for all the formulations. Mean particle size, entrapment efficiency and production yield were highly influenced by the type of polymer and polymer concentration. It is concluded from the present investigation that various Eudragit are promising controlled release carriers for 5-FU.     

Preface

The propagation step of the polymerization process of tetrahydrofuran was studied in detail. The influence of temperature and dielectric constant of the reaction medium on the rate and equilibrium constants of the elementary steps of the reaction was investigated. As the changes of temperature result in changes of the dielectric constant of the medium, it was found necessary to give the dependence of the reaction constants on both these parameters simultaneously.