A series of well-defined three-armed star-block copolymers (mPEG-a-PCL-a-)3 linked with acid-cleavable acetal groups have been prepared and used for the pH-triggered delivery of doxorubicin.
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.
Polyurea microcapsules containing oily substances were prepared by using cyanate and polyamine as the monomers with non-ionic surfactant as the emulsifiers. Results showed that TDI—DETA microcapsules had the best stability. The mean diameter decreased and the size distribution curves became narrower and sharper as the stirring speed and the emulsifier concentration during emulsification increased. Addition of Tween 80 to aqueous solution containing OP led to an increase in microcapsule diameter and wider distribution of microcapsules due to the changes in interfacial tension. The isoelectric point of the polyurea microcapsules was found to be pH 5 8.
Drug self-delivery systems consisting of small-molecule active drugs with nanoscale features for intracellular delivery without the need for additional polymeric carriers have drawn much attention recently. In this work, we proposed a highly efficient strategy to fabricate protonized and reduction-responsive self-assembled drug nanoparticles from an amphiphilic small-molecule camptothecin–ss-1,2,3-triazole–gemcitabine conjugate (abbreviated as CPT–ss-triazole–GEM) for combination chemotherapy, which was prepared via a Cu(I)-catalyzed azide–alkyne cycloaddition (CuAAC) "click" reaction. To obtain this drug–triazole–drug conjugate, we first prepared a CPT derivate containing a propargyl group linked with a disulfide group and a GEM derivate attached to an azide group. Subsequently, the two kinds of modified drugs were connected together through a CuAAC reaction between the alkynyl and azide groups to yield the CPT–ss-triazole–GEM prodrug. The characterizations of chemical structures of these intermediates and the final product were performed by 1H NMR, Fourier transform infrared, and liquid chromatography/mass spectrometry measurements. This amphiphilic small-molecule drug–triazole–drug conjugate displayed a high drug loading content, that is, 36.0% of CPT and 27.2% of GEM. This kind of amphiphilic small-molecule prodrugs could form spherical nanoparticles in an aqueous solution in the absence of any other polymeric carriers, in which the hydrophobic CPT formed the core of the nanoparticles, whereas the hydrophilic GEM and protonated 1,2,3-triazole group yielded the shell. In the tumor microenvironment, the prodrug nanoparticles could release both pristine drugs simultaneously. Under the conditions of pH 7.4, and pH 7.4 and 2 μM glutathione (GSH), the prodrug nanoparticles could maintain stability and only 7% of CPT was leaked. However, in a high-GSH environment (pH 7.4 and 10 mM GSH) with the same incubation time, the disulfide linkage would be dissociated and lead to about 34% of CPT release. The results of the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide test demonstrated that these prodrug nanoparticles showed a higher cytotoxicity toward HepG2 cells than free CPT and free GEM on both 48 and 72 h of incubation. Both in vitro cellular uptake and flow cytometry results implied that these prodrug nanoparticles could be internalized by HepG2 cells with efficient drug release inside cells. The pharmacokinetics and tissue distribution of the prodrug showed a moderate half-life in vivo, and the prodrug peak concentration in most of the collected tissues appeared at 0.25 h after administration. In addition, the CPT–ss-triazole–GEM prodrug could not cross the blood–brain barrier. Even more important is the fact that there is no accumulation in tissues and a rapid elimination of this small-molecule prodrug could be achieved. In brief, this protonized and reduction-sensitive prodrug simultaneously binds both antitumor drugs and has good self-delivery behavior through the donor–acceptor interaction of the H-bonding ligand, that is, the 1,2,3-triazole group. It provides a new method for combined drug therapy.
This paper introduces an improved tabu-based vector optimal algorithm for multiobjective optimal designs of electromagnetic devices. The improvements include a division of the entire search process, a new method for fitness assignment, a novel scheme for the generation and selection of neighborhood solutions, and so forth. Numerical results on a mathematical function and an engineering multiobjective design problem demonstrate that the proposed method can produce virtually the exact Pareto front, in both parameter and objective spaces, even though the iteration number used by it is only about 70% of that required by its ancestor.
A response surface model (RSM) based on a combination of interpolating moving least squares and multistep method is proposed. The proposed RSM can automatically adjust the supports of its weight functions according to the distribution of the sampling points when it is used to reconstruct a computationally heavy design problem. Numerical examples are given to demonstrate the feasibility and efficiency of the proposed method for solving inverse problems
Back Cover: Ming-Zhu Liu, Hua Wei, and co-workers report the fabrication of thermo-sensitive cyclic brush copolymers, which show higher stability and greater therapeutic efficacy than the bottle brush analogues for anti-cancer drug delivery. Further details can be found in article number 1700744.
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