Roles of adriamycin and adriamycin dimer in antitumor activity of the polymeric micelle carrier system

Adriamycin (ADR) dimer was prepared and its antitumor activity was evaluated with mouse colon adenocarcinoma 26 (C 26). As compared with original ADR, the dimer did not show significant antitumor activity, either in vitro or in vivo. Furthermore, polymeric micelles containing varied ratios of the dimer to the original ADR were prepared. Polymeric micelles with a higher dimer/ADR ratio (9.7) showed significant antitumor activity, but the effective dose shifted higher. Effective doses were found to largely depend on the concentration of the original ADR, rather than that of the dimer at the tumor sites. Therefore, it was presumed that the original ADR played a major role in antitumor activity, and the dimer played a supplementary role to contribute selective delivery of ADR to the tumor sites.     

叶酸介导的靶向性钆造影剂的制备及弛豫性能研究

在弱碱性的条件下，叶酸活化酯与牛血清白蛋白(BSA)反应生成叶酸-牛血清白蛋白偶联物(叶酸-BSA)，该偶联物再与二乙三胺五乙酸(DTPA)的酸酐反应，最后与GdCl₃进行螯合制得叶酸-BSA-(Gd-DTPA)_n。配合物的结构通过紫外光谱法进行了鉴定，并定量测定了配合物中叶酸、Gd-DTPA对BSA的偶联率。通过测定配合物的体外弛豫时间T₁，进一步分析其弛豫性能R₁。结果表明本研究制得的叶酸-BSA-(Gd-DTPA)_n配合物中叶酸的偶联率约为5，体外弛豫性能R1约为6×10^-3 L·mmol^-1·ms^-1，与未偶联叶酸的BSA-(Gd-DTPA)_n的弛豫性能无显著性差异，且比小分子Gd-DTPA的弛豫性能提高了3倍左右。     

Feedback law design and the Liapunov approach

We study the problem of designing targeting-type feedback control laws for systems with state and control constraints. A systematic approach to this problem is described in terms of a number of Liapunov-like criteria. This approach is presented in tutorial form and is illustrated by means of two examples having some background in the literature.This work was supported by the National Science Foundation under Grant ECS-8210284.     

A model for predicting magnetic targeting of multifunctional particles in the microvasculature

A mathematical model is presented for predicting magnetic targeting of multifunctional carrier particles that are designed to deliver therapeutic agents to malignant tissue in vivo. These particles consist of a nonmagnetic core material that contains embedded magnetic nanoparticles and therapeutic agents such as photodynamic sensitizers. For in vivo therapy, the particles are injected into the vascular system upstream from malignant tissue, and captured at the tumor using an applied magnetic field. The applied field couples to the magnetic nanoparticles inside the carrier particle and produces a force that attracts the particle to the tumor. In noninvasive therapy, the applied field is produced by a permanent magnet positioned outside the body. In this paper, a mathematical model is developed for predicting noninvasive magnetic targeting of therapeutic carrier particles in the microvasculature. The model takes into account the dominant magnetic and fluidic forces on the particles and leads to an analytical expression for predicting their trajectory. An analytical expression is also derived for predicting the volume fraction of embedded magnetic nanoparticles required to ensure capture of the carrier particle at the tumor. The model enables rapid parametric analysis of magnetic targeting as a function of key variables including the size of the carrier particle, the properties and volume fraction of the embedded magnetic nanoparticles, the properties of the magnet, the microvessel, the hematocrit of the blood and its flow rate.     

In vitro study of ferromagnetic stents for implant assisted-magnetic drug targeting

Implant-assisted-magnetic drug targeting (IA-MDT) was studied in vitro using a coiled ferromagnetic wire stent made from stainless steel 430 or 304, and magnetic drug carrier particle (MDCP) surrogates composed of poly(styrene/divinylbenzene) embedded with 20 wt% magnetite. The fluid velocity, particle concentration, magnetic field strength, and stent material all proved to be important for capturing the MDCP surrogates. Overall, this in vitro study further confirmed the important role of the ferromagnetic implant for attracting and retaining MDCPs at the target zone.     

Modeling of magnetic bandages for drug targeting: Button vs. Halbach arrays

Magnetic targeting of drugs to diseased tissues, such as non-healing wounds or skin tumors, is a promising clinical use of magnetic microspheres. For successful magnetic targeting, a magnet must be placed in close proximity to the target tissue. In this work the forces exerted on magnetic microspheres by different arrangements of magnets including a simple square magnet, a number of button magnet arrays, and a Halbach array were simulated and compared. Magnetic bandages utilizing a Halbach array configuration were found to yield the best trapping characteristics (large and uniform force distributions) for magnetic targeting applications close to a surface.     

In vitro investigation of the behaviour of magnetic particles by a circulating artery model

Magnetic drug targeting is the use of coated magnetic nanoparticles as carriers for cytostatic drugs. After intraarterial application of these carriers, they are attracted with an external magnetic field to, for example, an experimental VX2 tumour. The biological compatibility of this system depends on several physiological and physical parameters. We established an in vitro model to simulate in vivo conditions in a circulating system consisting of a circuit with an intact bovine femoral artery close to an external magnetic field. Nanoparticle suspensions were applied by a side inlet. After the magnetisation procedure particle size, concentration and distribution was examined.     

连续混沌系统的非线性自适应预测跟踪控制

基于混沌时间序列的非线性自适应预测原理,用一种sigmoid-Volterra自适应预测滤波器研究了连续混沌系统的非线性自适应预测跟踪控制.通过对Lorenz,R?ssler等典型混沌系统的控制,仿真证实了这种sigmoid-Volterra自适应预测控制器的有效性.这种方法的优点在于它既不需要知道精确的混沌系统模型,也不需要进行系统模型辨识. 关键词： 混沌 sigmoid-Volterra自适应预测滤波器 非线性自适应预测跟踪