生长抑素-葡聚糖的99Tcm标记及体外结合分析

采用还原氨化方法，将天然生长抑素（SMS）与葡聚糖(Dx20)偶联，并以125I－奥曲肽（125I-Tyr3-Octreotide)为放射配基，进行受体竞争结合实验，测定了SMS-Dx50的IC50；以SnCl2为还原剂对SMS-Dx50进行99Tcm标记，并进行99Tcm- SMS-Dx50受体结合分析，考察其对生长抑素受体的亲合能力。结果表明：SMS-Dx50保持了对SMS 2型受体的高亲和力；其IC50与奥曲肽的IC50（0.79 nmol/L）相近,为5.95 nmol/L；99Tcm- SMS-Dx50标记率>85％, 经PD-10柱分离纯化，其放化纯度>98%；99Tcm- SMS-Dx50对生长抑素2型受体特异性结合为25%～40％，保持了较高的亲和力；SMS-Dx50适合于99Tcm标记，可用于生长抑素受体阳性肿瘤诊断的进一步研究     

Central composite rotatable design for optimization of budesonide-loaded cross-linked chitosan–dextran sulfate nanodispersion: characterization,in vitro diffusion and aerodynamic study

Budesonide is a BCS class II drug with low water solubility (0.045?mg/mL) and low oral bioavailability (6–8%) due to high first pass effect. The aim is to prepare cross-linked chitosan–dextran sulfate nanoparticles and/or nanodispersion. Nebulizable cross-linked nanodispersion was prepared by the solvent evaporation technique and characterized through XRPD, FTIR, mean particle size (MPS), polydispersity index (PDI), zeta potential (ZP), drug loading, entrapment efficiency, SEM, % production yield, in vitro diffusion, aerodynamic and stability study. The optimization of formulation was done by using central composite rotatable design to study the effect of independent variables, concentration of chitosan (X1) and concentration dextran sulfate (X2) on the dependent variables, MPS (Y1), drug loading (Y2) and % CDR (% cumulative drug release) (Y3). The MPS, PDI, and ZP of budesonide-loaded nanoparticles were 160.8?±?0.27?nm, 0.36?±?0.04, and 13?±?0.894?mV, respectively. The percent drug loading of all the batches was found in range of 10–16%. The emitted drug in target region (alveoli) was measured by using HPLC and it was found to be 18.26%. It was found that, nanodispersion had the optimum in vitro aerodynamic behavior. Stability study results showed no significant change in MPS, PDI, ZP, and % CDR after three month storage. In conclusion, cross-linked chitosan–dextran sulfate nanoparticles had properties suitable for nebulizable dispersion of increased drug loading, in vitro drug release and avoiding the first pass effect.     

Biodegradable Spheres Protect Traumatically Injured Spinal Cord by Alleviating the Glutamate‐Induced Excitotoxicity

New treatment strategies for spinal cord injury with good therapeutic efficacy are actively pursued. Here, acetalated dextran (AcDX), a biodegradable polymer obtained by modifying vicinal diols of dextran, is demonstrated to protect the traumatically injured spinal cord. To facilitate its administration, AcDX is formulated into microspheres (≈7.2 µm in diameter) by the droplet microfluidic technique. Intrathecally injected AcDX microspheres effectively reduce the traumatic lesion volume and inflammatory response in the injured spinal cord, protect the spinal cord neurons from apoptosis, and ultimately, recover the locomotor function of injured rats. The neuroprotective feature of AcDX microspheres is achieved by sequestering glutamate and calcium ions in cerebrospinal fluid. The scavenging of glutamate and calcium ion reduces the influx of calcium ions into neurons and inhibits the formation of reactive oxygen species. Consequently, AcDX microspheres attenuate the expression of proapoptotic proteins, Calpain, and Bax, and enhance the expression of antiapoptotic protein Bcl‐2. Overall, AcDX microspheres protect traumatically injured spinal cord by alleviating the glutamate‐induced excitotoxicity. This study opens an exciting perspective toward the application of neuroprotective AcDX for the treatment of severe neurological diseases.     

温度敏感葡聚糖凝胶的合成及其细胞相容性研究

合成了N-异丙基丙烯酰胺（NIPAAm）与葡聚糖的共聚水凝胶，利用红外光谱表征了单体和凝胶结构，研究了水凝胶在去离子水和细胞培养基中的温度响应性，并对凝胶进行了细胞培养和脱附研究．结果表明，共聚凝胶具有很好的温度敏感性和细胞相容性，可以通过控制温度变化，实现对细胞的无损伤脱附．     

用原子力显微镜研究葡聚糖包覆纳米氧化铁微粒的形貌特征

采用化学共沉淀法合成了葡聚糖包覆的超顺磁纳米氧化铁微粒,用原子力显微镜对其分布状态、微粒形貌和尺度等进行了表征,并与透射电镜观察结果进行了比较。结果表明：葡聚糖包覆的超顺磁纳米氧化铁微粒大小均匀且有规律的定向分布,无团聚现象;透射电镜显示其核心氧化铁纳米粒子的外形主要为不规则的球形,粒径5～20nm被葡聚糖包覆后的纳米氧化铁微粒呈长方体,尺寸为（200-300）nm×（400-600）nm×（50-70）nm。     

寡胺-葡聚糖类阳离子化合物合成及其在基因转染中的应用

应用氧化葡聚糖与精胺通过还原胺法反应,制备了聚阳离子非病毒基因载体葡聚糖-寡胺化合物;用红外光谱测定仪、核磁共振波谱仪、紫外光谱仪,激光纳米粒度测定仪、透射电子显微镜进行了表征.证实了该载体为葡聚糖-精胺化合物DSP.其平均粒径为170nm,Zeta电位为+31.1mV,镜下呈园球形状.将载体DSP与pCMV-GFP的质粒DNA以8:1(N/P)组成复合物时,对SMMC-7721人肝癌细胞进行体外转染,转染效率高于阳性对照组transfectine 2000,为31.1%.实验表明该材料有望成为临床的非病毒基因载体.     

不同分子量的葡聚糖-花生分离蛋白接枝复合物的制备及其性质

通过不同分子量葡聚糖与花生分离蛋白发生接枝反应形成共价聚合物,并对它们的结构特性、功能特性和所形成乳浊液的流变学特性进行分析,多角度探讨葡聚糖分子量对花生分离蛋白结构及其乳浊液性质的影响并阐释原因。对接枝产物的接枝度结果测定证明了接枝反应的发生,且随着葡聚糖分子量的增加,接枝程度越低。共价聚合物的二级和三级结构都发生了改变,二级结构中α-螺旋结构减少,β-转角结构增多,以20 kDa分子量的葡聚糖与花生分离蛋白接枝形成的共价聚合物PDC2变化较为明显;三级结构中,PDC2变得更加松散,结构的变化引起其分子间疏水作用力增加,表面疏水性指数达到783±19,在其乳浊液体系中,内部分子间离子作用力明显,抗剪切作用力较大,这些作用力维持着乳浊液体系的稳定性。葡聚糖接枝能够改善花生分离蛋白的功能特性,其中以20 kDa分子量的葡聚糖改善程度最为明显,为拓宽花生分离蛋白在食品工业中的应用提供了一定的依据。     

高乳化活性的BSA-葡聚糖接枝物制备工艺的优化

牛血清白蛋白(bovine serum albumin,BSA)可通过糖基化反应与葡聚糖(dextran)形成复合物,可作为油溶性营养素的乳化包埋载体。以乳化活性为指标,通过单因素试验以及响应面试验,优化湿法美拉德反应制备BSA-dextran复合物的最佳工艺条件。研究结果表明:复合物最佳工艺条件为BSA浓度2.78mg/mL、dextran∶BSA(摩尔比)=6.89∶1、pH8.50、反应时间2.3h、反应温度95.0℃;所得BSA-dextran乳化活性为(31.743±0.45)m2/g;该复合物对叶黄素包埋的包封率为95.86%,明显高于BSA对叶黄素包埋的包封率(77.82%)。     

Effect of the polymeric cryoprotectant dextran on fluid secretion in the isolated rabbit pancreas

Physiological effects of the polymeric cryoprotectant dextran on an ion-transporting epithelium were investigated. In the isolated rabbit pancreas, dextran caused inhibition of fluid secretion and an increase of the concentrations of Na⁺, K⁺ and Cl^? in the secreted fluid. Dextran did not affect the basal or pancreozymin-stimulated enzyme secretion. These effects of dextran can partially be explained by the fact that it is osmotically active and does not permeate through the epithelium. The effect of dextran on water transport can be compensated by lowering the ion concentrations in the solvent of the cryoprotectant. It is concluded that in cryoprotected ion-transporting epithelia the absolute ion concentration values obtained by X-ray microanalysis of frozen-hydrated specimens may not be completely correct, but that valid conclusions about intracellular ion distribution may still be drawn.