两亲性壳聚糖基聚合物碳点的合成及其在载药方面的应用

通过水热法合成了系列具有高荧光量子产率（42.9%）辛基化壳聚糖基两亲性聚合物碳点荧光材料。利用红外光谱、紫外吸收光谱、光电子能谱、透射电镜、X射线衍射及荧光光谱对聚合物碳点进行了表征。以阿霉素为模型药物,研究了聚合物碳点对阿霉素的载药性能。当辛基取代度为76.42%时,其最大载药量和包封率分别为49.6%与47.4%。在磷酸盐缓冲液中,载药纳米胶束呈前期快速释放,后期缓慢释放的双相特征。将载药纳米胶束与鼻咽癌细胞作用,发现其存活率随着载药纳米胶束加入量的增加而降低,说明该纳米胶束对鼻咽癌细胞有一定的抑制作用。总之,该聚合物碳点材料在药物载体与荧光示踪方面有潜在的应用价值。     

HIV-1逆转录酶的分子对接及运动功能相关性分析

目的研究逆转录酶的运动性和生理功能的关系,以及N-乙酰基-β-芳基-1,2-二脱氢乙胺类衍生化合物与其的分子识别,方法采用高斯网络模型和各向异性网络模型研究了p66和p66-DNA的运动模式差异,并用分子对接方法研究化合物与逆转录酶的识别.结果 DNA的结合对p66各区域的运动方向影响不大,但其运动的幅度大大降低.分子对接结果发现Y115和M184的疏水结构在识别的过程中起到重要作用.结论基于各个区域的运动方向分析,推测手指区和RNase H区的开合运动可能是逆转录酶发挥逆转录功能的重要原因.并且,N-乙酰基-β-芳基-1,2-二脱氢乙胺类衍生化合物的N-甲基取代和反式的双键结构更有利于与逆转录酶的识别     

基于超临界流体技术制备葡萄糖脂质体的实验研究

脂质体由于其特殊的结构和性能,是一种很有发展潜力的药物载体,在医药和化妆品等行业具有广阔的应用前景。超临界逆向蒸发法是用超临界流体代替有机溶剂制备脂质体的方法,具有对水溶性药物脂质体制备过程简单、包覆率高等特点。以葡萄糖为模型药物,利用该方法制备出了葡萄糖脂质体,并详细考察了不同工艺条件对脂质体粒径和包覆率的影响。结果表明:用超临界逆向蒸发法可成功地制备出最小粒径为290nm、包覆率最高可达41.3%的葡萄糖脂质体。压力、温度和平衡时间对粒径和包覆率都有较大的影响。压力在10~30MPa时,随压力的增加,脂质体粒径显著减小至某一值后,基本趋于稳定,而包覆率逐渐增加,达到25.7%~27.5%,随后包覆率逐渐减小;温度在35~65℃时,随温度的增加粒径显著减小至最小值,然后逐渐增大,而包覆率一直增大,最高可达41.3%;平衡时间在15~45min时,随平衡时间的增加,粒径相对稳定,而包覆率显著增加,超过45min之后,粒径显著增加,包覆率显著下降。     

Polycaprolactone biopolymer thin films obtained by matrix assisted pulsed laser evaporation

We report the successful deposition of polycaprolactone polymer by MAPLE using a KrF* excimer laser (λ = 248 nm, τ = 7 ns). According to FTIR spectra the deposited films have similar chemical structure to the dropcast material. The fluence plays a key role in optimizing the performances of MAPLE-synthesized polycaprolactone structures. We demonstrated that MAPLE allows for controlling the morphology of films to the level required in targeted drug delivery of pharmacologic agents.     

In vitro study of magnetic particle seeding for implant assisted-magnetic drug targeting

The concept of using magnetic particles (seeds) as the implant for implant assisted-magnetic drug targeting (IA-MDT) was analyzed in vitro. Since this MDT system is being explored for use in capillaries, a highly porous (ε∼70%), highly tortuous, cylindrical, polyethylene polymer was prepared to mimic capillary tissue, and the seeds (magnetite nanoparticles) were already fixed within. The well-dispersed seeds were used to enhance the capture of 0.87 μm diameter magnetic drug carrier particles (MDCPs) (polydivinylbenzene embedded with 24.8 wt% magnetite) under flow conditions typically found in capillary networks. The effects of the fluid velocity (0.015–0.15 cm/s), magnetic field strength (0.0–250 mT), porous polymer magnetite content (0–7 wt%) and MDCP concentration (C=5 and 50 mg/L) on the capture efficiency (CE) of the MDCPs were studied. In all cases, when the magnetic field was applied, compared to when it was not, large increases in CE resulted; the CE increased even further when the magnetite seeds were present. The CE increased with increases in the magnetic field strength, porous polymer magnetite content and MDCP concentration. It decreased only with increases in the fluid velocity. Large magnetic field strengths were not necessary to induce MDCP capture by the seeds. A few hundred mT was sufficient. Overall, this first in vitro study of the magnetic seeding concept for IA-MDT was very encouraging, because it proved that magnetic particle seeds could serve as an effective implant for MDT systems, especially under conditions found in capillaries.     

An in vitro controlled release study of valproic acid encapsulated in a titania ceramic matrix

Despite the therapeutic efficacy of valproic acid towards numerous diseases, its poor bioavailability and systemic side effects pose significant barriers to long term treatment. In order to take advantage of controlled release implants of valproic acid, the drug was encapsulated into titania ceramic matrices via a sol-gel process. The integrity and structure of valproic acid-containing matrices were characterized through the use of FESEM, TEM, and BET analyses. In vitro controlled release studies and kinetic analyses were performed under ambient conditions (25 °C, atmospheric pressure) and controlled release behaviors were studied using a GC-MS method. Results showed first order dependence in the rate of valproic acid release as a function of drug concentrations in the titania ceramic device. A marked dependence on the surface area and pore size distribution with drug loading was also observed. This research opens new possibilities for the design of novel time-delayed controlled release systems for valproic acid encapsulates.     

荧光碳量子点的制备与生物医学应用研究进展

碳量子点是一类具有优异的荧光性能和高生物相容性的纳米材料,在很多领域有广泛的应用,是目前研究的热点材料。本文介绍了碳量子点不同的合成方法,以及碳量子点的荧光、化学发光、电化学发光、类过氧化物酶的活性及毒性等性能的最新研究进展。此外,还对碳量子点在生物传感、生物成像及药物传递等生物医学应用进行了概述。     

Solid-Phase Luminescence Determination of Ciprofloxacin and Norfloxacin in Biological Fluids

A simple, rapid, and sensitive luminescence test method for the determination of ciprofloxacin (CIP) and norfloxacin (NOR) has been described. The method is based on the intramolecular energy transfer from organic acid to terbium (Tb³⁺) ion. Luminescence of terbium (III) complex with CIP (NOR), sorbed on the zeolite has been studied. Under optimized conditions the detection limit is 1 g/mL in urine and human plasma.     

Optimization of Verapamil Drug Analysis by Excitation-Emission Fluorescence in Combination with Second-order Multivariate Calibration

Excitation emission fluorescence matrices (EEMs) of Verapamil drug were obtained by direct and by derivatization fluorescence spectroscopy. The fluorescence excitation and emission wavelengths were displaced to longer wavelengths and the fluorescence intensity was enhanced upon derivation with respect to the native fluorescence of the drug. The complete EEM of the native fluorescence of the drug and of the derivatization product were rapidly acquired by using a charged-coupled device detector (CCD), which is advantageous in terms of speed in the analysis, with respect to the use of a conventional photomultiplier detector. The EEMs were analyzed by several second-order multivariate calibration methods exploiting the second order advantage. The three-dimensional decomposition methods used, based in different assumptions about the trilinearity of the three way data structure under analysis, were parallel factor analysis (PARAFAC), bilinear least squares (BLLS), parallel factor analysis 2 (PARAFAC2) and multivariate curve resolution—alternating least squares (MCR-ALS). The determination was performed by using the standard addition approach. The figures of merit of the PARAFAC and BLLS methods were calculated, obtaining a lower limit of detection with the derivatization procedure, when compared with the direct measurement of the fluorescence of the drug. In Verapamil drug the best estimations were found with the BLLS and the MCR-ALS models. In the quantification of Verapamil in a pharmaceutical formulation the best estimation, when compared with the result obtained by the US Pharmacopeia high performance liquid chromatography approach, was obtained by direct fluorescence spectroscopy with MCR-ALS and by derivatization fluorescence spectroscopy with the PARAFAC2 model.     

太赫兹时域光谱技术在危险品检测方面的应用

太赫兹波(terahertz, THz, T-ray)是指频率介于0.1～10 THz之间的电磁辐射,在电磁波谱上位于微波和远红外线之间。大多数爆炸物、毒品在此波段有特征吸收。与在公共安全领域检测武器、爆炸物、毒品等危险品的传统方法相比,太赫兹辐射能量低,不会产生电离辐射,也不会引起安全担忧。而且,太赫兹波对于衣物等大多数包装材料有很强的穿透力,对物质的检测可以做到高灵敏、无损伤和远距离,因此在反恐、毒品、安全检测等方面具有显著潜在优势。文章介绍了国内外太赫兹时域光谱技术(terahertz time domain spectroscopy, THz-TDS)在爆炸物及毒品检测方面的研究最新进展;详细讨论了黑索金(RDX)的研究现状,并初步探讨了影响实验结果的几种因素。