固体脂质纳米粒的研究新进展

固体脂质纳米粒是近年来很受重视的一种新型药物传递载体,具有靶向、控释、提高药物稳定性、毒性小、可大批量生产等优点,是一种极有发展前景的新型给药系统.现综述了近年来国内外固体脂质纳米粒的制备技术、作为药物载体的应用、存在问题以及发展前景.     

固体脂质纳米粒用于细胞毒性药物传递系统综述的研究进展

目的:介绍固体脂质纳米粒(SLN)用于细胞毒性药物传递系统以治疗癌症的情况。方法:依据文献综述SLN用于抗癌药物载体的原理、包载细胞毒性药物后可解决的主要问题、用于癌症治疗的未来研究方向。结果与结论:设计合理的SLN可利用实体瘤组织的高通透性和滞留效应达到被动靶向的目的;解决的主要问题有提高对水溶性抗癌化合物的包封率、改进药物的控释速率和释放程度、避免被网状内皮系统清除;未来的研究方向为细胞毒性药物与增敏剂的联合治疗、细胞毒性药物SLN的特异性靶向,以及用于肿瘤治疗的基因传递。     

载药金纳米粒的研究进展

近年来,作为一种新型药物递送系统,金纳米粒已引起了广泛关注。由于其特殊的物理化学性质,能与多种类型药物发生相互作用,如蛋白质、核酸、小分子药物等,从而可应用于肿瘤治疗和检测。笔者对载药金纳米粒的制备方法、载药方式和安全性等问题进行综述。     

银模板法制备中空金纳米粒及其质量评价

目的 制备并表征一种可用于载药的中空金纳米粒载体.方法 以银纳米粒为模板,通过模板置换法使氯金酸与银纳米粒反应生成金壳,并裹覆于银纳米粒表面,最后形成一种中空结构的金纳米粒,通过单因素考察对中空金纳米粒的制备进行初步探究.使用透射电镜对中空金纳米粒进行结构观察,紫外全波长扫描考察其吸收情况,体外光热转化试验考察载体的光热转化能力,以及四甲基偶氮唑蓝(MTT)试验考察载体细胞毒性.结果 氯金酸的加入方式为逐滴加入,制备温度为60 ℃,氯金酸(25 mmol·L-1)的加入量为128 μL,中空金纳米的粒径为35~55 nm,壳厚4~6 nm,最大吸收波长750~800 nm,具备较强的光热转化能力.细胞毒性结果表明,中空金纳米粒对人皮肤成纤维细胞(HDF)没有明显的细胞毒性.结论 经过优化制备得到的中空金纳米粒具备较好的中空结构,以及优异的光热转化能力和较低的细胞毒性.     

载药纳米粒的脑内递药系统

介绍了载药纳米粒在脑内药物传递系统中的应用 ,提出了其脑靶向性可能的影响因素和机制     

超顺磁氧化铁纳米粒在药物传递系统中的研究进展

超顺磁氧化铁纳米粒作为一种新型纳米材料,不仅可用于临床磁共振成像对比剂,还可用于药物传递载体,近些年对它的研究和应用越来越受到人们的关注。本文从超顺磁氧化铁纳米粒的合成、表面修饰及其在药物传递中的应用进展情况做一综述。     

固体脂质纳米粒和纳米结构脂质载体在药物传递中的研究进展

基于固体脂质的纳米粒（Solid lipid - based nanoparticles,SLBNs）作为新型药物传递系统比常规的药物传递系统存在优势。通常,基于固体脂质的纳米粒可以分成两种形态,即固体脂质纳米粒（ Solid lipid nanoparticles, SLNs）和纳米结构脂质载体（Nanostructured lipid carriers,NLCs）。但固体脂质纳米粒与纳米结构脂质载体在基质的组成上不同,本文就基于固体脂质的纳米粒的制备技术、表征方法及应用的最新研究进展进行总结,为基于固体脂质的纳米粒进一步研究提供参考依据。     

聚合物纳米粒子作为药物载体的研究与应用

目的:介绍聚合物纳米粒子作为药物载体的研究与应用现状。方法:参阅国内外文献,进行分析、归纳和总结。结果:聚合物纳米粒子可作为疏水药物、靶向药物和生物大分子药物的载体制备聚合物纳米粒的材料与方法具有多样性。结论:可生物降解的聚合物纳米粒载药系统具有可控释、靶向、保护生物大分子药物的活性等优势,是一个很有发展潜力的药物传递系统。     

纳米粒技术在转运药物通过血脑屏障中的应用

纳米粒（nanoparticles）是一类粒径为1－1000nm的固体胶粒，现已被用作传递药物的载体。利用纳米粒将药物转运通过血脑屏障可能会提供更具有显著优势的脑内给药方法。纳米粒载体技术的主要优势在于纳米粒能克服血脑屏障限制治疗药物通过的特性，此外，这类给药系统还能延缓药物在脑内的释放，降低外周毒性。本文评价了以往的脑内给药方法，讲座了纳米粒通过血脑屏障的转运机制，描述了纳米粒的主要制备方法和特性。此外，对与药物转运通过血脑屏障有关的影响纳米粒制备的因素（聚合物和表面活性剂的类型、纳米粒的粒径和药物分子）也作了详细阐述。目前，评价纳米粒脑内给药的报道主要是针对麻醉药和化疗药。本文对这类报道中转运的机制和效果作了叙述。同时讨论了突破网状内皮系统的吞噬作用等生理因素对药物转运进入大脑的限制的方法。     

载巯基化阿霉素的中空金纳米粒的制备与光热性能研究

目的 制备一种载阿霉素（DOX）的中空金纳米粒（HGNPs）载体。方法 合成巯基化阿霉素（DOX-SH）,通过质谱（MS ESI）和核磁共振氢谱（1H-NMR）对其结构进行表征,再将其以金硫键共价结合方式负载到中空金纳米粒表面。通过粒径、等离子共振吸收（SPR）、透射电子显微镜（TEM）、近红外（NIR）激发的光热转化实验和细胞毒性实验对制备的中空金纳米粒载药体系进行评价。结果 质谱显示,合成的巯基化阿霉素的分子量为616,核磁共振氢谱所示的结构也与目标产物相符。阿霉素-中空金纳米粒复合载药体系(HGNPs-DOX)的粒径为70 nm左右;等离子共振吸收最大吸收波长为800 nm左右,具有良好的光热转化能力;透射电子显微镜显示,其为中空圆球形结构,壳厚4~6 nm;细胞毒性显示,在高浓度时,阿霉素-中空金纳米粒复合载药体系能显著减小阿霉素的毒性。结论 成功合成了阿霉素-中空金纳米粒复合载体,其具有良好的结构,良好的光热转化能力,较小的细胞毒性,未来可成为有研究前景的新一代化疗联合光热治疗的递送载体。     

环境响应的智能化递药系统在肿瘤靶向治疗研究的应用(英文)

环境响应的智能化递药系统可对肿瘤组织特殊生理环境及体外环境变化而发生相应变化,特异地靶向分布于肿瘤组织或在肿瘤组织的特殊生理环境下释放药物,从而可有效改善并提高抗癌药物对肿瘤靶向治疗效果,降低药物毒副作用,已成为近年来肿瘤靶向治疗研究领域的热点之一。本文综述了环境响应的智能化递药系统的靶向机理及其在肿瘤靶向治疗中的应用,以期为新型肿瘤靶向递药系统的开发及其对肿瘤的治疗提供参考。     

肿瘤治疗的细胞药物递送系统的研究进展

目前,肿瘤的临床治疗主要以手术、化疗和放射疗法为主,但仍存在复发和不良反应明显等问题。细胞药物递送系统不仅可以避免纳米颗粒药物的毒性,又可以增加药物的生物利用度,提高生物相容性、靶向性。总结了活细胞、死细胞、外泌体及其药物递送系统的载药特点和在肿瘤治疗中的应用,为肿瘤治疗提供了更多的治疗手段。     

Development, characterization, and toxicity evaluation of amphotericin B-loaded gelatin nanoparticles

Our aim in the present investigation was to develop a nanoparticulate carrier of amphotericin B (AmB) for controlled delivery as well as reduced toxicity. Nanoparticles of different gelatins (GNPs) (type A or B) were prepared by two-step desolvation method and optimized for temperature, pH, amount of cross-linker, and theoretical drug loading. AmB-loaded GNPs were characterized for size, polydispersity index (PI), shape, morphology, surface charge, drug release, and hemolysis. The developed GNPs (GNP(A300)) were found to be of nanometric size (213 +/- 10 nm), having low PI (0.092 +/- 0.015) and good entrapment efficiency (49.0 +/- 2.9%). All GNPs showed biphasic release characterized by an initial burst followed by controlled release. The in vivo hematological toxicity results suggest nonsignificant reduction (P > .05) in hemoglobin concentration and hematocrit. Nephrotoxicity results showed that there was a nonsignificant (P > .05) increase in blood urea nitrogen and serum creatinine levels. The results confirm that developed GNPs could optimize AmB delivery in terms of cost and safety, and type A gelatin with bloom number 300 was found suitable for such preparation.     

Programmed drug delivery system based on optimized “size decrease and hydrophilicity/hydrophobicity transformation” for enhanced hepatocellular carcinoma therapy of doxorubicin

Requirements on drug delivery systems to surmount a complex series of pathophysiological barriers bear “cascading contradictions”, especially size and hydrophilicity/hydrophobicity contradiction. Herein, a programmed drug delivery system (GNPs-Dox-Lac) based on optimized “size decrease and hydrophilicity/hydrophobicity transformation” was developed by combination the gelatin nanoparticle (GNPs) and prodrug Doxorubicin-Lactose (Dox-Lac). The results showed that GNPs-Dox-Lac (133.3 nm) were kinetically stable in blood circulation and inclined to accumulate at the tumor site. Then the degradation of the GNPs triggered by tumor extracellular matrix metalloproteinase-2 (MMP2) led to the release of prodrug Dox-Lac (Mw 898 Da) to facilitate the tumor tissue penetration and cellular uptake. Last, pH-responsive disassociation of Dox-Lac in tumor cells resulted in the free Dox (Mw 543 Da) release to induce toxicity. As expected, GNPs-Dox-Lac achieved superior tumor inhibition rate of 90.8% with low toxicity in vivo, suggesting its potential for enhanced hepatocellular carcinoma (HCC) therapy of doxorubicin in future.     

Effects of nanoparticle size and gestational age on maternal biodistribution and toxicity of gold nanoparticles in pregnant mice

Gold nanoparticles (GNPs) have considerable applications in biomedicine, such as in bio-sensing, bio-imaging, drug delivery and photothermal therapeutics. However, currently there are limited information regarding the impact of pregnancy on their biodistribution, elimination and toxicity. In this study, we investigated the biodistribution and potential toxic effects of different-sized GNPs (1.5, 4.5, 13, 30 and 70 nm in diameter) in non-pregnant and pregnant mice at different gestational ages (E5.5, 7.5, 9.5, 11.5 and 13.5). 5 h after intravenous injection, GNPs exhibited size-dependent biodistribution profiles; however, regardless of size, no significant biodistribution changes were observed between non-pregnant and pregnant mice. Kinetic studies showed that 4.5 nm GNPs were primarily excreted through urine within 5 h, whereas 30 nm GNPs had a more prolonged blood circulation time. No apparent toxic effects (e.g., increased mortality, altered behavior, reduced animal weight, abnormal organ morphology or reduced pregnancy duration) were observed with different-sized GNPs in pregnant mice. However, treatment with 30 nm GNPs induced mild emphysema-like changes in lungs of pregnant mice. These results indicated that the maternal biodistribution patterns of GNPs in pregnant mice depended on particle size, but not gestational age; organ-specific adverse effects may arise with treatment with some GNPs according to their size.     

Thermo-responsive systems for controlled drug delivery

Controlled drug delivery systems represent advanced systems that can be tightly modulated by stimuli in order to treat diseases in which sustained drug release is undesirable. Among the many different stimuli-sensitive delivery systems, temperature-sensitive drug delivery systems offer great potential over their counterparts due to their versatility in design, tunability of phase transition temperatures, passive targeting ability and in situ phase transitions. Thus, thermosensitive drug delivery systems can overcome many of the hurdles of conventional drug delivery systems in order to increase drug efficacies, drug targeting and decrease drug toxicities. In an effort to further control existing temperature-responsive systems, current innovative applications have combined temperature with other stimuli such as pH and light. The result has been the development of highly sophisticated systems, which demonstrate exquisite control over drug release and represent huge advances in biomedical research.     

天然药物靶向给药系统的研究

采用新型药物载体使天然药物具有靶向作用是近年来药剂学的研究热点之一。综述脂质体、纳米粒、微球、微乳、药质体等新型载体在天然药物靶向给药系统研究中的应用,并介绍膜融合脂质体、纳米脂质载体、药脂结合物纳米粒以及分泌颗粒类似物等几种新型靶向给药系统的药物载体。     

离子交换树脂在药剂学中的应用进展

离子交换树脂药物载体在给药系统中的应用由于具有很多优点而得到了人们的重视。目前在控释、透皮给药、定位给药、速溶、离子导入透皮、鼻腔、局部给药和掩盖药物苦味等方面都有很深入的研究，在缓控释给药中占有特殊的地位。综述了这一药物载体在给药系统和作用部位应用的新进展，并对其应用前景进行了展望。     

The Perspective and Next Generation Tools to prove Environmental Health in Inhalation Toxicology,White Biotechnology and Climate Changes

Recently, nanoparticles (NPs) are introduced to a broad range of biomedical applications including drug delivery, imaging, and sensors. With increased use of NPs and the emergence of consumer products containing NPs, there are growing concerns for the safety of NPs. Among many different types of NPs, gold nanoparticles (GNPs) are popular materials for various biomedical applications. GNPs can be fabricated in various forms using different concentrations of growth-directing surfactant. In this mini-review, we summarize the recent advancements made in the field of safety and biomedical applications of GNPs, and show that GNPs can also be applied in the ablation of thyroid cancer remnants after surgery