特殊性能毫微粒靶向制剂的研究进展

毫微粒是近年来研究的一咎固态胶体药物释放体系，是将药物溶解、夹嵌、包裹或吸附于聚合材料载体上制成的胶体固态颗粒，其粒径一般为１０－１００ｎｍ，是靶向制剂中粒径最小的一种。由于其粒子细，因而可供静脉注射和做成冻干品。毫微粒制品较脂质体稳定且易制易，是比较理想的靶向载体。本文就免疫毫微粒、磁性毫微粒、磷脂毫微粒和光敏毫微粒的特性、制备及用途作了简要的介绍。     

微粒作为靶向制剂载体的研究进展

综述了脂质体、微球、毫微粒、乳剂、红细胞５种包蔽型微粒载体系统和合成大分子、生物大分子、抗体３种化学交联型微粒载体系统的研究进展。微粒作为靶向制剂载体的研究已经取得了重大成绩，并仍在迅速发展中     

毫微粒载体研究进展

毫微粒作为药物载体具有许多优点，现已成为药剂学界研究的前沿热点之一。本文以三种常见的可生物降解聚合材料为例，综述了毫微粒的制备方法，同时介绍了毫微粒载体在靶向释药，性能改善方面的最新研究成果。     

口服毫微粒的研究进展

毫微粒用于口服具有诸多优点,开发潜力巨大,现已成为药剂学领域的研究热点之一。本文从制备工艺体内摄取与分布、应用等三方面综述了近年来口服毫微粒的最新研究进展,对全面了解和深入研究这类制剂具有一定的意义。     

靶向制剂的研究进展

以国内外发表的文献为依据，总结归纳了近年来靶向制剂的研究进展和存在的不足．展望靶向制剂的美好未来。     

靶向载药系统毫微粒及其应用

近年来发展了一系列新的载药系统如脂质体和纳米级大小的固态颗粒系统。后者被称作毫微粒(nanoparticles)。毫微粒用于运载药物,可以降低循环系统中游离药物或蛋白结合药物的量;减少用药量;可以使药物在某些     

Activated carbon particles as anti-cancer drug carrier into regional lymph nodes

The effect of a new dosage form for anti-cancer agents was studied on tissue distribution and compared with the aqueous solution form. The new dosage form, developed in order to distribute a greater amount of the agent to regional lymph nodes, comprises polyvinylpyrrolidone and small activated carbon particles adsorbing pepleomycin (PEP-CH) or mitomycin C (MMC-CH) in saline. Pepleomycin at 500 micrograms/kg or mitomycin C at 250 micrograms/kg were injected into the gastric wall of dogs in the new dosage form or the aqueous solution form. The activity level of the agents in tissues was bioassayed within 24 h after injection by the thin agar plate method. Statistically, the new dosage form maintained an activity level in lymph nodes that was significantly higher than the aqueous solution form (ratio of PEP-CH to solution form, 6-32 times in 24 h; MMC-CH, 100-1000 times in 6 h; p less than 0.05-0.01), and a concentration in blood that was significantly lower (PEP-CH, about 1/2 times in 2 h; MMC-CH, 1/10-1/5 times in 1 h; p less than 0.05).     

Targeted delivery of docetaxel to the metastatic lymph nodes: A comparison study between nanoliposomes and activated carbon nanoparticles

The objective of this study is to compare the targeting ability of activated carbon nanoparticles and nanoliposomes, which are used as carriers for delivering docetaxel (DTX) to the metastatic lymph nodes. In this study, we first prepared the DTX-loaded activated carbon nanoparticles (DTX-AC-NPs) by modifying the activated carbon with nitric acid oxidation and absorbing DTX in the concentrated nitro-oxide nanocarbon. We then prepared DTX-loaded nanoliposomes (DTX-LPs) by the proliposome method. The physiochemical properties of DTX-AC-NPs and DTX-LPs were carefully evaluated in vitro. The metastatic lymph node uptake and the injection site retention were investigated by analyzing the DTX concentration in metastatic lymph nodes and injection sites. The result showed that DTX-AC-NPs and DTX-LPs with suitable and stable physicochemical properties could be used for in vivo lymph node targeting studies. DTX-AC-NPs significantly increased DTX-AUC_(0–24) and prolonged DTX-retention in metastatic lymph nodes compared to DTX-LPs and non-modified activate carbon in vivo. This study demonstrated activated carbon nanoparticles may be potential intralymphatic drug delivery system to preferentially target regional metastatic lymph nodes.     

纳米载体药物应用的研究进展纳米载体药物应用的研究进展

载体药物是随着药物学研究、生物材料科学和临床医学的发展而新兴的给药技术。药物通过载体进入人体 ,载体对药物吸附、包裹和键合 ,使药物释放部位、速度和方式等具有选择性和可控性 ,实现药物的缓释和靶向传输 ,从而更好地发挥药物治疗效率。载体药物技术的关键是载体材料的选择 ,目前已有各种高分子材料和无机材料被用于载体药物的研究 ,但对材料的选择必须满足组织、血液、免疫等生物兼容性的要求[1] 。此外 ,载体药物的制备也很重要 ,因为这将影响到载体药物的给药效率。最近已有很多方法应用于这一领域 ,纳米技术的应用已引起关注。纳…     

碳纳米管作为药物载体的研究进展

新型药物载体的开发对药物的研究具有举足轻重的作用。碳纳米管具有独特的中空结构和纳米管径，可用作药物载体。采用肽、蛋白、核酸及药物分子修饰的碳纳米管作为载体，可运载生物活性分子进入细胞且不产生毒性。本文综述了近年来修饰碳纳米管作为药物载体的研究进展，评述了碳纳米管的细胞穿透性能和细胞毒性，概述了碳纳米管功能化修饰的方法。随着碳纳米管在药物载体领域研究日趋深入，碳纳米管修饰方式与其细胞穿透性能的相互关系、尺寸效应将会深入研究。制备溶解性好、低毒性的修饰碳纳米管作为药物载体，将是今后研究的主要方向。     

金属卟啉介导抗癌药物研究

目的 提高现有抗癌药物的靶向性，降低其不良反应。方法 采用对于增殖异常的组织具有一定亲和力的卟啉类物质作为先导化合物，对甲氨蝶呤进行修饰，合成四－对羟基苯卟啉（ZnⅡ）甲氨蝶呤衍生物，并使用红外、紫`外核磁和元素分析等手段对该化合物进行表征。结果 发现该化合物在细胞水平上抗EAC的IC50值为0.99mg/L，对小鼠体内的抗EAC实验表明在与甲氨蝶呤对照组折合相同剂量的前提下，动物死亡率下降了50％，但抑瘤率仍可保持在60％以上。结论 可能是由于金属锌卟啉中，锌有空的价电子轨道，在特定条件下，可以接受细胞膜上配体的孤电子对或成键π电子，形成轴向配位化学建，使得卟啉环易于吸附并穿过细胞膜，在卟啉的介导下，锌卟啉甲氨蝶啉衍生物产生靶向性分布，从而减少了它的不良反应，并保留其抗癌活性。     

新型抗癌药甲啶铂在多壁碳纳米管玻碳电极上的电化学及DPV测定研究

目的:研究新型抗癌药甲啶铂在多壁碳纳米管玻碳电极(MWCNTs/GCE)上的电化学行为,建立DPV法测定实际样品中甲啶铂的含量。方法:循环伏安法(CV)和差分脉冲伏安法(DPV)。结果:甲啶铂在MWCNTs/GCE上有1对明显的准可逆氧化还原峰,氧化峰电位Epa与还原峰电位Epc分别为0.5 V、-0.37 V,△E=0.87 V,Ipa/Ipc=1.30。在优化条件下,甲啶铂的DPV氧化峰电流Ipa与其浓度C在3.01～158.00μg.mL-1范围内呈良好的线性关系:Ipa=1.735C-0.0107(r=0.9997,n=9)。检出限为0.64μg.mL-1。样品测定平均加标回收率为100.4%,RSD为0.8%。结论:本方法简便灵敏、准确可靠,可用于甲啶铂的定量测定。     

Polymeric micelles as a new drug carrier system and their required considerations for clinical trials

Importance of the field: A polymeric micelle is a macromolecular assembly composed of an inner core and an outer shell, and most typically is formed from block copolymers. In the last two decades, polymeric micelles have been actively studied as a new type of drug carrier system, in particular for drug targeting of anticancer drugs to solid tumors.

Areas covered in this review: In this review, polymeric micelle drug carrier systems are discussed with a focus on toxicities of the polymeric micelle carrier systems and on pharmacological activities of the block copolymers. In the first section, the importance of the above-mentioned evaluation of these properties is explained, as this importance does not seem to be well recognized compared with the importance of targeting and enhanced pharmacological activity of drugs, particularly in the basic studies. Then, designs, types and classifications of the polymeric micelle system are briefly summarized and explained, followed by a detailed discussion regarding several examples of polymeric micelle carrier systems.

What the reader will gain: Readers will gain a strategy of drug delivery with polymeric carriers as well as recent progress of the polymeric micelle carrier systems in their basic studies and clinical trials.

Take home message: The purpose of this review is to achieve tight connections between the basic studies and clinical trials.     

纳米多孔二氧化硅作为药物载体的研究进展

目的介绍几种纳米多孔二氧化硅作为药物载体的应用及最新发展动态。方法以国内外有代表性的文献资料31篇为依据,对介孔二氧化硅、二氧化硅气凝胶、微粉硅胶等几种多孔二氧化硅药物载体的结构特性、应用及发展动态进行分析、整理和归纳。结果纳米多孔二氧化硅作为药物载体,借助于其纳米孔道结构、形貌或孔道的控制及表面功能化修饰,可以实现药物的速释、缓释及pH或温度敏感释放。结论纳米多孔二氧化硅作为药物载体具有广阔的应用前景。     

树枝状聚合物聚酰胺-胺作为药物载体应用研究进展

树枝状聚合物聚酰胺-胺(PAMAM)是一种三维的、高度枝化的树枝状高分子,具有单一分散性、无免疫原性、细胞毒性较低、生物可降解等特性,目前作为药物载体在药学领域引起了高度关注。文中分别综述了其载药机制及其在静脉、口服、经皮、眼部等不同给药途径的应用研究进展。研究发现其载药机制主要为物理包埋载药与静电、共价结合载药。PAMAM作为药物载体能够增加药物的溶解度,不同途径给药后能延缓药物的释放,增加药物皮肤渗透系数,延长角膜滞留时间,从而增加药物的生物利用度,是一种颇具发展潜力的新型药物载体。     

淋巴结病理学检查在药物安全性评价中的特点和意义

淋巴结(LN)是重要的外周免疫器官,免疫应答发生的场所。LN形态结构的改变可敏感提示药物免疫毒性的有无,表明LN毒性病理学评价是免疫毒性筛选的有力手段。本文综述了LN复杂的生理结构和毒性病理学变化特点,并阐述了LN病理检查在药物安全性评价中的作用和意义。