无机材料/天然高分子复合微球的制备研究进展

微球是一种新型药物载体,具有很大的开发与应用潜力.天然高分子具有良好的生物相容性、可降解性,易在生物体内分散,可制备成微球.无机材料(主要为无机矿物)力学性能优良,且价廉易得.通过天然高分子与无机材料两者耦合杂化作用,可优势互补、协同增效,进而产生许多优异的理化性能.使用无机材料改性天然高分子,通过乳化交联法、溶液混合法、原位合成法、挤出法等多种方法可制备得到无机材料/天然高分子复合微球.将无机材料/天然高分子复合微球应用于药物传递系统中,缓释效果明显,安全无毒害,且载体材料价格相对低廉,对于开发新型药物载体具有一定的意义.本文综述了近年无机材料/天然高分子复合微球的制备、载药与释药性能的相关研究,分析了常用制备方法的利弊,展望了复合微球的发展方向.     

高分子前药研究进展

高分子前药可以控制药物释放速度,降低小分子药物的毒副作用,减少抗药性,增强抗肿瘤药物的靶向性和选择性,提高多肽、蛋白质和核酸类药物的稳定性和有效利用率,引起国内外广泛关注.本文综述了近年来高分子药物的研究进展,主要从高分子载体材料的选择与改性对载药量、生物相容性和肾排泄的影响,以及化学合成过程中载体和药物末端的修饰、空...     

蛋白质高分子药物载体研究进展

作为一类具有独特优势的生物高分子,蛋白质具有很好的生物相容性、生物可降解性、生物稳定性、极低的细胞毒性,且具有较高的载药性。在现有的多种药物载体中,基于动物蛋白的药物载体是最有潜力和值得关注的载药系统。常用于药物载体的动物蛋白中,使用较多的是白蛋白、胶原蛋白、乳清蛋白、角蛋白等。本文就几类重要的动物蛋白质载体的研究进展进行综述,并指出蛋白质高分子药物载体的发展方向。     

热敏性可降解高分子胶束药物载体的研究进展

近年来刺激响应性聚合物胶束作为一种极有潜力的纳米药物载体得到了越来越广泛的关注,也是高分子领域研究的热点。本文概述了载药高分子胶束的发展特点和应用面临的主要困境,主要总结了温度敏感性高分子及其胶束的类别和特点,并重点阐述了热敏性可降解高分子及其胶束药物载体的最新研究进展,探讨了高分子胶束药物载体进入临床应用面临的挑战和解决问题的一些简单思路,相信多功能化的稳定的温敏性可降解载药高分子胶束系统在解决临床治疗问题上前景光明。     

天然高分子药物微球载体材料的研究进展

综述了国内外在天然高分子药物微球载体材料研究及应用中的进展状况,主要从天然高分子药物微球载体材料的分类、微球的制备方法及特点、载药微球的给药途径和应用等进行概括,并对目前所存在的问题进行了描述。     

乳酸-磷酸酯共聚物为载体的高分子药物的合成及其控释研究

以5-氟尿嘧啶(5-FU)为药物模型,以乳酸-磷酸酯共聚物为高分子药物载体,合成了侧链带药的乳酸-磷酸酯共聚物药物。用¹HNMR、IR、UV谱对其结构进行了表征。测定高分子药物中5-FU的含量,研究了高分子药物的体外释药性能及共聚物组成对释药性能的影响。     

高分子药物学的研究进展与期盼

自从20世纪70年代提出高分子前药的概念以来,伴随着纳米技术的发展,"高分子药物学"作为高分子科学和材料学、纳米科学、药物学、临床医学、分析科学的交叉学科,正在悄然形成.本文综述了近年高分子药物在药物化学、制剂学、药效学等方面所取得的进展,概述了高分子药物的药理学和药代动力学与小分子药物的区别与联系,指出了高分子药物药效学、药理学和药代动力学研究中的难题和瓶颈,特别是高分子药物可能存在的"三种状态"及从"纳米颗粒药"到"单个高分子药"再到"小分子药"的转变,分析了高分子药输送过程中存在的多重屏障如毛细血管壁、细胞外基质和细胞壁等,阐述了高分子药物的"生理靶向"和"EPR"效应的竞争,指出了高分子药在靶向输送和逆转耐药方面的优势,强调了发展相关分析方法的必要性,期盼高分子科学家与药物学家进行真诚有效的合作,大力促进我国高分子药物学和高分子药物产业的创新和发展.     

高分子载体材料在药用微球中的应用及进展

微球给药系统可实现药物的靶向给药,其在药物的缓控释放等方面表现出良好的应用前景,因而成为近年来药剂学领域的研究热点之一。高分子载体材料（Polymer Carriers）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起来的,是一类具有优良生物相容性、生物可降解性、可加工性,经过安全性评价并应用于药物制剂的高分子辅...     

乳酸—磷酸酯共聚物为载体的高分子药物的合成及其控释研究

以５－氟尿嘧啶为药物模型，以乳酸－磷酸酯共聚物为高分子药物载体，合成了侧链带药的乳酸－磷酸酯共聚物药物。用＾ＨＮＭＲ，ＩＲ，ＵＶ谱对其结果进行了表征。测定高分子药物中５－ＦＵ的含量，研究了高分子药物的体外释药物能及共聚物组成对释药性能的影响。     

基于天然高分子基元的阻隔层对磁性载药聚乳酸微球的控释作用

利用层层组装技术构建了基于天然高分子壳聚糖和海藻酸钠的阻隔层, 并研究了该阻隔层对磁性载药聚乳酸微球的药物释放作用. 实验结果表明, 阻隔层能够有效抑制模型药物的突释, 具有延缓药物释放的效果. 具有阻隔层的磁性载药体系具有药物释放平缓和生物相容性高等特点, 是理想的磁靶向载药体系.     

聚肽接枝共聚物的自组装行为研究

Polymeric micelles of poly(γ-benzyl L-glutamate)(PBLG)-poly(ethylene oxide)(PEO) graft copolymer were prepared by the dialysis method in deionized water. Fluorescence spectroscopy, nuclear magnetic resonance(NMR) and transmission electron microscope(TEM) were used for the investigation of the self-assembly of PBLG-PEO graft copolymer. Fluorescence spectrosco0y measurements suggest that PBLG-PEO graft copolymer associates to form polymeric micelles in water. ^1H NMR measurements further prove that in aqueous medium PBLG-PEO graft copolymer could assemble into polymeric micelles with PBLG segments as the hydrophobic inner core and PEO segments as the hydrophilic shell. The results of the TEM observations show that the polymeric micelles of PBLG-PEO graft copolymer are almost spindly shaped, which are different from the morphology of the spherical micelles formed by PBLG-PEO block copolymer. Polymeric micelles formed by polypeptide copolymer have potential application as drug carrier in controlled-release delivery system.     

Polymeric Nitrofuran Derivatives. II. Chemical Modification of Functionalized Resins with Nitrofuran Derivatives

Polymeric nitrofuran derivatives have been synthesized by chemical modification of macroporous styrene-divinylbenzene copolymers with low molecular weight nitrofurans. The 5-nitrofuryl groups are covalently attached to the polymeric carrier by azomethine, ester, N-alkyl, and sulfamide links, respectively. Comparative hydrolysis studies and biological tests of the modified resins suggested that the polymeric carrier-bound nitrofurans are antimicrobially active. The polymeric nitrofurans have been characterized by IR and “C-solid-NMR spectroscopy”.     

聚合物胶束作为药物载体的研究进展

聚合物胶束作为药物载体具有其独特的优势。本文综述了形成聚合物胶束的两亲性共聚物的组成、聚合物胶束的形成、形态以及近些年来作为药物载体的研究进展。     

Advanced drug delivery systems: Nanotechnology of health design A review

Nanotechnology has finally and firmly entered the realm of drug delivery. Performances of intelligent drug delivery systems are continuously improved with the purpose to maximize therapeutic activity and to minimize undesirable side-effects. This review describes the advanced drug delivery systems based on micelles, polymeric nanoparticles, and dendrimers. Polymeric carbon nanotubes and many others demonstrate a broad variety of useful properties. This review emphasizes the main requirements for developing new nanotech-nology-based drug delivery systems.     

基于温敏性双亲嵌段共聚物的纳米胶束作为药物载体的研究

温度敏感性双亲嵌段共聚物由于其潜在的应用价值而引起广泛的关注。在药物控制释放领域,基于温敏性嵌段共聚物的纳米胶束作为药物载体显示了诸多特异的性能。在嵌段共聚物中引入具有温度敏感性的链段,使聚合物胶束具备天然被动靶向功能的同时,赋予了其主动靶向给药功能。本文从温度敏感性双亲嵌段共聚物的分子设计、合成、自组装性质和胶束的载药释药行为等方面进行了相关总结。重点介绍了含聚N-异丙基丙烯酰胺链段双亲嵌段共聚物的相关研究进展。     

Immunopharmacological Properties of Methacrylic Acid Polymers as Potential Polymeric Carrier Constituents of Anticancer Drugs

Cytostatic chemotherapeutics provide a classical means to treat cancer, but conventional treatments have not increased in efficacy in the past years, warranting a search for new approaches to therapy. The aim of the study was, therefore, to obtain methacrylic acid (MAA) (co)polymers and to study their immunopharmacological properties. 4-Cyano-4-[(dodecylsulfanylthiocarbonyl)sulfanyl] pentanoic acid (CDSPA) and 2-cyano-2-propyl dodecyl trithiocarbonate (CPDT) were used as reversible chain transfer agents. Experiments were carried out in Wistar rats. The MTT assay was used to evaluate the cytotoxic effect of the polymeric systems on peritoneal macrophages. An experimental tumor model was obtained by grafting RMK-1 breast cancer cells. Serum cytokine levels of tumor-bearing rats were analyzed. The chain transfer agents employed in classical radical polymerization substantially reduced the molecular weight of the resulting polymers, but a narrow molecular weight distribution was achieved only with CDSPA and high CPDT concentrations. Toxicity was not observed when incubating peritoneal macrophages with polymeric systems. In tumor-bearing rats, the IL-10 concentration was 1.7 times higher and the IL-17 concentration was less than half that of intact rats. Polymeric systems decreased the IL-10 concentration and normalized the IL-17 concentration in tumor-bearing rats. The maximum effect was observed for a MAA homopolymer with a high molecular weight. The anion-active polymers proposed as carrier constituents are promising for further studies and designs of carrier constituents of drug derivatives.     

Characterization of novel pH-sensitive polymeric micelles prepared by the self-assembly of amphiphilic block copolymer with poly-4-vinylpyridine block synthesized by mechanochemical solid-state polymerization

We fabricated novel pH-sensitive polymeric micelles consisting of amphiphilic block copolymer containing pyridyl groups as side chains in the hydrophobic block. The number average particle diameter of the polymeric micelles at pH 7 was approximately 200 nm. A decrease in pH resulted in deformation of the polymeric micelles over a very narrow pH range (between pH 5.7 and 5.6). Interestingly, micellization and demicellization occurred reversibly in this narrow pH range. Polymeric micelles incorporating 5-fluorouracil (5FU) were also prepared. Decreasing the pH of this polymeric micelle solution from 7 to 5.5 resulted in the rapid release of 5FU at pH 5.6; the drug was completely released within 30 min. These results suggest that deformation of the polymeric micelles caused the rapid release of 5FU.     

Stimulus-responsive polymeric nanoparticles for biomedical applications

Polymeric nanoparticles with unique properties are regarded as the most promising materials for biomedical applications including drug delivery and in vitro/in vivo imaging.Among them,stimulus-responsive polymeric nanoparticles,usually termed as intelligent nanoparticles,could undergo structure,shape,and property changes after being exposed to external signals including pH,temperature,magnetic field,and light,which could be used to modulate the macroscopical behavior of the nanoparticles.This paper reviews ...     

Syntheses,electrochemistry and cytotoxicity of ferrocene-containing polyaspartamides as water-soluble polymeric drug carrier/drug conjugates

A general strategy towards the syntheses of water-soluble polymeric drug carriers and their drug conjugates is described. Methods of drug uptake by cells, drug release from the polymeric carrier and the relevance of electrochemistry to drug activity of the ferrocenyl group are highlighted. The advantages of these polymeric systems are demonstrated utilising cytotoxicity results of a polyaspartamide-ferrocenyl conjugate.