嵌段共聚物胶束作为药物载体的研究进展

嵌段共聚物胶束通过物理和化学方法将难溶性药物和基因治疗药物增溶,可实现主动或被动靶向给药.综述了嵌段共聚物胶束的特点、载体的制备方法、载药能力、药物的释放和研究实例.     

嵌段共聚物胶束作为抗肿瘤药物载体的研究进展

嵌段共聚物胶束作为抗肿瘤药的载体，可降低网状内皮系统对抗肿瘤药物的识别和摄取、减少药物的肾排泄及其在正常组织的积蓄；增加了药物在血中的稳定性和在肿瘤组织的积蓄量，是一种长效、高效、安全的抗肿瘤药物载体。嵌段共聚物胶束在肿瘤治疗中的应用具有广阔的发展前景，为肿瘤治疗带来了新的曙光。     

聚合物胶束作为药物载体及其在肿瘤靶向方面的研究进展

聚合物胶束具有粒径小、稳定性高、滞留时间长、良好的生物相容性等特点,这些优良性质使得聚合物胶束作为药物载体具有许多独特的优势。近年来,涌现了许多围绕聚合物胶束设计肿瘤靶向给药系统的报道,包括利用肿瘤的病理学性质,设计被动靶向给药系统和对聚合物胶束进行表面修饰,设计主动靶向给药系统。本文主要综述了聚合物胶束作为肿瘤靶向药物载体的研究进展。     

大分子胶束作为药物载体的应用

大分子胶束可以作为疏水性药物和核酸、蛋白等药物的载体，并具有高效、长效、安全性和靶向性等特点，是一种很有发展前景的药物载体。现主要从大分子胶束的特点、载药机制、形成材料、制备方法、包载的药物及其靶向性方面综述大分子胶束作为药物载体的应用。     

药物纳米载体——聚合物胶束的研究进展

目的对目前聚合物胶束作为药物纳米载体的国内外研究进展进行综述。方法参考近年来国内外文献50篇,从聚合物胶束的类别和构成,药物的包载方法,药物从聚合物胶束中的释放,聚合物胶束的稳定性,聚合物胶束的表征,聚合物胶束对药物的药动学和体内分布的影响以及聚合物胶束作为药物载体的应用等几个方面系统地介绍了其研究进展。结果聚合物胶束包括自聚集胶束,单分子胶束和交联的胶束,可采用化学结合法、物理包载和聚离子复合法包载药物;药物分子在聚合物胶束中的分布以及聚合物的降解行为决定了药物的释放速度;聚合物胶束的热力学和动力学稳定性与其结构组成密切相关;载药聚合物胶束可改变药物的药动学和体内分布;目前聚合物胶束已被用于作为肿瘤药物、难溶性药物的载体,也可作为药物药物经皮传递载体和药物的缓释载体,发展前景较好,但同时也面临挑战。结论聚合物胶束作为药物的纳米载体具有广泛的应用前景。     

星形聚合物胶束作为药物载体的研究进展

星形聚合物胶束是一类新型纳米药物载体,它具有独特的分枝结构,所形成的单分子胶束具有理想的粒径和稳定性,可使难溶性药物有效增溶,降低药物毒性,延长体循环时间,提高生物利用度和安全性。星形聚合物胶束作为药物载体具有良好的缓释效果,通过在聚合物表面接枝功能基团可产生靶向释放效果,聚酯结构的星形聚合物还具有良好的降解性能,不在体内蓄积产生毒副作用。本文对星形聚合物的合成及其胶束作为药物载体的理化性质、载药优势、制备方法等的研究进展进行综述。     

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…     

聚氨基酸胶束作为肿瘤靶向药物载体的研究进展

聚氨基酸作为一种毒副作用低、生物相容性好的高分子材料,被广泛应用于肿瘤以及基因治疗。聚氨基酸链的活性基团丰富,可通过多种反应途径与目的基团连接,从而实现药物的主动靶向性。同时又因为聚合物胶束的粒径为1～100纳米,而肿瘤组织毛细血管壁与正常组织血管壁相比间隙较宽,可以形成“渗透滞留”效应（EPR效应）,使载药纳米粒在肿瘤组织中不断蓄积,进而实现药物在肿瘤中的被动靶向性,本文简要综述了载药聚天冬氨酸、聚谷氨酸以及聚赖氨酸聚合物胶束的理化性质及优势,如肿瘤靶向性、缓释性等,并对近年来聚氨基酸胶束的研究进展进行综述。     

药物胶束嵌段共聚合物的研究进展

聚合物胶束作为药物载体具有其独特的优势。近年来纳米材料发展迅速，给聚合物胶束的发展带来了新机遇。本文就用于制备药物胶束的嵌段共聚合物近年来的进展作综述。     

药物胶束嵌段共聚合物的研究进展

聚合物胶束作为药物载体具有其独特的优势.近年来纳米材料发展迅速,给聚合物胶束的发展带来了新机遇.本文就用于制备药物胶束的嵌段共聚合物近年来的进展作综述.     

聚合物胶束在肿瘤靶向给药系统中的研究进展

摘 要 聚合物胶束作为一种有效的药物运送载体已经受到广泛关注,其在肿瘤治疗方面具有高效,长效和高载药量等优势。本文综述了聚合物胶束的类型,制备材料,载药方法,主要讨论了肿瘤靶向载药系统中的靶向策略和应用实例。     

壳聚糖在药物缓释中的应用

壳聚糖作为一种资源丰富的新型天然高分子化合物，具有良好的生物相容性，低毒性，易于吸收等特点，是一种良好的药物释放载体。文章综述了壳聚糖微球，纳米粒，膜等的制备方法，缓释效果及其在临床上的应用。     

温敏在体凝胶给药系统的研究与应用

综述N-异丙基丙烯酰胺类聚合物、聚氧乙烯-聚氧丙烯共聚物、聚氧乙烯-聚乳酸羟基乙酸共聚物和多糖类衍生物等温敏聚合物的性质、特点、胶凝机制及在温敏在体凝胶给药系统中的应用进展。温敏在体凝胶作为一种智能水凝胶,可用作药物缓、控释和靶向输送的有效载体。     

关于靶向制剂脂质体的微课设计

随着现代社会的发展和科技的日益进步,互联网逐渐在人们的生活中普及,学生进行线上学习已成为解决课堂上重难点、查漏补缺的利剑,教师紧跟时代的发展步伐,在靶向制剂——脂质体的理论教学课程中,结合微课短小紧凑的特点将脂质体课程相关重难点制作成微课,以便能提高课堂内外,线上线下的教学效率。主要包括教学背景、教学目标与重难点、教学方法和策略等几个方面,目的在于提高教学质量,服务广大学生群体。     

抗胞内菌感染的靶向载药系统的研究进展

摘 要细胞内病原体感染是临床抗感染治疗面临的严峻挑战。现阶段,临床上抗胞内菌感染治疗的常用策略是长周期使用高剂量抗菌药物,这不仅给患者带来了严重的不良反应,也给全社会造成了巨大的经济压力。因此,开发新策略使在体外试验中显示良好杀菌效果的抗菌药物更好地杀灭胞内菌显得尤为重要。用适当的载体将药物包埋或包封能够更好地控制其药物动力学行为,能够有效提高抗菌药物胞内抗菌的有效生物利用度。本文就近年来抗胞内菌的靶向载药系统的研究进行综述。     

Pharmacokinetics and Brain Uptake of Biotinylated Basic Fibroblast Growth Factor Conjugated to a Blood-Brain Barrier Drug Delivery System

Human basic fibroblast growth factor (bFGF) is a potent neuroprotective agent. The clinical efficacy of this neurotrophin, however, is restricted by poor permeability across the blood-brain barrier (BBB). This study was designed to test the hypotheses that bFGF will retain its biological activity and have an enhanced BBB transport after re-formulation and conjugation to a BBB peptide drug delivery vector. The BBB delivery vector is comprised of a conjugate of streptavidin (SA) and the murine OX26 monoclonal antibody against the rat transferrin receptor, and the conjugate of biotinylated bFGF (bio-bFGF) bound to a vector is designated bio-bFGF/OX26-SA. A radioreceptor binding assay shows that the native bFGF, bio-bFGF, and bio-bFGF/OX26-SA conjugate have IC 50 values of 0.12, 0.40, and 0.56 nM, respectively. After an IV bolus injection to the rat, [125 I]-bio-bFGF is avidly taken up by peripheral organs, with low brain uptake at 60 min, 0.010 ± 0.004% of injected dose (ID)/g brain. By contrast, the brain uptake of the [125 I]-bio-bFGF/OX26-SA is increased 5-fold to 0.050 ± 0.011%ID/g, although the uptake of the conjugate by peripheral tissues was decreased relative to the unconjugated bio-bFGF. In conclusion, conjugation of bio-bFGF to a BBB drug delivery vector (a) causes only a minor decrease in affinity for the bFGF receptor, (b) decreases the peripheral organ uptake of the bFGF, and (c) increases the brain uptake of the neurotrophin. The re-formulation of bFGF to enable receptor-mediated transcytosis across the BBB may improve the therapeutic index of this neurotrophin as a neuroprotective agent.     

Improved Delivery Through Biological Membranes LX: Intradermal Targeting of Acyclovir Using Redox-Based Chemical Drug Delivery Systems

Two types of novel chemical drug delivery systems (CDS's) for acyclovir, A-CDS-1 (based on oxidation, which utilized the 1,4-dihydrotrigonelline moiety) and A-CDS-2 (based on reduction, which utilized the lipoic acid moiety), were designed to create reservoirs of metabolic precursors for the enhanced local delivery of the antiviral agent acyclovir to the skin. They were evaluated in two-compartment diffusion cells using hairless-mouse skin in vitro. This approach could be useful in the treatment of mucocutaneous herpes simplex virus (HSV-1) infection in the epidermal region of the skin. Upon application to the freshly excised hairless-mouse skin, A-CDS-1 was rapidly oxidized to form the quaternary metabolite AQ⁺, which was extensively localized in the skin. AQ⁺ then served as a reservoir for the release of the antiviral agent in the skin. A-CDS-1 delivered almost equivalent amounts of acyclovir not only to the skin but also transdermally. On the other hand, A-CDS-2 specifically localized acyclovir delivery to the skin as opposed to transdermal delivery. Due to their redox properties, both CDS's demonstrated significant depot formation of metabolic precursors, thus enhancing intradermal acyclovir delivery. The CDS's exhibited greater skin membrane partition coefficients than the parent underivatized acyclovir and were able to release the antiviral agent in the skin tissue. The CDS's were susceptible to hydrolysis in biological media, resulting in the release of acyclovir under near physiological conditions. Thus, the CDS's can serve to enhance intradermal targeting and delivery of the antiviral agent acyclovir.     

Polymer Controlled Drug Delivery System for Growth Hormone

The use of biomaterials as vehicles for pharmacological agents, hormones, and growth factors is at times the best treatment for controlled local administration. Our study was designed to evaluate the in vitro biocompatibility and potential clinical use of a new polymer, hydroxyethyl methacrylate-vinyl pirrolidone. Human fibroblasts were incubated in the presence of the polymer and/or growth hormone, and evaluation was made of both the rate of polymer and hormone degradation and the proliferative effect on the fibroblast population. Results indicate that this polymer is biodegradable and lacks toxicity toward these cells. The hormone was slowly released, as suggested by enhanced cell proliferation.     

A Cell-Based Drug Delivery System for Lung Targeting: II. Therapeutic Activities on B16-F10 Melanoma in Mouse Lungs

The in vitro and in vivo anticancer activities of doxorubicin-loaded B16-F10 murine melanoma cells (DLTC) were evaluated. DLTC showed similar growth-inhibitory effects against live B16-F10 cells with doxorubicin solution in cell culture system, with the IC₅₀     

结合目前我国各级药检机构药品检验能力论提高药检能力的方法

目的：了解目前各级药检机构的药品检验能力．为药品安全“十二五”规划的顺利推进提供建议。方法：对部分省级市级药品检验所进行问卷调研,从人员、仪器、检验能力培训三方面进行统计汇总。结果：接受调查的省级和市级药检机构在人员、仪器、检验能力培训等方面均与药品安全“十二五”规划提出的要求存在一定的差距。结论：通过充实技术人员编制,配备必要的仪器,并进行适当的技术培训．可以有效提高药品检测的整体能力．确保药品安全“十二五”规划的顺利完成。