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     

载药纳米微粒的应用及研究进展

目的：对纳米、纳米科反及其在药物研究中的应用进行介绍。方法：通过对国内外文献的总结。概述了载药纳米微粒中的普通载药微粒,控释载药微粒、靶向定位载药微粒、载药磁性微粒等类别,介绍了复乳化法技术、超声乳化法、等电临界法、氧化还原法等制备载药纳米微粒的方法。结果：纳米技术与现代医药学结合的产物-载药纳米微粒具有易吸收、定向性强等优点。结论：载药纳米微粒的研究开发可解决口服易水解药物的给药途径,延长药物的体内半衰期,更精确的靶向定位给药。减少药物不良反应,消除生物屏障对药物作用的影响。     

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。     

载药磁性纳米微粒靶向治疗恶性肿瘤的研究与临床应用

随着纳米材料和纳米技术的发展,一种将载药磁性纳米微粒用作抗肿瘤靶向治疗已成为可能,并以其增加药物对靶细胞的指向性,降低对正常细胞的毒性和治疗安全性等诸多优越特性倍受国内外广泛关注。     

载药纳米微粒的研究进展

载药纳米微粒是纳米技术与现代医药学结合的产物,是一种新型的药物和基因输送载体。它具有缓释药物、透过生物屏障靶向输送药物、将 DNA导入细胞浆质内和建立新的给药途径等优势。     

淋巴靶向制剂——吸附抗癌药毫微粒活性炭的研究进展

目的介绍新型淋巴靶向制剂———吸附抗癌药毫微粒活性炭的研究进展。方法依据近年来的文献 ,对活性炭的制备工艺及体内外性质等方面进行了综述。结果活性炭具有很强的吸附功能 ,普通市售活性炭仅用作脱色、吸附热原与除味等。以微粒球磨机为粉碎器械 ,可加工制备粒径达1 0 0nm左右的纳米炭微粒 ,具有优越的淋巴趋向性。结论吸附抗癌药毫微粒活性炭在临床治疗癌症方面具有良好的运用前景     

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。     

纳米药物在肝癌靶向治疗中的研究进展

目的了解肝癌靶向治疗的纳米药物种类及不同靶向机制,为纳米药物的进一步研发提供参考。方法对国内外相关文献进行归纳和综述。结果和结论纳米药物在肝癌靶向治疗中有着独特的优势,具有广阔的研究和开发前景。     

靶向制剂研究进展

靶向制剂具有提高靶组织的药理作用强度和控制释药,恒定血药浓度,降低全身的不良反应等鲜明特点,是一种较理想的给药方式,因此靶向给药系统(TDDS)已成为现代药剂学的重要研究热点之一.本文就靶向制剂的研究近况及其进展进行概括.     

靶向哺乳动物雷帕霉素靶蛋白治疗卵巢癌的研究进展

哺乳动物雷帕霉素靶蛋白（Mammalian target of rapamycin,mTOR）是调控细胞代谢、生长和增殖等重要生命活动的蛋白激酶,mTOR异常表达在卵巢癌发生发展中起重要作用,已成为卵巢癌治疗的有效靶点。mTOR抑制剂雷帕霉素及其同系物能够抑制卵巢癌细胞生长和血管生成,并同其他抗肿瘤药物有协同作用,靶向m-IOR的研究将为卵巢癌的临床治疗带来新希望。     

Aptamer-based nanoparticles for cancer targeting

Abstract

Background: The use of mesoporous silica for cancer targeting is increasing rapidly. The association between rigid model of nanoparticles such as mesoporous silica and biological compounds with affinity for oncological diseases is a very promising drug targeting system nowadays.

Methods: In this study, we used the mesoporous silica (SBA-15) associated with aptamer (functionalized for the tumor marker MUC-1).

Results: The results obtained in the characterization were quite interesting and demonstrated that the silica produced were very uniform and with a size range of 50–100?nm. Thus, the results of cytotoxicity demonstrated that there is no cytotoxicity related to the nanoparticle.

Conclusion: We conclude that although further studies are required, the nanoparticle mesoporous silica model loaded with aptamer is very functional and its use can be widespread for other application especially in nuclear medicine.     

多柔比星纳米粒在大鼠体内的靶向性分布研究

目的 研究多柔比星纳米粒（NDXRB）经肝动脉给药后在大鼠体内靶向性分布。方法 SD大鼠30只,随机分为两组,每组各15只,经肝动脉按2mg/kg的剂量分别注入NDXRB或DXRB水溶液,于给药后的1、5、15h各处死5只大,分别提取心、肝、脾、肺、肾和血浆样品,以高效液相色谱法测定DXRB的浓度。结果15h以内NDXRB组大鼠肝和脾中DXRB浓度均极显著高于DXRB组（P＜0．01）,而血浆、心和肺中DXRB浓度极显著低于DXRB组（P＜0．01）。肾组织中DXRB组浓度在5h以内显著高于NDXRB组（P＜0．05）,15h时两组间无显著性差异（P＞0．05）。各时间点均以心脏药物浓度为最低。结论 NDXRB肝动脉给药后改变了DXRB的体内分布特征,在对肝脏和脾脏表现出显著靶向性的同时在心脏的分布显著减少。     

纳米粒与靶向制剂在抗肝癌药物中的应用

抗肿瘤药物的发展已进入新时期,纳米技术、新型靶向制剂的研究日趋成熟。本文通过检索大量相关文献,对纳米粒和靶向制剂在肝癌中的应用进行分析总结。     

功能化纳米粒在脑靶向递药中应用的研究进展

血脑屏障的存在,导致药物不能有效到达靶部位发挥作用,极大的影响神经系统药物的发展和进步。纳米技术已被证明是用于脑靶向治疗的一种有效工具,尤其在脑肿瘤和神经退行性疾病中应用甚广。功能化纳米粒通过表面修饰等提高药物的顺应性,在药物原来的治疗基础上,达到更加精准的靶向性,高效率在靶部位聚集,起到治疗作用。本文主要综述功能化纳米粒及其功能化策略,总结了影响功能化纳米粒脑靶向运输的因素,同时对功能化的纳米粒在脑部疾病治疗中的优势和应用进行阐述,为其相关研究提供参考。     

作用于Met靶点的非小细胞肺癌治疗药物研究进展

继表皮生长因子受体(EGFR)基因突变和间变性淋巴瘤激酶(ALK)基因融合之后,Met基因激活突变和扩增被认为是非小细胞肺癌(NSCLC)下一个重要的驱动基因,它与肿瘤的增殖、侵袭、转移及血管生成密切相关,已成为靶向治疗领域研究的一大亮点。主要靶向治疗药物可分为抗HGF单克隆抗体、抗c-Met单克隆抗体和小分子抑制剂3类,并多已进入临床试验阶段。对作用于Met靶点的非小细胞肺癌治疗药物的研究进展进行综述。     

Preparation of estradiol chitosan nanoparticles for improving nasal absorption and brain targeting

The aim of this study is to observe the synergistically enhanced percutaneous penetration and skin analgesia of tetracaine gel containing menthol and ethanol through experimental and clinical studies. Four anesthetic gels containing 4% tetracaine in carbomer vehicle named T-gel (containing no menthol or ethanol), 5%M/T-gel (containing 5% menthol), 70%E/T-gel (containing 70% ethanol, an optimal concentration for antiseptic), and 5%M+70%E/T-gel (containing both 5% menthol and 70% ethanol), respectively, were fabricated. The in vitro mouse skin permeation was investigated using a Franz diffusion cell. The mouse skin morphology was examined by a scanning electron microscope. The in vivo skin analgesic effect in mice was evaluated using the von Frey tests. To determine the efficacy of tetracaine gels for managing the pain in human volunteers, a paralleled, double-blinded, placebo-controlled, randomized controlled trial design combined with verbal pain scores (VPS) was performed. The combination of menthol and ethanol (5%M+70%E/T-gel) conferred significantly higher tetracaine diffusion across full-thickness mouse skin than 5%M/T-gel, 70%E/T-gel, and T-gel. The ultra structure changes of mouse skin stratum corneum treated with 5%M+70%E/T-gel were more marked compared with those of any other tetracaine gel. von Frey tests in mice showed a synergistically enhanced effect of menthol and ethanol on the analgesia of tetracaine gel. The mean VPS were significantly lower for volunteers treated with 5%M+70%E/T-gel than those receiving other gels or the EMLA cream. 5%M+70%E/T-gel possessed the shortest anesthesia onset time, the longest anesthesia duration and the strongest anesthesia efficacy. Seventy percent ethanol in 5%M+70%E/T-gel not only improved the analgesic efficacy of the tetracaine gel through synergistically enhanced percutaneous permeation with menthol but also served as an antiseptic agent keeping drug application site from infection. 5%M+70%E/T-gel is a potential topical anesthesia preparation for clinical use.     

Targeted delivery of nanoparticles for the treatment of lung diseases

Targeted delivery of drug molecules to organs or special sites is one of the most challenging research areas in pharmaceutical sciences. By developing colloidal delivery systems such as liposomes, micelles and nanoparticles a new frontier was opened for improving drug delivery. Nanoparticles with their special characteristics such as small particle size, large surface area and the capability of changing their surface properties have numerous advantages compared with other delivery systems. Targeted nanoparticle delivery to the lungs is an emerging area of interest. This article reviews research performed over the last decades on the application of nanoparticles administered via different routes of administration for treatment or diagnostic purposes. Nanotoxicological aspects of pulmonary delivery are also discussed.