介孔二氧化硅纳米粒子药物递送系统研究进展

介孔二氧化硅纳米粒子(MSNs)是一种新型的无机纳米粒子,近年来将其作为药物递送系统的研究受到广泛关注。本文对MSNs的制备、安全性、载药行为、在药物递送领域的应用等方面的研究进展加以综述。     

脂质体及纳米粒药物递送系统的研究进展

脂质体和纳米粒药物递送体系具有增加药物溶解度、延长药物在体内的滞留时间、增强药物的靶向性及降低毒性、抗肿瘤多药耐药等优点。由于近年来在其制备工艺、制备材料及表面修饰等方面取得了较大的进展,脂质体和纳米粒药物递送体系在抗肿瘤、克服生物屏障、装载生物药物及疫苗制备等领域的应用取得了成功。     

磁性介孔二氧化硅用于药物传输和光动力治疗

Objective: To prepare temperature-pH responsive and core-shell-structured magnetic fluorescent mesoporous silica nanoparticles for antitumor drug delivery and photodynamic therapy. Methods: First, the core of nonporous silica coated Fe₃O₄ was prepared via solvothermal reaction and reverse micelle method, then mesoporous silica as the middle layer was further coated on the core by modified sol-gel process, and finally the Fe₃O₄@SiO₂(F)@mSiO₂(P)@P(NIPAM-co-AA) nanoparticles were prepared with the polymer shell modified on the middle layer through seed precipitation polymerization. Transmission electron microscopy (TEM) was carried out to characterize the morphology of the nanoparticles. Doxorubicin hydrochloride (DOX) was used as a model drug to investigate the drug loading and releasing behavior. And MTT assay was adopted to evaluate the biocompatibility and cytotoxicity of the nanoparticles. Results: The results of TEM showed that the average diameter of the nanoparticles was 300 nm. The drug loading and releasing results indicated that the nanoparticles exhibited an excellent drug loading content of (206.75±17.59) μg/mg and encapsulation efficiency of (68.91±5.86) wt%, and controlled drug releasing could be obtained by changing the temperature or pH values. MTT assay showed that the cytotoxic effect of DOX-loaded nanoparticles irradiated with a 680 nm LED lamp was significantly higher than that achieved by chemotherapy and photodynamic therapy alone. Conclusion: Fe₃O₄@SiO₂(F)@mSiO₂(P)@P(NIPAM-co-AA) nanoparticles could be used as an antitumor drug carrier to achieve a synergistic effect by combining chemotherapy and photodynamic therapy.     

外排体作为新型给药系统的研究进展

外排体是由多泡体或称为多囊体与细胞膜融合并分泌到胞外的一种膜性小囊泡,具有多种免疫功能,其表面含有大量的与其来源和功能密切相关的蛋白质和脂质成分,具有去除细胞生长过程中的废弃蛋白、信号传导、提呈抗原激活T细胞以及诱发和增强机体免疫反应等功能。近年来,有研究者利用外排体负载药物,将其发展成为一种纳米给药体系,以避免某些外源性纳米载体可能发生的不良反应以及免疫排斥反应。本文综述了对这种新型纳米载体的发现、功能以及作为给药载体的研究进展,以丰富药剂学的载药系统,并为纳米给药系统的研究提供新的思路。     

小干扰RNA的靶向运送体系

靶向运送是小干扰RNA（siRNA）药物进入临床应用最关键的环节。研究人员利用配体、抗体和适配子构建了非常有效的靶向特异性细胞组织的siRNA运送体系。制备运送体系分3步：先使脂质体或多聚物与siRNA自发结合形成微粒，利用聚乙二醇等作为桥接分子包被在微粒外层，最后将配体、抗体或适配子等靶向性分子与桥接分子连接。     

左炔诺孕酮纳米粒缓释给药系统的研究

目的运用优化制备工艺,用可生物降解的材料制备性质稳定,缓释的左炔诺孕酮纳米粒(LNG-PBCA-NP).方法运用正交试验设计方法设计实验选出最优化实验条件,应用乳化聚合法制备LNG-PBCA-NP,观测粒径大小及分布,测量纳米药物的包封率和含药量,并测定体外释药速率.结果纳米粒粒径为72～170nm,分布均匀,包封率(87.6±0.47)%,控释时间延长.结论制备的LNG-PBCA-NP性质稳定,有明显的缓释性.     

眼用新型递药系统释药规律的研究

眼用新型递药系统释药规律主要是研究眼用制剂在体外的释放规律和体内药物的吸收、分布、代谢和排出,保证制剂的质量可控,同时为临床合理用药提供依据,减少不良反应和毒副作用的发生.     

苦参碱类药物新型给药系统的研究进展

苦参碱类药物主要包括苦参碱、氧化苦参碱、槐定碱等一类独特的生物碱[喹里西啶生物碱,也称羽扇生物碱（tetracyclo-quinolizindine alkaloids）]。苦参碱首先在1958年被分离确认,此后几十年里,陆续从苦参中发现氧化苦参碱、槐果碱、氧化槐果碱、槐定碱、槐胺碱等。这些生物碱均具有较好的生物活性,但目前临床上仅有肌注型苦参碱注射液及以氧化苦参碱为主要成分的苦参素注射液应用于慢性肝炎,同时也存在着生物利用度不高、不良反应多等问题。因此,如何减少苦参碱类药物的不良反应,提高其生物利用度并实现其缓控释及靶向作用,已经成为研究热点。本文对苦参碱类药物近几年来的新型给药系统的研究进展进行综述。     

以磺胺嘧啶为载体的氟尿嘧啶导向药物的合成

目的合成以磺胺嘧啶为载体的氟尿嘧啶导向药物。方法将氟尿嘧啶与氯甲酰三氯甲酯(TCF)反应生成氯甲酰氟尿嘧啶,再与磺胺嘧啶磺酰胺基端高分子连接臂聚乙二醇(PEG)的羟基反应,使氟尿嘧啶通过PEG与磺胺嘧啶相连。紫外分光光度法检测载药量,紫外光谱(UV)、红外光谱(IR)及差热分析(DSC)对合成产物进行鉴定。结果合成产物的载药量为3.2%,UV、IR、DSC检测表明氟尿嘧啶成功的接入。结论通过以TCF活化氟尿嘧啶可以使氟尿嘧啶与PEG的末端羟基成功地连接,从而合成氟尿嘧啶导向药物。     

长春新碱新型给药系统的研究进展

长春新碱是治疗急性淋巴细胞白血病、何杰金及非何杰金淋巴瘤等肿瘤疾病的重要抗癌药物，但具有较大的神经系统毒性和局部刺激性，为降低其不良反应和提高药物生物利用度，目前研究了许多新型给药系统。综述了近10年来有关长春新碱新型给药系统的研究进展。     

The bacterial inhibitory ability andin vivo drug release pattern of a new drug delivery system: Ciprofloxacine/tricalcium phosphate delivery capsule

Summary The bacterial inhibitory ability of a new drug delivery system (DDS): Ciprofloxacine/tricalcium phosphate delivery capsule (CTDC), itsin vivo drug release pattern, and the influence of ultrasonic irradiation on its drug release were investigated. It was found that CTDC had a strong and sustained inhibitory ability to some common pathogens of bone and joint infections, such as staphylococcus aureus, escherichia coli and pseudomonas aeruginosa.In vivo drug-release study in animals demonstrated a high concentration of ciprofloxacine in the bone tissue surrounding CTDC which was placed in the greater trochanter of the rabbit and continued to release ciprofloxacine for at least 5 weeks and the blood level of ciprofloxacine was low.In vivo study also showed ultrasonic irradiation could increase the amount of ciprofloxacine released from CTDC, which may be an economical, effecient and safe new method to achieve the control of drug release from DDS. This project was supported by the grant from National Natural Sciences Fundation of China (No. 39300167).     

雷公藤甲素纳米载药系统的研究进展

该文综述了该课题组近3年来关于雷公藤甲素纳米载药系统的研究工作,包括固体脂质纳米粒、微乳和聚合物纳米粒的制备、表征、药理及毒理等.结果表明雷公藤甲素纳米载药系统可维持较好的药效,降低其毒性.     

紫杉醇表面修饰脂质纳米粒的制备和性质

目的:以硬脂酸为载体材料制备紫杉醇的长循环脂质纳米粒.方法:用"乳化蒸发-低温固化"法制备纳米粒;用透射电镜考察了纳米粒的形态; 建立了于脂质纳米粒和血清中测定紫杉醇的HPLC方法;考察了纳米粒于30%(体积分数)乙醇溶液中的药物释放;以市售紫杉醇注射剂和自制的紫杉醇普通纳米粒为对照,测定了长循环纳米粒于小鼠体内的药物动力学参数.结果:紫杉醇长循环脂质纳米粒的体内半衰期为10.1 h,同时普通纳米粒的体内半衰期为2.3 h,注射剂的体内半衰期为1.3 h.结论:长循环脂质纳米粒可以延长紫杉醇的体内半衰期.     

超声触发药物递送系统用于癌症治疗的研究进展

癌症是威胁人类健康的一大杀手,化疗为其常规治疗手段,但是化疗药由于毒副作用大、缺乏靶向性等问题导致疗效不佳.超声触发药物递送系统是一种新型的高效、无创的药物递送技术,其利用药物载体对超声波的响应,实现药物在肿瘤组织特异性释放,在癌症治疗方面具有重大的应用价值.本文就超声触发药物递送系统的作用机理、分类及其在癌症治疗方面...     

立方晶及其在药剂学中的研究进展

立方晶是两亲性脂质和表面活性剂在水中自发形成的立方液晶的纳米分散体系。立方晶属于自稳定体系,是双连续的水相和脂相形成的类似“蜂窝”状的结构,在其中表面活性剂插入脂质双分子层,晶胞在三维方向上以无限循环方式排列,形成极小曲面的紧密结构。立方晶独特的脂水双连续相立方液晶结构,能够同时增溶亲水、亲脂及两亲性分子,具有生物可降解性、高生物黏附性、制备工艺简单等诸多优点使之在药物载体领域展现较大的优势。本文结合近年文献报道,阐述了立方晶的结构、制备、表征和药物载体的研究进展。     

复合功能传递系统的结构、铁转递蛋白的传递联系和药物载体的磁性颗粒

This paper describes a new formulation of magnetic nanoparticles coated by a novel polymer matrixO-Carboxylmethylated Chitosan (O-CMC) as drug/gene carrier. The O-CMC magnetic nanoparticles were derivatized with a peptide sequence from the HIV-tat protein and transferrin to improve the translocational property and cellar uptake of the nanoparticles. To evaluate the O-MNPs-Tat-Tf as drug carriers, Methotrexate (MTX) was incorporated as a model drug and MTX-loaded O-MNPs-Tat-Tf with an average diameter of 75nm were prepared and characterized by TEM, AFM and VSM. The cytotoxicity of MTX-loaded O-MNPs-Tat-Tf was investigated with C6 cells. The results showed that the MTX-loaded O-MNPs-Tat-Tf retained significant antitumor toxicity; additionally, sustained release of MTX from O-CMC nanoparticles was observed in vitro, suggesting that the O-MNPs-Tat-Tf could be a novel magnetic targeting carrier. We also studied the ability of O-MNPs-Tat-Tf crossing BBB in rats by single photon emission computed tomography (SPECT).     

Construction of multi-functional delivery system: transferrin mediated tat and drug-loaded magnetic nanoparticles

This paper describes a new formulation of magnetic nanoparticles coated by a novel polymer matrix-O-Carboxylmethylated Chitosan (O-CMC) as drug/gene carrier. The O-CMC magnetic nanoparticles were derivatized with a pepfide sequence from the HIV-tat protein and transferrin to improve the translocafional property and cellar uptake of the nanoparticles. To evaluate the O-MNPs-Tat-Tf as drug carriers, Methotrexate (MTX) was incorporated as a model drug and MTX-loaded O-MNPs-Tat-Tf with an average diameter of 75nm were prepared and characterized by TEM, AFM and VSM. The cytotoxicity of MTX-loaded O-MNPs-Tat-Tf was investigated with C6 cells. The results showed that the MTX-loaded O-MNPs-Tat-Tf retained significant anfitumor toxicity; additionally, sustained release of MTX from O-CMC nanoparticles was observed in vitro, suggesting that the O-MNPs-Tat-Tf could be a novel magnetic targeting carrier. We also studied the ability of O-MNPs-Tat-Tf crossing BBB in rats by single photon emission computed tomography (SPECT).     

固体脂质纳米粒给药系统新载体的研究进展

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,它综合了传统胶体给药系统如乳剂、脂质体及聚合物纳米粒等的优点,具有靶向、控释、提高药物稳定性、毒性小、可大批量生产等特性,可供多途径给药.本文就近年来固体脂质纳米粒的组成、制备方法、在给药途径中的应用以及发展前景作一综述.     

A new drug delivery system—Ciprofloxacine/tricalcium phosphate delivery capsule (CTDC) and itsIn Vitro drug release pattern

Summary A new drug delivery system (DDS), ciprofloxacine/tricalcium phosphate delivery capsule (CTDC) was developed by loading a broad-spectrum antibiotic ciprofloxacine into the central cylindrical cavity of tricalcium phosphate capsule. The new system showed good biocompatibility and could degrade gradually in our preliminary studies.In vitro study showed that CTDC could mantain high-level and long-term releae of ciprofloxacine and that ultrasonic irradiation within the range of physical therapy could increase the drug release amount from CTDC (P<0. 02), and might become a new technique to achieve the control of drug release from DDS. This project was supported by the National Natural Science Foundation of China (No. 39300167)     

聚合物纳米粒子作为抗肿瘤药物载体的应用

聚合物纳米粒子作为抗肿瘤药物载体具有优良的性能和广阔的应用前景,主要表现在其能增溶疏水性抗癌药物,增加抗癌基因药物与蛋白类药物的稳定性和提高基因的转染率,提高药物针对肿瘤的靶向性。聚合物纳米粒子作为抗癌中药的载体将为中药的发展带来巨大机遇。