凝集素修饰的纳米粒给药系统研究进展

通过检索和总结国内外相关文献,阐述了近年来凝集素修饰的纳米粒给药系统的研究进展,包括凝集素对黏膜及癌细胞特异作用机制,对纳米粒修饰的研究现状和应用,及对纳米粒的键合方法,展望了凝集素修饰的纳米粒在黏膜给药系统中的应用前景,旨在为靶向给药研究提供新思路。     

凝集素介导的生物黏附微粒制剂研发趋势

阐述了第二代生物黏附微粒制剂的概念及黏附机制，介绍了影响凝集素黏附性能的因素和凝集素的类型，并对该系统的应用及发展趋势进行了概述。生物黏附释药系统作为一种新颖的药物释放系统，以特有的靶向性，缓、控释等优势成为很有前途的给药系统。其中凝集素介导的第二代生物黏附给药系统具有特异靶向性，微粒制剂又在提高药物稳定性、控制药物释放等方面具有优势。     

胃肠道特异性生物黏附给药系统的研究进展

胃肠道特异性生物黏附给药系统是一类兼具靶向特异性和生物黏附功能的新型口服给药制剂,通过以配体修饰载药微粒,实现特异性生物黏附功能.介绍了4种不同配体材料(凝集素、维生素B_(12)和B_1、甘露糖和鞭毛蛋白)介导的 胃肠道特异性生物黏附给药制剂及其作用机制的研究进展.     

疫苗微粒给药系统的研究进展

微粒作为疫苗载体,在疫苗投递系统中的优势已越来越明显.从疫苗微粒在疫苗的口服给药、皮内注射给药、呼吸道黏膜直接接种和其他接种途径等四个方面对微粒给药系统在疫苗投递中的应用现状进行了总结与评价:同时对疫苗微粒给药系统常用高分子化合物进行综述;从单剂量疫苗、新型疫苗、老疫苗新用等方面对微粒给药系统在疫苗投递中的应用前景进行了综述与总结.     

制剂新技术和新型给药系统在蛋白多肽药物研究中的应用

蛋白多肽药物已经成为国内外药学研究和开发的热点,文中介绍几种新制剂技术和新型给药系统在多肽蛋白药物中的应用,分别阐述了聚乙二醇(PEG)修饰技术、聚乙烯吡咯烷酮(PVP)修饰技术、超临界流体技术和脂质体、微粒和纳米粒、脉冲给药系统、微组装给药系统、微乳、聚合物胶束等的应用和研究新成果.上述新技术和新给药系统研究在多肽蛋白药物制备中取得较大进展,明显改善了蛋白多肽的稳定性和体内药动学性质,在新蛋白多肽药物研究中有广阔的应用前景.     

新型给药系统和新技术在光动力疗法中的应用

目的 阐述新型给药系统和制剂新技术在改善光动力疗法（photodynamic therapy,PDT）中的应用研究进展。方法 根据文献,对脂质体、纳米粒、聚合物胶束、微粒表面修饰、微针阵列技术、电学技术、自发光技术、上转换技术等新型给药系统和制剂新技术在PDT中的研究新进展进行阐述。结果 新型给药系统和制剂新技术在较好改善多数光敏剂生理条件下呈疏水性、易聚集及对病变组织选择性不高方面具有独特优势,值得进一步研究。结论 新型给药系统和制剂新技术的开发,有希望将光敏剂传递到人体较深部位并浓集于靶组织,具有广阔的应用前景。     

两亲性环糊精衍生物在毫微粒给药系统中的应用

目的 综述两亲性环糊精衍生物在毫微粒给药系统中的应用研究。方法 对相关文献进行分析、归纳和总结，结果与结论 两亲性环糊精适合作为难溶性药物的载体，可应用于毫微粒给药系统，应用前景广阔。     

现代分析技术在微粒给药系统质量评价中的应用

简介了微粒给药系统的分类、特点及质量控制的主要指标,概述了光学显微观测技术、理化分析检测技术等现代分析技术的特点,并对这些分析技术在微粒给药系统质量评价中的应用进行了综述。     

环糊精在药物制剂方面的新应用

环糊精及其衍生物在改善药物理化性质、改进处方、提高药效等方面具有重要价值，尤其在靶向及微粒给药系统等尖端制剂技术方面的应用越来越广泛。对环糊精及其衍生物在速释和缓释制剂、控释给药、定位给药、微粒给药系统、药物微粉化等方面的发展现状进行了综述，以促进国内在这方面的研究。     

疫苗微粒鼻腔给药系统的研究进展

疫苗微粒鼻腔给药作为一种新型非侵入性疫苗给药系统,具有能延长免疫时间、增强免疫效果、提高病人顺应性等优点。综述疫苗鼻腔免疫诱导机制、常用的微粒系统、免疫效果影响因素及其评价方法及目前该给药系统存在的问题,旨在为研究开发疫苗微粒鼻腔给药系统提供新的思路和方法。     

Floating microspheres: to prolong the gastric retention time in stomach

A gastroretentive drug delivery system with prolong retention time in the stomach have great practical importance for drugs with an absorption window in the upper small intestine. Floating drug delivery system are expected to remain buoyant in the gastric content for prolong duration of time thus enhance the bioavailability of drugs. There are several gastroretentive drug delivery systems, which are floating microspheres, granules, tablets, powder, pills, laminated films and capsules. Floating microspheres are gaining special attention because of their wide applicability in the targeting of drug to stomach. Floating microspheres have several advantages, that they remain buoyant in the stomach and distributed uniformly to avoid the vagaries of gastric emptying and release the drug for prolong period of time.     

A novel pH-dependent gradient-release delivery system for nitrendipine II. Investigations of the factors affecting the release behaviors of the system

Nitrendipine, a dihydropyridine calcium antagonist, was used as a poorly water-soluble model drug. To improve its dissolution rate and extend the therapeutic period in vivo as well, a novel pH-dependent gradient-release drug delivery system for nitrendipine having a solid dispersed matrix structure was developed. Four factors, i.e. the amount of excipients, the pH of the dissolution medium, the rotating speed of the paddle of the dissolution apparatus and the particle size of the microspheres, all of which affect the drug-release behavior of the pH-dependent microspheres of the system were investigated in detail. The release profiles of the pH-dependent drug delivery system under simulated gastrointestinal tract pH conditions were also investigated. The results showed that the release rate of drug from the microspheres increased on increasing the amount of respective pH-dependent polymers formulated. Due to the fact that the active drug was incorporated in pH-dependent polymers and was present in a solid dispersion state in the microspheres, the release rate of the drug from the microspheres depended on the dissolution rate of the polymers, which was mainly influenced by the pH of dissolution medium, whereas the rotating speed of the paddle and the particle size of the microspheres had only a relatively minor effect. The release behavior of the system under simulated gastrointestinal tract conditions exhibited obvious gradient-release characteristics, showing that the release rate of the active drug could be controlled efficiently before the microspheres reached the appropriate region of the gut for absorption. These findings suggest that the pH-dependent drug delivery system could be fabricated by using present microspheres.     

口服结肠定位甲硝唑微球的部分因子设计与体外释放

口服结肠定位给药系统 (ｏｒａｌｃｏｌｏｎ ｓｐｅｃｉｆｉｃｄｒｕｇｄｅｌｉｖｅｒｙｓｙｓｔｅｍ ,ＯＣＤＤＳ)有利于治疗多种结肠疾病 ,如结肠炎、结肠癌、结肠性寄生虫病。ＯＣＤＤＳ可避免因大剂量用药而引起的全身副作用[1] 。甲硝唑用于厌氧菌引起的结肠炎有效 ,但其口服吸收良好(>80 % ) ,在结肠部位难于达到有效治疗浓度[2 ] 。目前临床上治疗结肠炎的主要给药途径是将甲硝唑长期灌肠 ,病人顺应性差。本文拟设计甲硝唑ＯＣＤＤＳ微球 ,有利于给药系统在结肠快速释药 ,有重要的临床意义。国内外未见报道。材料和方法　　材料与仪…     

Preparation of Eudragit E100 microspheres by modified solvent evaporation method

The objective of this investigation was to develop the hollow microspheres as a new dosage form of floating drug delivery system with prolonged stomach retention time. Hollow microspheres containing ranitidine hydrochloride were prepared by solvent evaporation method using Eudragit RLPO dissolved in a mixture of dichloromethane and ethanol. The maximum yield and drug loading amount of hollow microspheres were 88.45% and 80 +/- 4.0%, respectively. The in vitro release profiles showed that the drug release rate decreased with increasing viscosity of Eudragit RLPO, while diameter of hollow microspheres increased with the increase of drug polymer weight ratio. Hollow microspheres could prolong drug release time (approximately 24 h) and float over stimulate gastric fluid for more than 12 h. These results demonstrated that ranitidine HCl hollow microspheres were capable of sustained delivery of the drug for longer period with increased bioavailability.     

Application of a drug delivery system to a steroidal ophthalmic preparation with lipid microspheres

The applicability of a drug delivery system to an ophthalmic preparation was examined using lipid microspheres containing hydrocortisone 17-butyrate 21-propionate (HBP). A 3H-labelled HBP ophthalmic suspension and 3H-labelled HBP lipid microspheres were applied to rabbit eyes, which were then enucleated at fixed intervals to determine the level of 3H-labelled HBP in ocular tissues. The lipid microspheres were shown to deliver the drug to the anterior ocular tissues more effectively than the ophthalmic suspension. It is suggested that a lipid microsphere ophthalmic preparation of various lipophilic drugs including steroids may be useful as a drug delivery system for ophthalmic therapy.     

壳聚糖微球给药系统

主要介绍壳聚糖微球的制备方法，影响其载药的主要因素，及其在缓控释、靶向给药、黏膜给药、生物大分子给药等方面的应用。近年来壳聚糖微球作为新型给药系统备受关注。     

A novel method to prepare magnetite chitosan microspheres conjugated with methotrexate (MTX) for the controlled release of MTX as a magnetic targeting drug delivery system

The purpose of the present study is to develop a new method to prepare magnetite chitosan microspheres conjugated with methotrexate (MTX) for the controlled release of MTX as a magnetic targeting drug delivery system. MTX was first conjugated to the chitosan chain via a peptide bond and then a suspension cross-linking technique was used for the production of magnetic chitosan microspheres with glutaraldehyde as the cross-linker. The MTX-loading capacity of the magnetic chitosan microspheres was determined and drug release experiments were also carried out to discuss the MTX release behavior. All the data support that the magnetic chitosan-MTX microspheres prepared in this method would have great potential application in magnetic targeting drug delivery technology.     

微载体药物递送系统在姜黄素中的应用研究进展

目的综述微载体药物递送系统在姜黄素中的应用研究进展,进一步了解姜黄素的研究概况。方法分别介绍姜黄素的纳米粒、微球、微乳、微囊、胶束、脂质体、磷脂复合物、环糊精包合物等递送系统的研究进展。结果微载体药物递送系统被广泛的应用于提高姜黄素的溶解度和稳定性,进而提高药物在体内的生物利用度。结论微载体药物递送系统在姜黄素中的应用研究为姜黄素进一步应用于临床提供研究基础。     

Design and development of nasal mucoadhesive microspheres containing tramadol HCl for CNS targeting

In the present study, tramadol HCl microspheres were designed in order to accomplish rapid delivery of drug to the brain. For this purpose, lower viscosity grade HPMC (E15) was chosen as mucoadhesive polymer and used at different drug/polymer ratios in the microspheres formulations. The spray-dried microspheres were evaluated with respect to the production yield, incorporation efficiency, particle size, mucoadhesive property, in vitro drug release, histopathological study, and radio imaging study in rabbits. DSC and XRD study showed molecular dispersion and conversion of the drug into amorphous form. Size and surface morphology of microspheres was analyzed by SEM and found to be spherical in shape with smooth surface. It was found that the particle size, swelling ability, and incorporation efficiency of microspheres increase with increasing drug-to-polymer ratio. Microspheres show adequate mucoadhesion and do not have any destructive effect on nasal mucosa. In vitro drug release of optimized formulation was found to be 94% after 90?min. The radio imaging study indicated localization of drug in the brain. Hence, tramadol HCl microspheres based on a HPMC E15 may be a promising nasal delivery system for CNS targeting.     

A novel approach to stabilization of protein drugs in poly(lactic-co-glycolic acid) microspheres using agarose hydrogel

A novel approach has been taken to stabilize protein drugs in poly(lactic-co-glycolic acid) (PLGA) microspheres. This approach creates a new protein drug delivery system, which is based on the combination of agarose hydrogel particles and PLGA microspheres. This combination produces a heterogeneously structured polymeric composite. The protein drug molecules are encapsulated in the agarose hydrogel particles and the drug-containing agarose hydrogel particles are further dispersed in the PLGA microspheres. One PLGA microsphere may contain many agarose hydrogel particles to form a PLGA–agarose composite microsphere. The PLGA–agarose composite microspheres have spherical shape and a smooth surface. They possess a normal or Gaussian size distribution and an average diameter of 150 μm. The PLGA–agarose composite microspheres have higher protein loading efficiency than that of the conventional PLGA microspheres. The hydration of the PLGA–agarose composite microsphere matrix is faster than that of the conventional PLGA microspheres. Protein drugs can be slowly released from the PLGA–agarose composite microspheres. The agarose hydrogel particles can stabilize protein drugs in the PLGA matrix, which is the major advantage of this novel protein drug delivery system over the conventional PLGA microspheres.