多糖微粒制剂的研究进展

目的 介绍多糖微粒制剂的研究进展。方法 综述了近年来国内外相关报道,介绍和评价多糖微粒制剂的制备方法、性能和药效等,指出多糖纳米制剂的研究前景。结果 多糖微粒制剂有助于改善多糖药物稳定性差、生物利用度不高以及对某些细胞穿透能力不强等缺点,并使多糖药物获得抗肿瘤增效、靶向等作用。结论 多糖新型微粒制剂为癌症治疗提供了新的研究途径,具有很大的发展前景。     

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.     

去甲斑蝥素新型制剂研究进展

目的 综述去甲斑蝥素新型制剂研究进展.方法 通过查阅近年来有关去甲斑蝥素新型制剂的中外文献,对其研究进展进行归纳总结与分析.结果 经过对微球、纳米粒、脂质体和微乳等载药系统包载去甲斑蝥素的情况进行分析,结果表明去甲斑蝥素新型制剂是极具开发潜力的新型制剂.结论 去甲斑蝥素是一种优良的抗肿瘤药物,但传统的注射剂和片剂在临床...     

国内靶向制剂的研究现状

目的：研究靶向制剂在中国的发展现状。方法：通过大量国内文献检索，从靶向制剂（主动靶向，被动靶向，物理化学靶向）三方面进行探讨。结果与结论：发现国内靶向制剂潜力巨大，具有较广阔的开发及应用前景。     

肝靶向微粒给药系统的研究进展

目的对近年来微粒给药系统在肝靶向治疗的研究进展做一综述。方法根据国内外文献资料进行整理归纳。结果纳米粒、微球、脂质体及微乳等微粒系统具有被动靶向于肝的趋势,利用肝细胞表面某些受体则可特异性靶向于肝达到主动靶向作用。结论微粒给药系统在肝靶向治疗领域具有重要意义。     

肝靶向微粒给药系统的研究进展

目的对近年来微粒给药系统在肝靶向治疗的研究进展做一综述。方法根据国内外文献资料进行整理归纳。结果纳米粒、微球、脂质体及微乳等微粒系统具有被动靶向于肝的趋势,利用肝细胞表面某些受体则可特异性靶向于肝达到主动靶向作用。结论微粒给药系统在肝靶向治疗领域具有重要意义。     

核苷类抗病毒靶向制剂的研究进展

目的综述核苷类靶向制剂研究进展。方法在查阅国内外文献得基础上,从被动靶向制剂方面进行探讨。结果与结论核苷类靶向制剂市场潜力巨大,有很好的应用和开发价值。     

新型抗结核药物制剂研究进展

结核病(tuberculosis,TB)是一种由结核分枝杆菌(Mycobacterium tuberculosis,MTB)引起的慢性传染病,它积聚在各个器官,特别是肺部。目前临床上常用的抗结核药物主要以胶囊剂、片剂或注射剂为主,但这些常规剂型往往难以在结核病核心病灶区域有效分布,药物通过全身循环向其他组织和器官非特异性分布,导致局部药物浓度低,易产生不良反应,进而影响抗结核药的治疗效果。微球、脂质体、纳米粒等新剂型能够选择性地将药物浓集于结核病变部位,从而达到降低药物不良反应,提高患者依从性的目的。因此,本文旨在对抗结核药物新剂型的相关研究进行综述。     

胶粒系统用于眼用制剂的研究进展

目的更好地使治疗药物进入眼内发挥疗效。方法广泛查阅近几年的文献资料,进行分析、综合和归纳,分别对眼用脂质体、微球、纳米粒、微乳等胶粒分散系统的国内外研究概况进行阐述。结果与结论眼用微粒给药系统可改善药物在角膜或结膜的滞留时间,提高药物在眼部组织的生物利用度,获得比较理想的局部治疗效果。     

蛋白多肽类药物注射缓控释制剂的研究进展

研制开发蛋白多肽类药物注射缓控释制剂新技术，使此类药物更好地用于疾病的预防和治疗，已成为现代药剂学的热点。本文主要介绍国内外注射用蛋白多肽类药物在微球、纳米粒、脂质体、原位水凝胶等制剂新技术的发展概况。     

双水相萃取技术及其在药物提取分离中的应用近况

目的介绍近年来双水相萃取技术在药物提取分离中的应用情况。方法对近几年国内外文献资料进行总结和归纳,介绍了双水相萃取技术的基本原理与特点,综述了近年来该技术在蛋白质、酶、氨基酸类药物,中药体系及抗生素类药物的提取分离等方面的应用进展。结果双水相萃取技术广泛应用于药物提取分离中,取得了较大进展。结论该技术用于药物提取分离中,有着广阔的应用前景,将推动我国医药工业的发展。     

Mucoadhesive Hybrid Polymer/Liposome Pastes Based on Modified Polysaccharides

Mucoadhesive hybrid polymer/liposome paste is a new drug delivery system presenting controllable and tailorable delivery mechanism. By using mucoadhesive material, the delivery can be more specific and local. Here, we present a study investigating the effect of polymer type, concentration, functional end group, and cross-linking on the release profile of nanoliposomes from polymer pastes. Polymer pastes can be expected to combine the mucoadhesion mechanisms of dry and wet dosage forms but have not been studied extensively. To better understand the mucoadhesion of pastes, we investigated a series of pastes based on the same polymer and used different chemical modifications that can produce interactions at different levels. Native and thiolated polymers presented enhanced mucoadhesion in a wet environment in comparison to acrylated polymers which dissolved rapidly because of the enhanced solubility of PEG chains in water. Paste cross-linking resulted in a sustained release profile compared to non–cross-linked pastes. Pectin-SH pastes, especially 3% (w/v), showed a linear liposomal release profile which is ascribed to the combination of ionic cross-linking and disulfide bridging. By configuring the polymer type or concentration, we can control the release mechanisms and achieve distinct inherent properties which can be applied for diverse medical applications.     

靶向分化群47-信号调节蛋白α的抗肿瘤药物递送系统研究进展

巨噬细胞是肿瘤微环境的重要组成部分,肿瘤细胞通过表达分化群47（CD47）与巨噬细胞受体信号调节蛋白α（SIRPα）相互作用而避免被吞噬。目前通过阻断CD47-SIRPα的相互作用进而恢复巨噬细胞吞噬功能的研究已经受到了广泛关注,包括抗CD47抗体在内的多种药物已经开展了临床试验研究。然而常见的血液毒性限制了这类药物的临床应用,除了筛选肿瘤特异性结合的药物外,通过药物递送系统包载CD47抑制剂用于肿瘤的治疗是一种有效策略。通过以CD47-SIRPα的结构和信号通路为基础,详细综述了靶向CD47-SIRPα的递送系统,包括白蛋白、脂质等不同载体材料构建的纳米递送系统,凝胶递送系统和抗体偶联药物等,以期为临床药物开发提供借鉴。     

Current advances in development of new docetaxel formulations

Introduction: Docetaxel (DTX) is one of the most important chemotherapeutic agents and has been widely used for treatment of various types of cancers. However, the clinical chemotherapy of DTX gives many undesirable side effects due to the usage of organic solvent in the injection and its low selectivity for tumor cells. With the evolution of pharmaceutical technologies, great efforts have been paid to develop new DTX formulations to overcome these problems.

Areas covered: This review provided an overview of the preparation and activities of new DTX formulations, which were classified by administration methods, including injection, oral, transdermal and rectal administration. Besides, up to date information of the clinical status of new DTX formulations was summarized. We also discussed the challenges and perspectives of the future development of DTX formulations.

Expert opinion: There have been numerous studies on new DTX-based formulations in recent years, and many of them exhibited significantly enhanced anti-tumor and targeting activity compared with DTX in preclinical studies. However, only a few entered clinical trials, and none has been approved into market. The clinical translation of experimental drug faces many hurdles, including the limited knowledge of nanomedicine and oncology, safety issues, controllable and reproducible production.     

胶束传递系统逆转肿瘤多药耐药的研究进展

肿瘤多药耐药是目前肿瘤治疗的一大障碍。研究采用药物传递系统如胶束、脂质体、纳米粒等, 以逆转多药耐药, 显示其安全可靠, 并具有良好的应用前景。本文重点综述了药物传递系统中的聚合物胶束逆转多药耐药的研究结果及其可能的作用机制。随着研究的深入, 药物传递系统在逆转肿瘤多药耐药的研究领域将发挥更加重要的作用。     

脂质体药物递送系统的研究进展

注射剂作为一种特殊的药物剂型,具有起效快、定位准等优点,因而被广泛应用于临床。随着临床应用需求的增多,在传统注射剂的基础上,许多新型注射剂应运而生。脂质体、混悬剂、纳米粒、微球和包合物等注射给药系统的出现,不仅减少了药物在体内外的降解,还具有缓释、控释的优点,受到研究人员密切关注。重点介绍了几种新型注射剂的特点,并对国内外已上市和在研的新型注射剂进行简要介绍,旨在为其深度开发提供参考。

     

磁性微球和磁性纳米粒的研究进展

介绍了磁靶向给药系统的主要类型、分类及组成,重点综述了磁靶向给药系统中的磁性微球和磁性纳米粒的特性、制备方法、体内外磁控试验的研究进展.     

Use of nanoscale delivery systems to maintain synergistic drug ratios in vivo

Importance of the field: Drug combinations have been the standard of care in the treatment of cancer for > 50 years. Typically, combination chemotherapy uses agents with non-overlapping toxicities which are escalated to their maximum tolerated dose. However, emerging evidence indicates that this approach may not be providing optimal efficacy depending on the drug ratios to which the tumor is exposed. Combined drugs can be synergistic whereas other ratios of the same agents may be antagonistic or additive.

Areas covered in this review: In this review, we examine the importance of drug ratios in cancer therapy. We describe how manipulation of the lipid membrane and internal buffer composition maintains synergistic ratios of irinotecan and floxuridine (CPX-1), daunorubicin and cytarabine (CPX-351) or cisplatin and irinotecan (CPX-571). For polymer-based nanoparticles, prodrug hydrophobicity was exploited to coordinate the release of gemcitabine and the more hydrophobic paclitaxel. We present preclinical data for liposomal drug combinations which demonstrate that the most efficacious formulation is not always the highest dose of both agents.

What the reader will gain: An insight into the use of liposomes and polymer-based nanoparticles to deliver synergistic drug combinations to the tumor site and avoid antagonistic drug–drug interactions.

Take home message: The ability to control and maintain drug ratios in vivo through the use of nanoscale delivery vehicles results in a significant improvement in therapeutic activity.     

酵母多糖脂质体的免疫增强作用

本文比较了酵母多糖脂质体、酵母多糖及脂质体对小鼠免疫功能的影响。结果表明,前两者对小鼠免疫功能均有促进作用,但经脂质体包封后的酵母多糖(多糖脂质体)表现出更强的促进能力,其差异有显著性(P＜0.01)。单纯脂质体的免疫增强作用不明显。     

生物素在肿瘤靶向递药中的研究进展

运用靶向递药系统给药是目前治疗癌症的有效方法,靶向配体的选择是靶向递药的关键。生物素受体在多数肿瘤细胞表面过表达,但在正常细胞中低表达或不表达,因此,生物素可作为配体与药物载体相连,用于肿瘤靶向递药。简述生物素及生物素受体,综述生物素修饰的脂质体、胶束、纳米粒等载药系统在肿瘤靶向诊断和治疗中的研究进展,以期为相关研究开发与临床应用提供参考。