离子导入经皮给药系统

综述了离子导入技术的基本组成、促渗机制、影响因素及应用前景。离子导入技术可有效提高药物的经皮渗透性，该技术扩大了经皮给药系统的研究范围，其对多肽和蛋白质等大分子药物的透皮促渗作用日益受到关注。     

蛋白质和多肽类药物口服给药研究进展

蛋白质和多肽类药物具有良好的选择性和生物活性,已成为治疗众多疾病的首选药物。由于胃肠道内酶的降解作用以及肠道粘膜的低通透性,蛋白质和多肽类药物口服生物利用度极低,其常规给药一直以注射为主。为了使蛋白质和多肽类药物能够广泛应用于临床,研究人员对蛋白质和多肽类药物口服给药系统做了大量研究。目前用于提高蛋白质和多肽类药物口服生物利用度的方法主要有微粒给药系统、内源性细胞转运系统、应用酶抑制剂和黏附给药系统等。文章就这些方法在蛋白质和多肽类药物口服给药中的应用进行了综述。     

蛋白质及多肽类药物给药系统的研究进展

综述了近年来微球、长效脂质体及鼻腔、肺部、口服等给药方式的特点及应用前景。     

促进多肽和蛋白质类药物透皮给药技术的研究进展

综述了近年来以物理方法促进多肽和蛋白质药物透皮给药技术研究的进展，包括目前广泛研究的离子导入、电致孔导入和超声导入技术。     

促进多肽和蛋白质类药物透皮给药技术的研究进展

综述了近年来以物理方法促进多肽和蛋白质药物透皮给药技术研究的进展,包括目前广泛研究的离子导入、电致孔导入和超声导入技术.     

促进多肽和蛋白质类药物透皮给药技术的研究进展

综述了近年来以物理方法促进多肽和蛋白质药物透皮给药技术研究的进展,包括目前广泛研究的离子导入、电致孔导入和超声导入技术。     

蛋白质和多肽类药物的口服给药：尚未实现的希望

实现蛋白质和多肽类药物的口服给药是药物递送长期追求的目标 ,具有很好的发展前景 ,同时也存在许多问题。渗透性、稳定性及在胃肠内的转运时间等是影响该类药物口服吸收的因素 ,但分子大小一般认为是最主要的障碍。本文主要介绍处方组成、包囊技术、大分子复合物和化学修饰四种改善蛋白质和多肽类药物在胃肠道吸收状况的基本方法。对于吸收促进剂和酶抑制剂已进行了多年的研究。此技术着重于通过改变多肽的渗透性和可消化性来改善其在胃肠道的吸收状况 ,这些组分会改变粘膜表面的完整性 ,甚至会产生全身和局部的副作用。最近开发出一种新的…     

微乳在多肽、蛋白质类药物口服给药中的应用

随着生物技术的飞速发展,多肽、蛋白质类等生物技术药用活性大分子物质在临床上的应用越来越广泛。由于本身结构特点原因,此类药物通常生物半衰期短,生物利用度较低,不易通过生物屏障,且稳定性差,易被胃肠道中的蛋白质水解酶降解,其给药途径通常为静脉或肌内注射,基本剂型是冻干粉注射剂[1],但频繁的注射给药,患者依从性较差,导致疗效下降甚至治疗中断。寻求多肽、蛋白质类药物     

多肽及蛋白质类药物的研究进展

介绍了目前多肽多蛋白质类药物口服液制的研究概况。     

Emerging strategies for the transdermal delivery of peptide and protein drugs

Transdermal delivery has been at the forefront of research addressing the development of non-invasive methods for the systemic administration of peptide and protein therapeutics generated by the biotechnology revolution. Numerous approaches have been suggested for overcoming the skin’s formidable barrier function; whereas certain strategies simply act on the drug formulation or transiently increase the skin permeability, others are designed to bypass or even remove the outermost skin layer. This article reviews the technologies currently under investigation, ranging from those in their early-stage of development, such as laser-assisted delivery to others, where feasibility has already been demonstrated, such as microneedle systems, and finally more mature techniques that have already led to commercialisation (e.g., velocity-based technologies). The principles, mechanisms involved, potential applications, limitations and safety considerations are discussed for each approach, and the most advanced devices in each field are described.     

多肽透皮给药研究进展

针对近年来多种多肽类药物的透皮给药系统进行综述。通过查阅国内外多种相关期刊文献。将多肽类药物透皮给药方法分为化学促渗剂、多种物理促渗技术,以及透皮肽、微针技术并对其进行论述。反向离子导入技术应用前景广阔,微针给药系统研究逐步深入,出现了胰岛素智能化微针给药系统,透皮肽的研究发展迅速,相信未来多种蛋白质及多肽的透皮给药方式将应用于临床,极大地促进医疗事业的发展。     

In-vitro and in-vivo transdermal iontophoretic delivery of tramadol, a centrally acting analgesic

Objectives The feasibility of transdermal delivery of tramadol, a centrally acting analgesic, by anodal iontophoresis using Ag/AgCl electrodes was investigated in vitro and in vivo. Methods To examine the effect of species variation and current strength on skin permeability of tramadol, in‐vitro skin permeation studies were performed using porcine ear skin, guinea‐pig abdominal skin and hairless mouse abdominal skin as the membrane. In an in‐vivo pharmacokinetic study, an iontophoretic patch system was applied to the abdominal skin of conscious guinea pigs with a constant current supply (250 µA/cm²) for 6 h. An intravenous injection group to determine the pharmacokinetic parameters for estimation of the transdermal absorption rate in guinea pigs was also included. Key findings The in‐vitro steady‐state skin permeation flux of tramadol current‐dependently increased without significant differences among the three different skin types. In the in‐vivo pharmacokinetic study, plasma concentrations of tramadol steadily increased and reached steady state (336 ng/ml) 3 h after initiation of current supply, and the in‐vivo steady‐state transdermal absorption rate was 499 µg/cm² per h as calculated by a constrained numeric deconvolution method. Conclusions The present study reveals that anodal iontophoresis provides current‐controlled transdermal delivery of tramadol without significant interspecies differences, and enables the delivery of therapeutic amounts of tramadol.     

提高蛋白质及多肽类药物肺部给药生物利用度的方法及其作用机制

目的 介绍国内外提高蛋白质与多肽类药物肺部给药系统生物利用度的方法及其作用机制的最新研究进展。方法 对国内外最新发表的相关文献进行分析、整理和综合。结果 吸收促进剂、酶抑制剂及脂质体均可使蛋白质及多肽类药物的肺部吸收明显提高,甚至达到治疗所需的生物利用度。结论 蛋白质及多肽类药物的肺部给药系统具有广阔的应用前景。     

Non-invasive iontophoretic delivery of peptides and proteins across the skin

Introduction: Peptides and proteins are playing an increasingly important role in modern therapy. Their potency and specificity make them excellent therapeutic agents; however, their physicochemical properties and stability requirements almost invariably necessitate their administration by subcutaneous, intramuscular or intravenous injection. Controlled non-invasive administration using more patient-friendly advanced delivery technologies may combine the precision afforded by parenteral administration with improved compliance and the potential for individualized therapy.

Areas covered: Transdermal iontophoresis enables hydrophilic charged molecules to be administered through the skin in an effective, non-invasive, patient-friendly manner. This review presents the basic concepts and an analysis of the effect of iontophoretic parameters and molecular properties on electrotransport rates across the skin along with a summary of experimental studies with peptides and proteins. The last section covers other techniques used in conjunction with iontophoresis.

Expert opinion: It has long been known that iontophoresis can administer therapeutic amounts of biologically active peptides into the body. More recent studies have shown that it is also capable of delivering structurally intact, functional proteins non-invasively into and across intact human skin. The next step is to develop cost-effective and easy-to-use iontophoretic patch systems that ensure biomolecule stability, optimize delivery efficiency and address unmet therapeutic needs.     

Novel reverse electrodialysis-driven iontophoretic system for topical and transdermal delivery of poorly permeable therapeutic agents

Topical and transdermal drug delivery has great potential in non-invasive and non-oral administration of poorly bioavailable therapeutic agents. However, due to the barrier function of the stratum corneum, the drugs that can be clinically feasible candidates for topical and transdermal delivery have been limited to small-sized lipophilic molecules. Previously, we fabricated a novel iontophoretic system using reverse electrodialysis (RED) technology (RED system). However, no study has demonstrated its utility in topical and/or transdermal delivery of poorly permeable therapeutic agents. In this study, we report the topical delivery of fluorescein isothiocyanate (FITC)–hyaluronic acid (FITC–HA) and vitamin C and the transdermal delivery of lopinavir using our newly developed RED system in the in vitro hairless mouse skin and in vivo Sprague–Dawley rat models. The RED system significantly enhanced the efficiency of topical HA and vitamin C and transdermal lopinavir delivery. Moreover, the efficiency and safety of transdermal delivery using the RED system were comparable with those of a commercial ketoprofen patch formulation. Thus, the RED system can be a potential topical and transdermal delivery system for various poorly bioavailable pharmaceuticals including HA, vitamin C, and lopinavir.     

多肽类药物鼻腔给药研究进展

随着生物制药技术的发展,越来越多的多肽类药物在医药领域得到应用.但由于这类药物稳定性不佳、口服易被酶解等问题,临床多采用注射途径给药.鼻腔给药不仅能够克服口服给药的首过效应、注射给药的顺应性差等问题,而且具有脑靶向、低剂量高活性的优点.本文主要就多肽类药物的鼻腔给药进行综述,系统地介绍了鼻腔的组织构造,药物本身性质、制...     

细胞促渗肽在透皮给药中的应用

细胞促渗肽（CPP）最早于细胞研究中发现,此后被引入透皮制剂领域,相关透皮机制尚未阐明。CPP在透皮制剂领域中应用广泛,对小分子药物、多肽、蛋白质、核酸和胶粒载体均有皮肤促渗作用。本文综述CPP在透皮领域中的应用。     

Transdermal iontophoretic drug delivery: advances and challenges

The stratum corneum continues to pose considerable impediment to transdermal drug delivery. One of the effective ways of circumventing this challenge is through the use of iontophoresis. Iontophoresis uses low-level current to drive charged compounds across the skin. This review discusses progress made in the field of iontophoretic transport of small and large molecules. The major obstacles are also touched upon and advances made in the last few decades described. A number of iontophoretic systems approved for clinical use by regulatory authorities is also discussed.