微乳和基于微乳的经皮给药制剂的研究进展

近年来,微乳作为一种具有粒径小、渗透性强、溶解度大、易于制备的新型递药载体,在药物制剂的开发过程中得到广泛研究。本文总结了近年来国内外微乳和基于微乳的经皮给药制剂在不同种类药物中应用的相关文献,介绍了微乳的组成、形成机制、优缺点及在各治疗领域的研究实例。微乳具有促进药物透皮吸收、提高稳定性、延长作用时间和降低皮肤刺激性的优势,因此在经皮给药制剂领域具有广阔的应用前景。     

经皮给药系统研究进展及临床应用概述

经皮给药系统因为具有较小副作用、较强安全性、较高局部浓度和易去除、可控释的特点,在临床上应用范围愈加广泛。经皮给药新剂型包括微针、囊泡、水凝胶、微乳、纳米粒等,综合运用新技术和新剂型能够取得控释的目的,同时还能够使药物经皮吸收量得到增加。     

经皮给药系统中新型载体的应用

摘 要经皮给药相比于传统的口服给药和注射给药,有着使用方便、药物局部浓度高、安全性强的特点。本文综述了近几年国内外文献报道的有关经皮给药系统中,可以增加药物经皮转运效率的新型载体（微乳、醇质体、传递体、囊泡、前体脂质体、凝胶等）的组成、特点及应用。这些新型的经皮给药载体所呈现出来的优越性,使其具有良好的研究价值和广阔的发展空间。     

微乳经皮给药系统的研究进展

近年来对微乳在经皮给药系统的研究日益增多,因此本文就微乳的透皮机制、影响因素、应用进展及现阶段存在的问题等作一综述。     

微乳在经皮传递系统中的应用

目的:综述微乳作为载体在经皮传递系统中的最新应用进展。方法:根据国内外发表的文献,对微乳在经皮传递系统中的应用加以分析和讨论。结果:微乳作为药物经皮传递载体可以起到增加药物溶解度、促进药物渗透等作用,提高药物疗效。结论:微乳作为经皮传递载体具有良好的应用前景。     

基于微乳凝胶新载体的丹皮酚经皮给药系统的构建及药代动力学研究

为构建基于微乳凝胶 (microemulsion-based gels, MBGs) 新载体的丹皮酚经皮给药系统, 采用皮肤、血液双位点同步微透析结合LC/MS联用技术测定丹皮酚微乳、微乳凝胶及市售丹皮酚软膏在大鼠皮肤、血液中的药物浓度随时间的变化过程, 并对其药代动力学参数进行比较分析。方法学研究表明, 丹皮酚线性探针体内回收率 (R_{in vivo}) 为 (69.7 ± 4.8) %, 同心圆探针体内回收率为 (51.6 ± 7.2) %。大鼠腹部脱毛, 分别给予丹皮酚微乳 (1% 丹皮酚)、微乳凝胶和市售丹皮酚软膏, 以PBS (pH 7.4) 溶液作为灌流液, 灌流速度为5 μL·mL⁻¹, 每隔20 min收集1次微透析样品, 共收集12 h, 透析液采用LC/MS进行测定。皮肤药动学结果表明丹皮酚微乳、微乳凝胶与市售软膏相比, 显著提高了药物在皮肤组织中的浓度; 血液药动学结果表明微乳凝胶与市售软膏具有相近的生物利用度, 但前者的血药浓度更平稳。本研究所构建的丹皮酚微乳凝胶有望为皮肤湿疹的治疗提供一种新的制剂; 所建立的微透析/LC-MS联用技术能够在体、同步、实时监测大鼠皮肤、血液中的药物浓度, 为经皮给药药代动力学研究提供了新的方法。     

国外上市新型注射剂的研究进展

纳米粒、微球、脂质体、原位凝胶和微乳或亚微乳等给药系统能减少药物在体内外的降解,实现药物的控制释放.基于上述给药系统的新型注射剂已成为药物研发的关注热点.本文综述了近年国外上市的新型注射剂的剂型特点及其临床应用概况,并介绍了几种新型注射装置.     

微乳在经皮给药系统中的应用

微乳经皮给药是目前国内外药学工作者研究的重点,也是目前药物制剂研发热点之一。本文主要从微乳的组成、促渗机制、微乳在经皮给药中的应用3个方面进行了综述。微乳经皮给药具有很好的应用前景。     

蛋白多肽类口服给药微粒载体研究进展

蛋白多肽类药物已经成为国内外药学研究和开发的热点,文中介绍几种给药微粒载体在多肽蛋白类药物口服中的应用,分别阐述了纳米粒、微球、脂质体、微乳等的应用和研究新成果。上述新型给药微粒载体研究在蛋白多肽药物制备中取得较大进展,明显改善了蛋白多肽药物的稳定性和体内药动学性质,在蛋白多肽药物研究中有广阔的应用前景。     

微针新型经皮给药新技术的应用及研究进展

药物通过皮肤表面进入体内,并通过循环发挥其药效就是所谓的经皮给药,但是经皮给药这种给药方式有一个很大的障碍——皮肤。如何克服皮肤的障碍,促进药物的渗透是药剂研究者一直以来备受关注的。通过经皮给药的药物载体有很多,如醇质体、传递体、微乳、非离子囊泡等,这些都是化学促渗透的方法。本文主要对一种新型的物理促渗透方法进行介绍,经过大量文献资料的查阅,对微针这种经皮给药新技术的应用和研究的最新进展进行阐述。     

Organogels in drug delivery

In the last decade, interest in physical organogels has grown rapidly with the discovery and synthesis of a very large number of diverse molecules, which can gel organic solvents at low concentrations. The gelator molecules immobilise large volumes of liquid following their self-assembly into a variety of aggregates such as rods, tubules, fibres and platelets. The many interesting properties of these gels, such as their thermoreversibility, have led to much excitement over their industrial applications. However, only a few organogels are currently being studied as drug/vaccine delivery vehicles as most of the existing organogels are composed of pharmaceutically unacceptable organic liquids and/or unacceptable/untested gelators. In this paper a brief overview of organogels is presented, followed by a more in-depth review of the gels that have been investigated for drug and/or vaccine delivery. These include microemulsion-based gels and lecithin gels (studied for transdermal delivery), sorbitan monostearate organogels and amphiphilogels (studied as vaccine adjuvants and for oral and transdermal drug delivery, respectively), gels composed of alanine derivatives (investigated as in situ forming gels) and Eudragit organogels (studied as a matrix for suppositories). Finally, pluronic lecithin organogels, descendents of lecithin gels but which are not really organogels, are briefly discussed for their interesting history, their root and the wide interest in these systems.     

Organogels in drug delivery

In the last decade, interest in physical organogels has grown rapidly with the discovery and synthesis of a very large number of diverse molecules, which can gel organic solvents at low concentrations. The gelator molecules immobilise large volumes of liquid following their self-assembly into a variety of aggregates such as rods, tubules, fibres and platelets. The many interesting properties of these gels, such as their thermoreversibility, have led to much excitement over their industrial applications. However, only a few organogels are currently being studied as drug/vaccine delivery vehicles as most of the existing organogels are composed of pharmaceutically unacceptable organic liquids and/or unacceptable/untested gelators. In this paper a brief overview of organogels is presented, followed by a more in-depth review of the gels that have been investigated for drug and/or vaccine delivery. These include microemulsion-based gels and lecithin gels (studied for transdermal delivery), sorbitan monostearate organogels and amphiphilogels (studied as vaccine adjuvants and for oral and transdermal drug delivery, respectively), gels composed of alanine derivatives (investigated as in situ forming gels) and Eudragit organogels (studied as a matrix for suppositories). Finally, pluronic lecithin organogels, descendents of lecithin gels but which are not really organogels, are briefly discussed for their interesting history, their root and the wide interest in these systems.     

凝胶材料及其在经皮给药系统中的应用与研究进展

凝胶材料具有触感舒适、透气性好、高粘弹性等其他材料所无法比拟的优势,在经皮给药系统中备受青睐,被广泛应用于现代经皮给药制剂如贴剂、贴膏剂、凝胶剂、膜剂当中。随着医药材料的创新发展,许多具有优异功能的新型凝胶材料涌现,使经皮给药制剂的应用范围得到扩大,性能得以优化。通过综述凝胶材料的分类、性能及其在经皮给药系统中的应用,总结最新研究进展,为凝胶材料在经皮给药系统的创新应用提供借鉴和参考。     

Microemulsion-based gel of fluorouracil for transdermal delivery

This study is to prepare the microemulsion-based gel based on the W/O microemulsion and fluorouracil (5-Fu) as a model drug to study the transdermal characterization and observe its skin irritation of the microemulsion-based gel in vitro. IPM acted as oil phase, AOT as surfactant, Tween 85 as cosurfactant, water was added dropwise to the oil phase to prepare W/O microemulsion at room temperature using magnetic stirring, then 5-Fu powder was added. The gelatin was used as substrate to prepare 5-Fu microemulsion-based gel. The permeation flux of 5-Fu from 5-Fu microemulsion-based gel across excised mice skin was determined in vitro using Franz diffusion cell to study the influence of the amount of gelatin and the drug loading capacity. Refer to 5-Fu cream, the irritation of microemulsion and microemulsion-based gel on the rat skin was studied. Based on the water/AOT/Tween 85/IPM microemulsion, only the gelatin can form the microemulsion-based gel. At 25 degrees C, 32 degrees C and 40 degrees C, the amount of gelatin required for the formation of microemulsion-based gel were 7%, 14% and more than 17%, respectively. The 12 h transdermal cumulated permeation amount of 5-Fu from microemulsion-based gel containing 14% gelatin and 0.5% drug loading were (876.5 +/- 29.1) microg x cm(-2), 12.3 folds and 4.5 folds more than 0.5% 5-Fu aqueous solution and 2.5% (w/w) 5-Fu cream, respectively. Microemulsion-based gel exhibited some irritation, but could be subsided after drug withdrawal. Microemulsion-based gel may be a promising vehicle for transdermal delivery of 5-Fu and other hydrophilic drug.     

微针透皮给药系统应用研究进展

微针透皮给药系统是近年来透皮给药系统研究的热点。微针透皮给药系统具有注射给药和透皮给药的双重优势,具有快速、方便、无痛等众多优点,研究表明可以显著提高药物透皮速率和吸收量,特别是在蛋白质、多肽、DNA和RNA等大分子物质的透皮制剂研究领域表现出良好的效果和应用前景,本文对微针透皮给药系统应用研究的最新进展进行了综述。随着微针加工技术、载药技术和应用研究的不断深入,微针透皮技术在临床领域将会有更广泛的应用。     

经皮给药促透方法的研究进展

目的由于皮肤的屏障作用,经皮给药系统的应用受到限制,促透方法的研究成为焦点。许多方法可用于促进药物的经皮吸收。本文主要从化学法、物理法、药剂学法、生物法及促透方法的综合应用等方面阐述了近年来国内外在经皮给药促透方法的研究上所取得的进展。     

微针在儿童经皮递药中的研究进展

与传统的口服和肠外给药途径相比,经皮给药系统作为一种非侵入性替代方法非常有吸引力。特别对于儿童患者,它有助于克服该群体特有的问题,如吞咽困难、口服制剂的适口性以及与针头相关的恐惧和疼痛。然而,儿童的皮肤屏障功能有效地限制了药物的经皮吸收。微针可突破皮肤最外层的角质层,增加经皮给药的药量。过去几十年,以微针为基础药物输送系统的研究取得了显著进展。与微针相关的研究论文呈指数级激增。本文概括了微针的分类及特点,讨论了微针在儿童经皮递药中的研究进展,最后对微针介导的儿童经皮递药的未来前景进行了简要展望。