微乳凝胶经皮给药制剂的研究与应用进展

目的 介绍微乳凝胶经皮给药制剂的研究与应用进展。方法 根据近年来国内外相关文献,对微乳凝胶作为经皮给药载体的处方筛选、制备、体外释药性能、质量检查、研究应用进展等方面进行介绍。结果 微乳凝胶具有显著增强药物的经皮渗透能力、降低药物刺激性和延缓药物释放等作用,且更便于给药。结论 微乳凝胶有望成为一种具有重要应用价值的经皮给药新剂型。     

微乳制剂的吸收特性研究进展

目的:了解微乳制剂的吸收特性研究进展及方向.方法:对微乳制剂分为经皮给药、注射和口服3种给药方式,查阅近年文献进行评述.结果:根据药物性质采用不同乳化方法制备微乳,主要应用于经皮、注射和口服给药.结论:随着对微乳形成机制及制备工艺的研究不断深入,预测微乳的发展前景和应用范围.     

微乳透皮给药载体的制备及透皮影响因素研究进展

目的:介绍微乳透皮给药载体的制备及透皮吸收的影响因素。方法:根据文献,综述了微乳的形成机制、透皮给药载体的作用、微乳的制备及其载体的透皮吸收影响因素等方面的内容。结果与结论:微乳的形成机制主要有混合膜理论和增溶理论;其透皮给药载体的作用包括促透皮作用和缓释及降低药物刺激性作用;可通过基于相图的自发乳化法、转相乳化法、相转变温度乳化法、机械法制备微乳;药物、水相、油相、表面活性剂和助表面活性剂、化学促渗剂等因素可影响微乳载体的透皮吸收。微乳透皮给药载体在制备时要考虑其透皮吸收的效能,从透皮影响因素等方面综合考察,使其发挥透皮给药的独特优势。     

纳米载体应用于透皮给药系统的研究进展

纳米载体经皮给药系统是近几年经皮给药的研究热点。本文综述了各种纳米载体在经皮给药系统中应用的研究进展,其中囊泡、微乳和固体脂质纳米粒作为经皮给药载体已得到相对深入的研究,而新型纳米载体如胶束、树状大分子和细胞促透多肽等尽管研究较少,但基于其明显的促渗作用,将会为经皮给药系统的研究提供新方向。     

微乳透皮给药系统的研究进展

微乳是一种新型的药物载体,具有提高难溶性药物的溶解度、促进药物透皮吸收等特性,近年来已成为临床应用领域的研究热点。目前,微乳已经作为多种剂型的载体应用于药物制剂的开发。在中药制剂研究中,近年来已有大量文献报道,并取得了一定的研究成果,本文主要从透皮给药途径来介绍微乳在药剂学中的应用。     

微乳透皮给药系统的研究概况

微乳(microemulsion,ME)是一种透明、热力学稳定、黏度低的混合物,一般由油相、表面活性剂、助表面活性剂和水组成。从结构上可分为水包油型(O／W)、油包水型(W／O)及双连续型。因微乳具有良好的透皮及局部皮肤给药特性,国外从上世纪90年代开始开展了一系列微乳透皮给药的基础及应用研究,近年来国内也有相关报道。本文就微乳透皮给药系统的促渗作用及影响因素、制备工艺、体内外评价方法及微乳透皮制剂应用进展作一概述。     

微乳给药系统研究进展

微乳是一种新型给药系统，能提高水难溶性药物的溶解度和生物利用度，延长水溶性药物的释放，并具有较好的靶向性。近年来研究表明，微乳有利于药物的吸收、分布，可改善药动学，在透皮与口服给药、新制剂研发中得到应用。     

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。     

微乳系统在透皮给药中的应用

概述了微乳透皮给药的渗透机制，微乳的各组分及结构对透皮渗透的影响和微乳中加入促渗剂的可行性。     

盐酸罂粟碱 卵磷脂微乳的制备与透皮吸收

［摘要］目的探讨以卵磷脂微乳为载体，制备盐酸罂粟碱 卵磷脂微乳透皮给药系统，促进盐酸罂粟碱的透皮吸收。方法以伪三元相图考察油包水型微乳形成区域;以十四酸异丙酯 卵磷脂 乙醇 水作为微乳的组成部分，正交分析法筛选微乳处方，测定微乳黏度;采用智能透皮仪，大鼠离体皮肤作为透皮模型，与盐酸罂粟碱水溶液及盐酸罂粟碱 卵磷脂混悬液对比，用高效液相色谱（HPLC）法测定微乳中盐酸罂粟碱经皮渗透稳态流量。结果微乳各组分及比例对微乳粒径均有影响；盐酸罂粟碱 卵磷脂微乳的经皮渗透稳态流量大于对照组。结论微乳各组分及比例对微乳体系处方的选择具有重要意义；以微乳为载体可以促进盐酸罂粟碱的经皮渗透。     

Dermal peptide delivery using colloidal carrier systems

The advancement in synthetic and molecular biology techniques over the past years has resulted in the application of peptides or peptide-like drugs becoming a growing field in therapeutics. Because of the unfavorable chemical properties of peptides, it poses a challenge to find an optimized way of drug administration. The transdermal route has attracted interest as a promising way to advance the delivery of these drugs. The objective of this review is to summarize the level of research of microemulsions as colloidal carrier for dermal peptide drug delivery. The presented studies resulted in enhanced drug delivery or superior penetration profiles of peptides incorporated in microemulsions in comparison to conventional vehicles. Due to their benefits like high solubilization capacity, enhanced drug delivery, noninvasive administration or easy preparation, microemulsions offer a suitable vehicle for dermal and transdermal drug delivery.     

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。     

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。     

微乳在现代药剂学中的研究进展

从透皮、粘膜、注射和口服给药系统等方面综述了微乳在现代药剂学中的研究进展以及微乳中药物的吸收机理.     

Microemulsions: applications in transdermal and dermal delivery

Microemulsions have gained much interest as second-generation colloidal carrier systems for the dermal/transdermal delivery of the various hydrophilic and lipophilic drugs. The advantages associated with microemulsions include spontaneity of formation, ease of manufacturing, high solubilization capacity, and improved drug stability. This review focuses on the excipients available for the formulation of topical microemulsions and the potential mechanisms responsible for improvements in the dermal/transdermal delivery of therapeutic agents. It also describes the in vitro and in vivo investigations reported for the various classes of therapeutic agents, along with the recent developments.     

囊泡及微粒经皮给药系统的研究进展

近年来,各种方法被用于促进药物的经皮渗透,其中囊泡及微粒系统是一种简单便捷的方法.本文综述了促进药物经皮渗透的各种囊泡(变形脂质体、醇质体、类脂囊泡)及微粒系统(微乳、固体脂质纳米粒及纳米脂质载体)用于经皮给药系统的作用机制以及相关研究工作的进展.     

Influence of microemulsions on cutaneous drug delivery

In attempt to increase cutaneous drug delivery, microemulsion vehicles have been more and more frequently employed over recent years. Microemulsion formulations have been shown to be superior for both transdermal and dermal delivery of particularly lipophilic compounds, but also hydrophilic compounds appear to benefit from application in microemulsions compared to conventional vehicles, like hydrogels, emulsions and liposomes. The favourable drug delivery properties of microemulsions appear to mainly be attributed to the excellent solubility properties. However, the vehicles may also act as penetration enhancers depending on the oil/surfactant constituents, which involves a risk of inducing local irritancy. The correlation between microemulsion structure/composition and drug delivery potential is not yet fully elucidated. However, a few studies have indicated that the internal structure of microemulsions should allow free diffusion of the drug to optimise cutaneous delivery from these vehicles.     

Transdermal delivery of methotrexate: iontophoretic delivery from hydrogels and passive delivery from microemulsions

In vitro assays were performed to investigate the effectiveness of transdermal administration of methotrexate (MTX) by iontophoretic delivery from two types of hydrogel and passive delivery from two types of microemulsion. Both iontophoretic delivery of MTX from hydrogels and passive delivery from microemulsions were more effective than passive delivery from aqueous solutions of the drug. In the iontophoretic delivery assays, the type of hydrogel used and the concentration of the drug in the loading solution had little influence on effectiveness of delivery. In the passive delivery assays, we used both water/oil (w/o) and oil/water (o/w) microemulsions: effectiveness of delivery was higher from o/w systems. At the end of all assays, significant amounts of MTX were detected in the skin. These results suggest that both hydrogels and microemulsions may be of value for the topical administration of MTX in the treatment of psoriasis.     

Application of microemulsions in dermal and transdermal drug delivery

Microemulsions are thermodynamically stable colloidal dispersions of water and oil stabilized by a surfactant and, in many cases, also a cosurfactant. In the pharmaceutical field, microemulsions have been used as drug carriers for percutaneous, ocular, oral and parenteral administration. This review discusses some of the applications of microemulsions specifically for topical and transdermal applications. Microemulsion nomenclature and composition, with particular emphasis on choice of surfactant and cosurfactant, is discussed. Methods used to characterize microemulsions are reviewed. Microemulsion formulations for dermal and transdermal delivery of pharmaceutical agents with particular emphasis on anti-inflammatory and anaesthetic agents are critically evaluated. Finally, the issues which warrant further investigation by researchers in order to realize the full potential of the technology are discussed.     

Enhance transdermal delivery of flurbiprofen via microemulsions: Effects of different types of surfactants and cosurfactants

Background and the purpose of the study

Microemulsions are thermodynamically stable, clear dispersions of water, oil, surfactant, and cosurfactant. This study was aimed to develop flurbiprofen microemulsion for enhanced transdermal delivery and investigate the effects of different surfactants and cosurfactants on its delivery and phase behavior.

Method

Various surfactant-cosurfactant mixtures in ratio of 2:1 (Smix) along with oleic acid (oil) were selected and phase diagrams were constructed. Six microemulsions each containing 5% drug, 5% oil, 56% Smix and 34% water, were prepared and compared for their permeation and phase behaviors to determine the effects of the type of Smix.

Results

In vitro transdermal permeation through rabbit skin of all microemulsions was high than saturated aqueous drug solution. Tween 20 and ethanol as Smix produced the highest flux amongst all the Smix, and were used to prepare formulations with different values of oil and Smix. While the type of surfactant did not affect the droplet size, propylene glycol as cosurfactant produced the largest droplets and highest viscosity. Decrease in oil or Smix concentration resulted in decrease of the droplet size and increase in permeation flux while decrease in viscosity also increased the permeation flux of microemulsions. Finally the selected microemulsion formulation comprising 5% flurbiprofen, 5% oleic acid, 46% Tween 20:ethanol (2:1) and 44% water, showed the highest transdermal flux and caused no skin irritation.

Conclusion

Type of surfactant and cosurfactant affect both the phase behavior and transdermal drug delivery of microemulsion; and results of this study showed that they are promising vehicles for improved transdermal delivery and sustained action of flurbiprofen.