物理技术促进药物经皮吸收的研究进展

发布时间：2018-04-22 20:21

本文选题：经皮给药系统 + 经皮吸收　；参考：《中国药房》2017年31期

【摘要】：目的:为加强经皮给药制剂的开发与应用提供参考。方法:以"微针""驻极体""离子导入""经皮给药系统""促渗""Microneedle""Electret""Inotophoresis""Transdermal drug delivery system"等为关键词,组合查询2001年1月-2017年2月在PubMed、ScienceDirect、中国知网、万方、维普等数据库中的相关文献,对促进药物经皮吸收的物理技术的研究进行综述。结果与结论:共检索到相关文献584篇,其中有效文献65篇。常用的单一物理技术促渗方法有微针、驻极体、离子、超声、电致孔、激光、磁场导入、热穿孔。其中,微针经皮给药适用于大分子药物(如皮肤渗透率较低的多肽、蛋白质和疫苗等);微针的针体长度、形状以及硬度、针壁厚度、载药量、滞留时间和体内降解问题是今后重点的研究对象。驻极体对离子型药物和非离子型药物都有良好的透皮促渗作用,但对离子型药物效果更佳;国内对于驻极体促渗的实验研究少,目前其临床应用无相关报道。离子导入、电致孔促渗在中药中的运用较热门,适用于电离性能较好的小分子药物(如胰岛素),但依赖带电装置及能量的特点导致推广受限。离子导入适用于慢性疾病如癌症和糖尿病的治疗;今后研究重点在于明确导入体内发挥作用的主要成分及其作用机制。超声导入主要适用于水溶性好的药物(如多肽和蛋白质);加强系统的安全性研究以及空化作用的机制研究、改善装置设计缺陷是今后研究的重点。利用激光破坏表皮的屏障作用促进药物经皮吸收,在医药领域应用前景良好。目前磁场导入与热穿孔技术促渗的国内外相关文献报道较少,今后的重点是加强这两者的机制、优化装置性能研究以及解决安全性问题。两种或多种物理技术的联用尽管能大大提高药物经皮透过率,但制作的复杂性和高成本是亟需突破的难题。
[Abstract]:Objective: to provide reference for the development and application of transdermal drug delivery. Methods: using "microneedle" "electret" "ion introduction" "percutaneous drug delivery system" "Microneedle", "Electret", "Inotophoresis" "Transdermal drug delivery system" as the keywords, the relevant documents in the database of PubMedine Science Direct, China knowledge Network, Wanfang, Weip, etc., from January 2001 to February 2017, were investigated. This paper reviews the research on physical techniques to promote drug percutaneous absorption. Results & conclusion: a total of 584 related literatures were retrieved, of which 65 were valid. The commonly used single physical techniques are microneedle, electret, ion, ultrasonic, electroporation, laser, magnetic field introduction, hot perforation. Among them, microneedle transdermal administration is suitable for macromolecular drugs (such as peptides, proteins and vaccines with low skin permeability, etc.); needle length, shape, hardness, thickness of needle wall, drug load, etc. Retention time and degradation in vivo are the key research objects in the future. Electret has good transdermal permeation effect on ionic drugs and Nonionic drugs, but it has better effect on ionic drugs. There are few experimental studies on electret permeation in China, and there are no related reports on its clinical application at present. The application of ion introduction and electroporation in traditional Chinese medicine is more popular. It is suitable for small molecular drugs with good ionization performance (such as insulin), but its popularization is limited due to its dependence on charged devices and energy. Iontophoresis is suitable for the treatment of chronic diseases such as cancer and diabetes. Ultrasonic introduction is mainly suitable for water-soluble drugs (such as peptides and proteins). It is the focus of the future research to strengthen the safety study of the system and the mechanism of cavitation mechanism, and to improve the design defects of the device. Using laser to destroy the barrier of epidermis to promote drug transdermal absorption has a good prospect in the field of medicine. At present, there are few reports about magnetic field introduction and hot perforation technology in domestic and foreign literature. In the future, the emphasis is to strengthen the mechanism of the two, optimize the performance of the device and solve the safety problems. Although the combination of two or more physical technologies can greatly improve the transdermal transmittance of drugs, the complexity and high cost of preparation are the difficult problems that need to be overcome.
【作者单位】：广东药科大学药学院/广东省药物新剂型重点实验室;
【基金】：广州市重点实验室专项项目(No.2014SY000005)
【分类号】：R943

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