University of Kentucky, College of Pharmacy, Department of Pharmaceutical Sciences, 459 Wethington Bldg, Lexington, KY 40536-0082, USA.
Expert Opin Drug Deliv. 2010 May;7(5):617-29. doi: 10.1517/17425241003663228.
The efficacy of microneedles in the area of transdermal drug delivery is well documented. Multiple studies have shown that enhancement of skin permeation by means of the creation of microscopic pores in the stratum corneum can greatly improve the delivery rates of drugs. However, skin pretreatment with microneedles is not the only factor affecting drug transport rates. Other factors, including drug formulation and rate of micropore closure, are also important for optimizing delivery by this route.
This review aims to highlight work that has been done in these areas, with an emphasis on drug formulation parameters that affect transdermal flux.
This review creates an appreciation for the many factors affecting microneedle-enhanced delivery. Most results clearly indicate that microneedle skin pretreatment by itself may have different effects on drug transport depending on the formulation used, and formulation characteristics have different effects on the transport through untreated skin and microneedle-treated skin. Several formulation approaches are reported to optimize microneedle-enhanced drug delivery, including co-solvent use, vesicular, nanoparticulate and gel systems.
In addition to well-established factors that affect microneedle-assisted delivery (geometry, type of microneedle, etc.), formulation and pore viability are also critical factors that must be considered.
微针在经皮药物传递领域的功效已有充分记录。多项研究表明，通过在角质层中创建微小孔隙来增强皮肤渗透，可以大大提高药物的递送速率。然而，微针预处理并不是影响药物传输速率的唯一因素。其他因素，包括药物配方和微孔闭合率，对于通过这种途径优化递送也很重要。
本综述的重点是突出在这些领域所做的工作，重点介绍影响透皮通量的药物配方参数。
本综述使人们对影响微针增强传递的许多因素有了更深入的了解。大多数结果清楚地表明，根据所用配方的不同，微针皮肤预处理本身可能对药物传输有不同的影响，并且配方特性对未处理皮肤和微针处理皮肤的传输有不同的影响。有几种配方方法被报道可以优化微针增强药物递送，包括共溶剂使用、囊泡、纳米颗粒和凝胶系统。
除了影响微针辅助递送的既定因素（几何形状、微针类型等）外，配方和孔的活力也是必须考虑的关键因素。
