The School of Pharmacy and Bioengineering, Keele University, Keele, Staffordshire ST5 5BG, United Kingdom.
The School of Pharmacy, University of Nottingham, University Park, Nottingham NG7 2RD, United Kingdom.
J Pharm Pharmacol. 2024 Oct 3;76(10):1284-1300. doi: 10.1093/jpp/rgae080.
Poly(amidoamine) dendrimers have been widely investigated as potential nanomaterials that can enhance the skin permeation of topically applied drugs. This article reviews the studies that have used dendrimers as penetration enhancers and examines the mechanisms by which enhancement is claimed.
A wide range of studies have demonstrated that, in certain circumstances and for certain drugs, the incorporation of dendrimers into a topically applied formulation can significantly increase the amount of drug passing into and through the skin. In some cases, dendrimers offered little or no enhancement of skin permeation, suggesting that the drug-dendrimer interaction and the selection of a specific dendrimer were central to ensuring optimal enhancement of skin permeation. Significant interactions between dendrimers and other formulation components were also reported in some cases.
Dendrimers offer substantial potential for enhancing drug delivery into and across the skin, putatively by mechanisms that include occlusion and changes to surface tension. However, most of these studies are conducted in vitro and limited progress has been made beyond such laboratory studies, some of which are conducted using membranes of limited relevance to humans, such as rodent skin. Thus, the outcomes and claims of such studies should be treated with caution.
聚酰胺-胺树枝状大分子已被广泛研究为潜在的纳米材料,可增强局部应用药物的皮肤渗透。本文综述了将树枝状大分子用作渗透增强剂的研究,并考察了据称的增强机制。
大量研究表明,在某些情况下,对于某些药物,将树枝状大分子掺入局部应用制剂中可以显著增加进入和穿过皮肤的药物量。在某些情况下,树枝状大分子对皮肤渗透几乎没有增强作用,这表明药物-树枝状大分子相互作用和特定树枝状大分子的选择对于确保皮肤渗透的最佳增强至关重要。在某些情况下,还报道了树枝状大分子与其他制剂成分之间的显著相互作用。
树枝状大分子为药物递送入和穿过皮肤提供了很大的潜力,推测其机制包括封闭和表面张力的改变。然而,这些研究大多是在体外进行的,除了这些实验室研究之外,进展甚微,其中一些研究使用与人类相关性有限的膜,例如啮齿动物皮肤。因此,此类研究的结果和结论应谨慎对待。