Department of Pharmaceutical Sciences, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, Liaoning 110016, China.
Int J Pharm. 2010 May 31;391(1-2):73-8. doi: 10.1016/j.ijpharm.2010.02.021. Epub 2010 Feb 17.
Anastrozole is a potent aromatase inhibitor and there is a need for an alternative to the oral method of administration to target cancer tissues. The purpose of the current study was to prepare a drug-in-adhesive transdermal patch for anastrozole and evaluate this for the site-specific delivery of anastrozole. Different adhesive matrixes, permeation enhancers and amounts of anastrozole were investigated for promoting the passage of anastrozole through the skin of rats in vitro. The best in vitro skin permeation profile was obtained with the formulation containing DURO-TAK 87-4098, IPM 8% and anastrozole 8%. For local tissue disposition studies, the anastrozole patch was applied to mouse abdominal skin, and blood, skin, and muscle samples were taken at different times after removing the residual adhesive from the skin. High accumulation of the drug in the skin and muscle tissue beneath the patch application site was observed in mice compared with that after oral administration. These findings show that anastrozole transdermal patches are an appropriate delivery system for application to the breast tumor region for site-specific drug delivery to obtain a high local drug concentration.
阿那曲唑是一种强效的芳香化酶抑制剂，需要一种替代口服给药的方法来靶向肿瘤组织。本研究的目的是制备阿那曲唑的药物贴剂，并评估其在阿那曲唑的局部递送上的应用。研究考察了不同的粘性基质、渗透促进剂和阿那曲唑的用量，以促进阿那曲唑在体外大鼠皮肤中的穿透。含有 DURO-TAK 87-4098、IPM 8%和阿那曲唑 8%的制剂获得了最佳的体外皮肤渗透谱。为了进行局部组织处置研究，将阿那曲唑贴片应用于小鼠腹部皮肤，并在从皮肤上去除残留的粘性物质后不同时间采集血液、皮肤和肌肉样本。与口服给药后相比，在贴剂应用部位下方的皮肤和肌肉组织中观察到药物的高蓄积。这些发现表明，阿那曲唑透皮贴片是一种合适的递药系统，可用于乳房肿瘤区域，以实现局部药物的靶向递送，从而获得高局部药物浓度。
