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用于增强药物向离体和体内猪皮传递的长形微粒。

Elongate microparticles for enhanced drug delivery to ex vivo and in vivo pig skin.

机构信息

Dermatology Research Centre, School of Medicine, The University of Queensland, Princess Alexandra Hospital, Translational Research Institute, Brisbane 4102, QLD, Australia.

School of Veterinary Science, The University of Queensland, Gatton Campus, Gatton 4343, QLD, Australia.

出版信息

J Control Release. 2013 Nov 28;172(1):96-104. doi: 10.1016/j.jconrel.2013.07.025. Epub 2013 Aug 7.

Abstract

The delivery of therapeutics and cosmaceuticals into and/or through the skin is hindered by epidermal barriers. To overcome the skin's barriers we have developed a novel cutaneous delivery method using high aspect ratio elongate microparticles (EMPs). Using ex vivo and in vivo pig skin we assess the penetration and delivery characteristics of the elongate microparticles. With reflectance confocal microscopy we observed that the elongate microparticles successfully penetrated the epidermis and upper dermis. Delivery was then assessed using two different length populations of EMPs, comparing their delivery profile to topical alone using sodium fluorescein and confocal microscopy. We observed a relatively uniform and continuous delivery profile in the EMP treated area within the upper layers of the skin--up to seven times greater than topical alone. Finally, we delivered two therapeutically relevant compounds (Vitamins A and B3), showing enhanced delivery using the EMPs. To our knowledge this is the first report using high aspect ratio elongate microparticles in this manner for enhanced topical delivery to the skin.

摘要

治疗药物和化妆品进入和/或穿透皮肤的过程受到表皮屏障的阻碍。为了克服皮肤的屏障,我们开发了一种使用高纵横比的长形微颗粒(EMPs)的新型皮肤传递方法。我们使用离体和体内猪皮评估长形微颗粒的穿透和传递特性。通过反射共聚焦显微镜观察到,长形微颗粒成功穿透表皮和上部真皮。然后使用两种不同长度的 EMP 种群评估传递,将其与单独使用钠荧光素和共聚焦显微镜的局部传递进行比较。我们观察到在 EMP 处理区域内的皮肤上层中呈现出相对均匀和连续的传递曲线——比单独局部处理高 7 倍。最后,我们传递了两种治疗相关的化合物(维生素 A 和 B3),发现使用 EMP 可以增强其传递。据我们所知,这是首次以这种方式使用高纵横比的长形微颗粒来增强皮肤的局部传递。

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