CBMN, Université de Bordeaux, CNRS, Bordeaux INP, Pessac, France.
U1312-BRIC, Inserm, Université de Bordeaux, National Reference Center for Rare Skin Diseases, Bordeaux, France.
J Liposome Res. 2023 Sep;33(3):314-327. doi: 10.1080/08982104.2023.2177309. Epub 2023 Feb 13.
Hydrocortisone (HyC), a hydrophobic pharmaceutical active, was encapsulated in multi-lamellar liposomes (MLLs) composed of P100, a mixture of phospholipids, and Tween®80. Three different HyC-loaded formulations were designed to target the , the living epidermis and the hypodermis. The impact of encapsulation on their size, elasticity and zeta potential, the three key factors controlling MLLs skin penetration, was studied. Raman mapping of phospholipids and HyC allowed the localisation of both components inside an artificial skin, Strat-M®, demonstrating the efficiency of the targeting. Percutaneous permeation profiles through excised human skin were performed over 48 h, supporting results on artificial skin. Their modelling revealed that HyC encapsulated in MLLs, designed to target the and living epidermis, exhibited a non-Fickian diffusion process. In contrast, a Fickian diffusion was found for HyC administered in solution, in a pharmaceutical cream and in transdermal MLLs. These results allowed us to propose a mechanism of interaction between HyC-containing MLLs and the skin.
将氢化可的松(HyC)这种疏水性药物活性成分包封于多层脂质体(MLL)中,该脂质体由磷脂混合物 P100 和吐温®80 组成。设计了三种不同的载有 HyC 的制剂,以针对角质层、生活表皮和真皮层。研究了包封对其大小、弹性和zeta 电位的影响,这三个关键因素控制着 MLL 对皮肤的穿透性。在人工皮肤 Strat-M®上进行的磷脂和 HyC 的 Raman 映射证明了两种成分在内部的定位,证明了靶向的效率。通过离体人皮肤进行了长达 48 小时的经皮渗透曲线,支持了人工皮肤的结果。其模型表明,设计用于靶向角质层和生活表皮的 HyC 包封于 MLL 中,表现出非菲克扩散过程。相比之下,HyC 在溶液中、在药物乳膏中和经皮 MLL 中的给药则呈现出菲克扩散。这些结果使我们能够提出 HyC 载于 MLL 与皮肤之间的相互作用机制。