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聚酰胺-胺树枝状大分子 G3 和 G4 对 8-甲氧基补骨脂素经皮渗透的影响——体内研究。

Effect of polyamidoamine dendrimer G3 and G4 on skin permeation of 8-methoxypsoralene--in vivo study.

机构信息

Department of Cosmetology, University of Information Technology and Management In Rzeszów, 2 Sucharskiego Str., 35-325 Rzeszów, Poland.

Department of Cosmetology, University of Information Technology and Management In Rzeszów, 2 Sucharskiego Str., 35-325 Rzeszów, Poland.

出版信息

Int J Pharm. 2012 Apr 15;426(1-2):280-283. doi: 10.1016/j.ijpharm.2012.01.041. Epub 2012 Jan 30.

Abstract

In the present study we have assessed the ability of (PAMAM) dendrimers G3 and G4 to facilitate transdermal delivery of 8-methoxypsoralen (8-MOP) in vivo. In vitro study using Franz diffusion cell revealed an enhanced transdermal flux for 8-MOP in complex with G3 and G4 dendrimer in relation to standard 8-MOP solution. In present study in vivo skin permeation potential of 8-MOP complex with G3 and G4 PAMAM dendrimer was assessed using confocal laser scanning microscopy (CLSM), which revealed an enhanced permeation of the 8-MOP to the deeper layers of the skin and significantly higher concentration in comparison with standard 8-MOP solution. Skin tissue 8-MOP concentration, evaluated by HPLC indicates that G3 and G4 PAMAM application significantly increase 8-MOP skin deposition in comparison with standard 8-MOP solutions after 1 and 2h. G4 appeared to be a more effective 8-MOP penetration enhancer than G3 PAMAM. Our results suggest the feasibility of G3 and G4 PAMAM dendrimers for transdermal delivery of 8-MOP resulting in better skin permeation and higher concentration of 8-MOP in epidermis and dermis of the drug that could help to improve effectiveness and safety of PUVA therapy.

摘要

在本研究中,我们评估了(PAMAM)树枝状大分子 G3 和 G4 促进 8-甲氧基补骨脂素(8-MOP)体内经皮传递的能力。使用 Franz 扩散池的体外研究表明,与标准 8-MOP 溶液相比,G3 和 G4 树枝状大分子与 8-MOP 形成复合物后,8-MOP 的经皮通量得到增强。在本研究中,使用共聚焦激光扫描显微镜(CLSM)评估了 8-MOP 与 G3 和 G4 PAMAM 树枝状大分子复合物的体内皮肤渗透潜力,结果表明 8-MOP 向皮肤深层的渗透增强,与标准 8-MOP 溶液相比,皮肤中的浓度显著更高。通过 HPLC 评估皮肤组织中的 8-MOP 浓度表明,与标准 8-MOP 溶液相比,G3 和 G4 PAMAM 应用后 1 和 2 小时,8-MOP 在皮肤中的沉积显著增加。与 G3 PAMAM 相比,G4 似乎是一种更有效的 8-MOP 渗透增强剂。我们的研究结果表明,G3 和 G4 PAMAM 树枝状大分子可用于 8-MOP 的经皮传递,从而改善 8-MOP 的皮肤渗透和表皮和真皮中的 8-MOP 浓度,这可能有助于提高 PUVA 治疗的效果和安全性。

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