Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, Mercer University, Atlanta, GA 30341, USA.
Skin Res Technol. 2011 May;17(2):234-44. doi: 10.1111/j.1600-0846.2010.00490.x. Epub 2011 Jan 28.
BACKGROUND/PURPOSE: Current Herpes labialis infection treatment by oral, parenteral or topical routes is inefficient. The objective of this study was to investigate the use of iontophoresis for improved topical delivery of acyclovir (ACV) in vivo in hairless rat.
Iontophoresis was performed for 10 min using a 5% ACV gel formulation. Tape stripping and skin extractions were performed at different time points following treatment for drug quantification in stratum corneum (SC) and underlying skin, respectively.
Fourfold more ACV was detected in the SC immediately following 10-min iontophoresis as compared with passive delivery. Similarly, high ACV levels (29.27±3.52 μg/cm(2)) were achieved in the underlying skin following a single 10-min iontophoretic treatment while no drug detected following passive delivery (P<0.05). At 24-h post-iontophoresis, ACV levels in the SC decreased with a corresponding increase in the underlying skin due to drug migration. After 24-h post-iontophoresis, drug levels gradually decreased in both skin compartments until no ACV was detected at 72-h post-iontophoresis.
Iontophoretic delivery of ACV resulted in high drug levels in skin layers to form a drug depot, which persisted over 2-3 days.
背景/目的：目前，通过口服、肠胃外或局部途径治疗唇疱疹感染的效果并不理想。本研究旨在研究电渗疗法在提高无毛发大鼠体内阿昔洛韦（ACV）的局部递送效率中的应用。
采用 5% ACV 凝胶制剂进行电渗 10 分钟。在治疗后不同时间点进行胶带剥离和皮肤提取，分别用于测定角质层（SC）和下层皮肤中的药物含量。
与被动给药相比，电渗 10 分钟后 SC 中检测到的 ACV 增加了 4 倍。同样，单次 10 分钟电渗治疗后，下层皮肤中可达到高 ACV 水平（29.27±3.52μg/cm²），而被动给药后则未检测到药物（P<0.05）。在电渗后 24 小时，SC 中的 ACV 水平因药物迁移而降低，同时下层皮肤中的 ACV 水平相应增加。电渗后 24 小时后，两种皮肤隔室中的药物水平逐渐降低，直到电渗后 72 小时后未检测到 ACV。
ACV 的电渗递药可在皮肤层中产生高药物水平，形成药物库，持续 2-3 天。
