Siddoju Srujana, Sachdeva Vishal, Friden Phillip M, Banga Ajay K
College of Pharmacy and Health Sciences, Mercer University, Atlanta, GA.
PDA J Pharm Sci Technol. 2011 Sep-Oct;65(5):432-44. doi: 10.5731/pdajpst.2011.00756.
The objective of this study was to investigate the effect of iontophoresis on the intradermal and transdermal delivery of acyclovir using hairless rat skin on a vertical Franz diffusion cell. In this study, cathodal iontophoretic delivery of acyclovir from a pH 11 formulation was explored. The effects of time of iontophoresis (10 min, 1 h, and 4 h) and current density (0.2, 0.3, and 0.5 mA/cm(2)) on skin permeation were examined. In vitro dermal microdialysis was performed to identify the drug depot formed in the dermis during iontophoresis. Acyclovir delivery into the receptor compartment was not influenced by current density or duration of current application. However, greater drug levels were delivered into the skin as a function of time of current application to form a drug depot. These results were further confirmed by in vitro dermal microdialysis in which higher drug levels were observed in dialysate in the 4 h iontophoresis group due to higher drug levels delivered into the skin layers as compared to 1 h iontophoresis group. Short duration iontophoresis enhanced acyclovir delivery into the skin layers rapidly and thus may be beneficial to improve treatment for cold sores (herpes labialis infection). Microdialysis could be used as a tool to simultaneously monitor drug levels in the tissue's interstitial fluid in real time in an in vitro setting.
The objective of this study was to investigate the effect of current on the delivery of acyclovir into and across the skin using hairless rat skin mounted on glass diffusion cells. Acyclovir was delivered under negative polarity from a formulation with a very basic pH. The effect of current intensity and duration of application on delivery of acyclovir was investigated. The amount in the skin was also determined by inserting a probe into the skin with a semipermeable membrane that allows sampling of the drug that has entered the skin. When the current intensity or duration was increased, greater drug levels were seen in the skin but not across the skin. It was found that even short duration of current application can deliver acyclovir into the skin and this has potential use for treatment of cold sores.
本研究的目的是使用垂直式Franz扩散池，以无毛大鼠皮肤为模型，研究离子导入对阿昔洛韦皮内和经皮递送的影响。在本研究中，探索了从pH值为11的制剂中进行阿昔洛韦的阴极离子导入递送。研究了离子导入时间（10分钟、1小时和4小时）和电流密度（0.2、0.3和0.5 mA/cm²）对皮肤渗透的影响。进行了体外真皮微透析，以确定离子导入过程中在真皮中形成的药物储库。阿昔洛韦向受体室的递送不受电流密度或电流施加持续时间的影响。然而，随着电流施加时间的延长，更多的药物进入皮肤形成药物储库。体外真皮微透析进一步证实了这些结果，与1小时离子导入组相比，4小时离子导入组的透析液中观察到更高的药物水平，这是因为有更多的药物进入皮肤层。短时间离子导入可迅速增强阿昔洛韦向皮肤层的递送，因此可能有利于改善唇疱疹（唇疱疹感染）的治疗。微透析可作为一种工具，在体外实时同时监测组织间质液中的药物水平。
本研究的目的是使用安装在玻璃扩散池上的无毛大鼠皮肤，研究电流对阿昔洛韦进入皮肤和透过皮肤递送的影响。阿昔洛韦从具有高碱性pH值的制剂中在负极性下递送。研究了电流强度和施加持续时间对阿昔洛韦递送的影响。还通过将带有半透膜的探头插入皮肤来测定皮肤中的药物量，该半透膜允许对进入皮肤的药物进行采样。当电流强度或持续时间增加时，皮肤中的药物水平升高，但透过皮肤的药物水平未升高。发现即使是短时间的电流施加也能将阿昔洛韦递送至皮肤，这在唇疱疹治疗中具有潜在用途。
