阿昔洛韦乳膏和凝胶制剂经皮离子导入给药的评价。

Evaluation of acyclovir cream and gel formulations for transdermal iontophoretic delivery.

作者信息

Siddoju Srujana, Sachdeva Vishal, Friden Phillip M, Banga Ajay K

机构信息

Department of Pharmaceutical Sciences, Mercer University. 3001 Mercer University Drive, Atlanta, GA 30341, USA.

出版信息

Ther Deliv. 2012 Mar;3(3):327-38. doi: 10.4155/tde.11.152.

DOI:10.4155/tde.11.152

PMID:22833993

Abstract

BACKGROUND

Efficient iontophoretic transdermal delivery of hydrophilic drug molecules requires selection of appropriate aqueous formulation. In this study, oil/water cream and gel formulations were investigated for iontophoretic transdermal delivery of acyclovir (ACV), a model hydrophilic small-drug molecule, across hairless rat skin on Franz diffusion cells.

RESULTS

Iontophoresis (0.2 mA/cm2) enhanced ACV delivery from both 5% cream (pH 6.8) and 4% gel (pH II) formulations. However, sixfold higher drug levels were delivered across the skin using gel formulation (12.25 +/- 4.04 microg/cm2) as compared with cream formulation (2.03 +/- 0.05 microg/cm2). Significantly higher drug levels were delivered when iontophoresis was performed at higher current density (0.32 mA/cm2; p < 0.05). Influence of formulation co-solvents (glycerin and propylene glycol) on drug delivery was also investigated in vitro using Franz cells and in vivo in hairless rats using microdialysis.

CONCLUSION

Iontophoretic transdermal delivery of ACV was feasible and dependent on the selection of formulation components and delivery parameters.

摘要

背景

亲水性药物分子的高效离子电渗透皮给药需要选择合适的水性制剂。在本研究中，研究了油/水乳剂和凝胶制剂用于阿昔洛韦（ACV，一种典型的亲水性小分子药物）在Franz扩散池上透过无毛大鼠皮肤的离子电渗透皮给药。

结果

离子电渗（0.2 mA/cm²）增强了ACV从5%乳剂（pH 6.8）和4%凝胶（pH 11）制剂中的释放。然而，与乳剂制剂（2.03±0.05 μg/cm²）相比，使用凝胶制剂（12.25±4.04 μg/cm²）时经皮肤递送的药物水平高出六倍。当在更高电流密度（0.32 mA/cm²；p<0.05）下进行离子电渗时，递送的药物水平显著更高。还使用Franz细胞在体外以及在无毛大鼠体内使用微透析研究了制剂助溶剂（甘油和丙二醇）对药物递送的影响。