Rajan Sunita
University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, 160014, India.
AAPS PharmSciTech. 2009;10(2):559-65. doi: 10.1208/s12249-009-9242-1.
The present investigation aims at developing microemulsion-based formulations for topical delivery of acyclovir. Various microemulsions were developed using isopropyl myristate/Captex 355/Labrafac as an oil phase, Tween 20 as surfactant, Span 20 as cosurfactant, and water/dimethylsulfoxide (1:3) as an aqueous phase. Transcutol, eucalyptus oil, and peppermint oil were used as permeation enhancers. In vitro permeation studies through laca mice skin were performed using Franz diffusion cells. The optimum formulation containing 2.5% Transcutol as the penetration enhancer showed 1.7-fold enhancement in flux and permeation coefficient as compared to marketed cream and ointment formulation. In vivo antiviral studies were performed in female Balb/c mice against induced herpes simplex virus I infection. A single application of microemulsion formulation containing 2.5% Transcutol given 24 h post-injection resulted in complete suppression of development of herpetic skin lesions.
本研究旨在开发用于阿昔洛韦局部给药的微乳剂配方。使用肉豆蔻酸异丙酯/癸二酸二异丙酯/ Labrafac作为油相、吐温20作为表面活性剂、司盘20作为助表面活性剂以及水/二甲基亚砜（1:3）作为水相来制备各种微乳剂。使用了二乙二醇单乙基醚、桉叶油和薄荷油作为渗透促进剂。通过Franz扩散池对无毛小鼠皮肤进行体外渗透研究。含有2.5%二乙二醇单乙基醚作为渗透促进剂的最佳配方与市售乳膏和软膏配方相比，通量和渗透系数提高了1.7倍。在雌性Balb/c小鼠中针对诱导的单纯疱疹病毒I感染进行了体内抗病毒研究。在注射后24小时单次应用含有2.5%二乙二醇单乙基醚的微乳剂配方可完全抑制疱疹性皮肤损伤的发展。
