更昔洛韦脂质体的制备及其眼部药代动力学
Preparation and ocular pharmacokinetics of ganciclovir liposomes.
作者信息
Shen Yan, Tu Jiasheng
机构信息
Department of Pharmaceutics, China Pharmaceutical University, Nanjing, China.
出版信息
AAPS J. 2007 Dec 7;9(3):E371-7. doi: 10.1208/aapsj0903044.
Abstract
Ophthalmic liposomes of ganciclovir (GCV) were prepared by the reverse phase evaporation method, and their ocular pharmacokinetics in albino rabbits were compared with those obtained after dosing with GCV solution. The in vitro transcorneal permeability of GCV liposomes was found to be 3.9-fold higher than that of the solution. After in vivo instillation in albino rabbits, no difference was found in the precorneal elimination rate of GCV from liposome vs solution dosing. The aqueous humor concentration-time profiles of both liposomes and solution were well described by 2-compartmental pharmacokinetics with first-order absorption. The area under the curve of the aqueous humor concentration-time profiles of GCV liposomes was found to be 1.7-fold higher than that of GCV solution. Ocular tissue distribution of GCV from liposomes was 2 to 10 times higher in the sclera, cornea, iris, lens, and vitreous humor when compared with those observed after solution dosing. These results suggested that liposomes may hold some promise in ocular GCV delivery.
摘要
采用逆相蒸发法制备了更昔洛韦（GCV）眼用脂质体，并将其在白化兔中的眼药代动力学与给予GCV溶液后的药代动力学进行了比较。发现GCV脂质体的体外角膜透过率比溶液高3.9倍。在白化兔体内滴注后，脂质体给药与溶液给药相比，GCV在角膜前的消除率没有差异。脂质体和溶液的房水浓度-时间曲线均可用具有一级吸收的二室药代动力学很好地描述。发现GCV脂质体房水浓度-时间曲线的曲线下面积比GCV溶液高1.7倍。与溶液给药后相比，脂质体中GCV在巩膜、角膜、虹膜、晶状体和玻璃体液中的眼组织分布高2至10倍。这些结果表明脂质体在眼部递送GCV方面可能具有一定的前景。
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