To enhance the activity of amantadine against HCV, its amide prodrugs with thiazolidine-4-carboxylic acid derivatives (6-9) and bile acids (10 and 11) were designed and synthesized. In vitro kinetic stability of amide prodrugs 8 and 10 were investigated in aqueous buffer solution with variable pH values (1.2, 4.5. 6.8, 7.4. 8.0) and in biological fluids of 90% human plasma and rat liver homogenate at 37°C. In vivo release of the parent drug from these prodrug was investigated in mice with the thioazolidine-4-carboxylic acid amide 8 as representative of these delivery systems. Results from the in vivo distribution study indicated that the level of amantadine increased significantly in liver from 8 when compared to amantadine itself. The study suggested the synthesized delivery systems is promising carrier to enhance the hepatic bioavailability of amantadine.
قسم البحث
مجلة البحث
Digest Journal of Nanomaterials and Biostructures
الناشر
the Academy of Romanian Scientists
تصنيف البحث
1
عدد البحث
Vol. 6, No. 4
موقع البحث
http://www.chalcogen.infim.ro/1675_Fadl.pdf
سنة البحث
2011
المشارك في البحث
ملخص البحث