Dipartimento di Scienze del Farmaco, Università degli Studi di Catania, Viale A. Doria 6, 95125 Catania, Italy.
Int J Pharm. 2012 Oct 15;436(1-2):135-40. doi: 10.1016/j.ijpharm.2012.06.034. Epub 2012 Jun 21.
1,1',2-Trisnorsqualenoic acid was conjugated to paclitaxel to obtain the squalenoyl-paclitaxel prodrug with the aim to improve the incorporation in phospholipid bilayers. Differential scanning calorimetry technique was employed to compare the interaction of squalenoyl-paclitaxel prodrug and free paclitaxel with phospholipid bilayers. The possibility of using lipid vesicles as carrier for the prodrug was also evaluated. An increased encapsulation into phospholipid bilayers of squalenoyl-paclitaxel with respect to the free drug was observed. The ability of lipid vesicles to retain the loaded prodrug was also observed which make this system to be considered as carrier for the prodrug.
1,1',2-三异戊烯基 squalenic 酸与紫杉醇连接，得到 squalenoyl-紫杉醇前药，旨在提高其在磷脂双层中的掺入。采用差示扫描量热法比较 squalenoyl-紫杉醇前药与游离紫杉醇与磷脂双层的相互作用。还评估了脂质体作为前药载体的可能性。观察到与游离药物相比，salenoyl-紫杉醇更能包封入磷脂双层中。还观察到脂质体保留负载前药的能力，这使得该系统被认为是前药的载体。
