Johnstone Sharon, Ansell Steven, Xie Sherwin, Mayer Lawrence, Tardi Paul
Celator Pharmaceuticals Inc., 1779 W 75th Avenue, Vancouver, BC, Canada V6P 6P2.
J Drug Deliv. 2011;2011:349206. doi: 10.1155/2011/349206. Epub 2011 Jul 7.
Diblock copolymer nanoparticles encapsulating a paclitaxel prodrug, Propac 7, have been used to demonstrate the usefulness of a nonmetabolizable radioactive marker, cholesteryl hexadecyl ether (CHE), to evaluate nanoparticle formulation variables. Since CHE did not exchange out of the nanoparticles, the rate of clearance of the CHE could be used as an indicator of nanoparticle stability in vivo. We simultaneously monitored prodrug circulation and carrier circulation in the plasma and the retention of CHE relative to the retention of prodrug in the plasma was used to distinguish prodrug release from nanoparticle plasma clearance. Nanoparticles labelled with CHE were also used to evaluate accumulation of nanoparticles in the tumour. This marker has provided relevant data which we have applied to optimise our nanoparticle formulations.
包裹紫杉醇前药Propac 7的双嵌段共聚物纳米颗粒已被用于证明一种不可代谢的放射性标记物——十六烷基胆固醇醚（CHE）在评估纳米颗粒制剂变量方面的有用性。由于CHE不会从纳米颗粒中交换出来，CHE的清除率可作为纳米颗粒在体内稳定性的指标。我们同时监测了前药在血浆中的循环和载体在血浆中的循环，并利用CHE相对于前药在血浆中的保留率来区分前药从纳米颗粒血浆清除中的释放情况。用CHE标记的纳米颗粒也被用于评估纳米颗粒在肿瘤中的积累情况。这种标记物提供了相关数据，我们已将其应用于优化我们的纳米颗粒制剂。
