A Thermoresponsive Bubble-Generating Liposomal System for Triggering Localized Extracellular Drug Delivery

作者：Chen Ko Jie; Liang Hsiang Fa; Chen Hsin Lung; Wang Yucai; Cheng Po Yuan; Liu Hao Li; Xia Younan^*; Sung Hsing Wen

来源：ACS Nano, 2013, 7(1): 438-446.

DOI：10.1021/nn304474j

• thermoresponsive liposome
• triggered release
• drug delivery
• doxorubicin
• chemotherapy

The therapeutic effectiveness of chemotherapy is optimal only when tumor cells are subjected to a maximum drug exposure. To increase the intratumoral drug concentration and thus the efficacy of chemotherapy, a thermoresponsive bubble-generating liposomal system is proposed for triggering localized extracellular drug delivery. The key component of this liposomal formulation is the encapsulated ammonium bicarbonate (ABC), which is used to create the transmembrane gradient needed for a highly efficient encapsulation of doxorubicin (DOX). At an elevated temperature (42 degrees C), decomposition of ABC generates CO2 bubbles, creating permeable defects in the lipid Mayer that rapidly release DOX and instantly increase the drug concentration locally. Because the generated CO2 bubbles are hyperechogenic, they also enhance ultrasound imaging. Consequently, this new liposomal system encapsulated with ABC may also provide an ability to monitor a temperature-controlled drug delivery process.

• 出版日期2013-1
• 单位长春大学; 清华大学