MRI Monitoring of Tumor-Selective Anticancer Drug Delivery with Stable Thermosensitive Liposomes Triggered by High-Intensity Focused Ultrasound

• DOI: 10.1021/acs.molpharmaceut.6b00013
• Publication Date: 2016-03-21T22:14:31Z
• Authors: Hyun Ryoung Kim; Dong Gil You; Sang-Jun Park; Kyu-Sil Choi; Wooram Um; Jae-Hun Kim; Jae Hyung Park; Young-sun Kim
• Keywords: High-intensity focused ultrasound

Monitoring of drug release from a heat-activated liposome carrier provides an opportunity for real-time control delivery and allows prediction the therapeutic effect. We have developed short-chain elastin-like polypeptide-incorporating thermosensitive liposomes (STLs). Here, we report development STL encapsulating gadobenate dimeglumine (Gd-BOPTA), MRI contrast agent, doxorubicin (Dox) (Gd-Dox-STL). The Dox profile Gd-Dox-STL was comparable to Gd-Dox-LTSL; however, serum stability much higher than Gd-Dox-LTSL. studies showed that difference in T1 relaxation time between 37 42 °C larger Although relaxivity both at similar, 2.5-fold lower This likely due Gd-BOPTA leakage LTSL because low °C. Pharmacokinetic plasma half-lives 4.85 1.95 h Gd-Dox-LTSL, respectively, consistent with vitro data. In vivo experiments demonstrated corelease under mild hyperthermia induced by high-intensity focused ultrasound (HIFU), which suggests is promising tumor selective formulation when coupled MR-guided HIFU.