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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 34, Number 1
BKCSDE 34(1)
January 20, 2013 

Dual Functional Gd(III)-DOTA Liposomes for Cancer Therapy and Diagnosis as a Theragnostic Carrier
Hee Dong Han, Suk Hyun Jung, Hasoo Seong, Sun Hang Cho, Byung Cheol Shin*
Liposome, Ultrasound sensitivity, Contrast agent, Doxorubicin
Development of dual functional liposome has been studied for cancer theragnostics. Therefore, we focused on ultrasound-sensitive liposomes with doxorubicin (DOX) and gadolinium (Gd) as a theragnostic carrier having a potential for cancer therapy and diagnosis. In this study, Gd(III)-DOTA-modified sonosensitive liposomes (GL) was developed using chemically synthesized Gd(III)-DOTA-DPPE lipid. Sonosensitivity of GL to 1 MHz ultrasound induced 25% of DOX release. The relaxivities (r1) of GL were 7.33-10.34 mM−1s−1, which was higher than that of MR-bester®. Intracellular delivery of DOX from GL by ultrasound irradiation was evaluated according to ultrasound intensity, resulting in increase of uptake of DOX released from ultrasoundtriggered GLs compared to GL3 or Doxil® without ultrasound. Taken together, this study shows that the paramagnetic and sonosensitive liposomes, GL, is a novel and highly effective delivery system for drug with the potential for broad applications in human disease.
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