Title:Improvement of Thermosensitive Liposome Stability by Cerasome Forming Lipid with Si-O-Si Network Structure
VOLUME: 15 ISSUE: 4
Author(s):Qin Su, Ximing Pu, He Bai, Xianchun Chen, Xiaoming Liao, Zhongbing Huang and Guangfu Yin*
Affiliation:College of Materials Science and Engineering, Sichuan University, Chengdu 610064, College of Materials Science and Engineering, Sichuan University, Chengdu 610064, College of Materials Science and Engineering, Sichuan University, Chengdu 610064, College of Materials Science and Engineering, Sichuan University, Chengdu 610064, College of Materials Science and Engineering, Sichuan University, Chengdu 610064, College of Materials Science and Engineering, Sichuan University, Chengdu 610064, College of Materials Science and Engineering, Sichuan University, Chengdu 610064
Keywords:Ceramic-like structured Si-O-Si net, cerasome forming lipid, DOX-loading, drug delivery, liposomes, structural
stability.
Abstract:Background: Liposomes have been widely used in gene transfection and drug delivery
systems due to their excellent biocompatibility and encapsulation ability, especially, the ability to
deliver the gene/drug into the cells via the membrane fusion. Thermosensitive liposomes have been
proven to be a precise and effective method for cancer treatment in many preclinical studies. But the
imperfect crystalline arrangement between grains occurred, resulting in planar defects at the boundaries
of membranes, compromising the stability of thermosensitive liposomes.
Objective: In the present study, we developed a facile method to improve the stability of ordinary thermosensitive
liposomes by introducing organic-inorganic hybrid materials with local Si-O-Si net.
Method: A cerasome forming lipid, N, N-Dihxadecyl-N'- [(3-triethoxysilyl) propyl] urea, was synthesized
and then introduced into the thermosensitive lipids to form the composite liposomes (named as
cera-liposomes). The effects of the cerasome forming lipid on the cera-liposomes characteristics, including
the morphology, drug loading, Zeta potential and stability of vesicles, were investigated.
Results: Cera-liposomes were thermosensitive, and they had a loading efficiency over 2 folds more than
conventional thermosensitive liposomes. With the enhanced sustain of Si-O-Si, cera-liposomes were
able to avoid collapsing and fusing during storage, and had a good resistance to nonionic surfactant.
More than 80% drug was still retained after storage of 15 days at room temperature.
Conclusion: The cerasome forming lipid showed potential in improving the stability of thermosensitive
liposomes. This novel kind of cera-liposomes could be a stable and effective drug carrier for anticancer
applications.
