Nanoparticle-Stabilized Liposomes for pH-Responsive Gastric Drug Delivery

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• 作者：Soracha Thamphiwatana ; Victoria Fu ; Jingying Zhu ; Diannan Lu ; Weiwei Gao ; Liangfang Zhang
• 刊名：Langmuir
• 出版年：2013
• 出版时间：October 1, 2013
• 年：2013
• 卷：29
• 期：39
• 页码：12228-12233
• 全文大小：292K
• 年卷期：v.29,no.39(October 1, 2013)
• ISSN：1520-5827

文摘

We report a novel pH-responsive gold nanoparticle-stabilized liposome system for gastric antimicrobial delivery. By adsorbing small chitosan-modified gold nanoparticles (diameter 10 nm) onto the outer surface of negatively charged phospholipid liposomes (diameter 75 nm), we show that at gastric pH the liposomes have excellent stability with limited fusion ability and negligible cargo releases. However, when the stabilized liposomes are present in an environment with neutral pH, the gold stabilizers detach from the liposomes, resulting in free liposomes that can actively fuse with bacterial membranes. Using Helicobacter pylori as a model bacterium and doxycycline as a model antibiotic, we demonstrate such pH-responsive fusion activity and drug release profile of the nanoparticle-stabilized liposomes. Particularly, at neutral pH the gold nanoparticles detach, and thus the doxycycline-loaded liposomes rapidly fuse with bacteria and cause superior bactericidal efficacy as compared to the free doxycycline counterpart. Our results suggest that the reported liposome system holds a substantial potential for gastric drug delivery; it remains inactive (stable) in the stomach lumen but actively interacts with bacteria once it reaches the mucus layer of the stomach where the bacteria may reside.