AI Article Synopsis
- PEGylated cholesterol-containing liposomes are effective drug carriers, but their application is limited by cholesterol drawbacks and a phenomenon known as accelerated blood clearance (ABC) caused by PEG.
- Replacing cholesterol and PEG with ginsenoside Rg3 in liposomes (Rg3-lipo) offers comparable membrane stability and prolonged circulation without the complications of ABC.
- Studies show that Rg3-lipo maintains strong stealth properties in the bloodstream, avoiding immune reactions that typically occur with repeated doses of conventional liposomes, making it a promising alternative for drug delivery.
Article Abstract
PEGylated cholesterol-containing liposomes (Chol-PEG-lipo) have been widely used as a drug carrier for their good stealth property in blood circulation where cholesterol maintains the stability of the liposomal lipid bilayer and PEGylation endows liposomes with long circulation capability. However, cholesterol-related disadvantages and the accelerated blood clearance (ABC) phenomenon caused by PEGylation greatly limit the application of conventional stealth liposomes in clinic. Herein, ginsenoside Rg3 was selected to substitute cholesterol and PEG for liposomes preparation (Rg3-lipo). Rg3 was proved with similar liposomal membrane regulation ability to cholesterol and comparable long circulation effect to PEG. In addition, repeated administrations of Chol-PEG-lipo and Rg3-lipo were performed. The circulation time of the second dose of Chol-PEG-lipo was substantially reduced accompanied by a greatly increased accumulation in the liver due to the induction of anti-PEG IgM and the subsequent activated complement system. In contrast, no significantly increased level of relative plasma cells, IgM secretion and the complement activation in blood circulation was observed after the second injection of Rg3-lipo. As a result, Rg3-lipo showed great stealth property without ABC phenomenon. Therefore, developing liposomes utilizing Rg3 instead of PEG and cholesterol presents a promising strategy to prolong the blood circulation time of liposomes without triggering the ABC phenomenon and activated immune responses.
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| http://dx.doi.org/10.1016/j.jconrel.2023.10.023 | DOI Listing |
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