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Updated: Aug 10, 2025

Delivery of Therapeutic siRNA to the CNS Using Cationic and Anionic Liposomes
Published on: July 23, 2016
Anionic liposomes prepared without organic solvents for effective siRNA delivery
Xiu Han1, Yan Lu2, Zhaoluo Xu1
1Department of Clinical Pharmacy, Affiliated Jinling Hospital, Medical School of Nanjing University, Nanjing, China.
Glycerol enables simple, solvent-free preparation of anionic liposomes for effective siRNA delivery. These liposomes show high encapsulation efficiency, promote endosomal escape, and are non-toxic, offering a safe platform for nucleic acid drugs.
Area of Science:
- Biotechnology
- Materials Science
- Drug Delivery
Background:
- Traditional anionic liposome preparation for siRNA delivery relies on organic solvents, posing challenges in removal and stability.
- Residual organic solvents can be hazardous and negatively impact liposome integrity.
Purpose of the Study:
- To develop a novel, efficient, and safe method for preparing anionic liposomes using glycerol as a physiologically compatible medium.
- To evaluate the efficacy of glycerol-prepared anionic liposomes for siRNA encapsulation, delivery, and therapeutic potential.
Main Methods:
- Anionic liposomes were prepared using glycerol to promote lipid dispersion and liposome formation, avoiding organic solvents.
- Small interfering RNA (siRNA) encapsulation was achieved using calcium ions (Ca2+), with encapsulation efficiency optimized.
- Cell viability assays and studies on siRNA resistance to degradation were performed.
Main Results:
- Spherical anionic liposomes with an average particle size of 188.9 nm were successfully synthesized using glycerol.
- A maximum siRNA encapsulation efficiency of 91% was achieved at 2.4 mM Ca2+.
- Calcium phosphate formation facilitated endosomal escape, anionic liposomes enhanced siRNA stability, and demonstrated effective gene knockout with no significant cytotoxicity.
Conclusions:
- Glycerol provides a safe, efficient, and solvent-free method for anionic liposome preparation, suitable for siRNA delivery.
- These liposomes represent a promising platform for delivering siRNA and other nucleic acid therapeutics, enhancing stability and efficacy.
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