Serum-Stable, Long-Circulating, pH-Sensitive PEGylated Liposomes.

Methods Mol Biol

Institute of Pharmaceutical Sciences, ETH Zürich, Vladimir-Prelog-Weg 3, HCI H 301, 8093, Zürich, Switzerland.

Published: January 2018

AI Article Synopsis

  • pH-sensitive liposomes are engineered to release drugs specifically in acidic cellular environments, enhancing their effectiveness.
  • These liposomes remain stable at normal physiological pH but release their contents when they enter acidic organelles, protecting the drugs from degradation.
  • The chapter also discusses the synthesis of a copolymer that improves the stability and drug release profile of these liposomes, alongside methods for preparing and analyzing them.

Article Abstract

pH-sensitive liposomes have been designed to deliver active compounds, specifically to acidic intracellular organelles, and to augment their cytoplasmic concentrations. These systems combine the protective effects of other liposomal formulations with specific environment-controlled drug release. They are stable at physiological pH, but abruptly discharge their contents when endocytosed into acidic compartments, allowing the drug to be released before it is exposed to the harsh environment of the lysosomes.Serum-stable formulations with minimal leakage at physiological pH and rapid drug release at pH 5.0 to 5.5 can be easily prepared by inserting a hydrophobically modified N-isopropylacrylamide/methacrylic acid copolymer (poly(NIPAM-co-MAA)) in the lipid bilayer of sterically stabilized liposomes. The present chapter describes polymer synthesis, as well as the preparation and characterization of large unilamellar pH-sensitive vesicles.

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http://dx.doi.org/10.1007/978-1-4939-6591-5_15DOI Listing

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