title: Liposomal stabilization using a sugar-based, PEGylated amphiphilic macromolecule.
abstract: Liposomes are an important class of colloidal drug delivery systems, yet the clinical applications of conventional liposomes can be hampered by poor colloidal and biological stabilities. In this work, a sugar-based, PEGylated amphiphilic macromolecule (AM) was evaluated for its ability to stabilize dipalmitoyl phosphatidylcholine (DPPC)-based liposomes. Compared to unmodified liposomes, AM-stabilized liposomes exhibited enhanced colloidal stability, maintaining relatively constant particle sizes for 5 weeks without aggregation. AM-stabilized liposomes also showed significantly decreased membrane permeability, even in the presence of serum. Finally, AM-stabilized liposomes displayed improved biological stability, significantly inhibiting phagocytosis by macrophages. Overall, the effectiveness of AM to stabilize liposomes was comparable to a conventional stabilizing agent, PEG-modified phosphatidylethanolamine. Based upon these results, AM is a promising stabilizing agent for colloidal drug delivery applications and currently being optimized.
authors.affiliation: Department of Pharmaceutics, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, NJ 08854, USA.
authors.forename: Li
authors.initials: L
authors.lastname: Tao
authors.affiliation: Department of Chemistry and Chemical Biology, Rutgers, The State University of New Jersey, Piscataway, NJ 08854, USA.
authors.forename: Allison
authors.initials: A
authors.lastname: Faig
authors.affiliation: Department of Pharmaceutics, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, NJ 08854, USA; Department of Chemistry and Chemical Biology, Rutgers, The State University of New Jersey, Piscataway, NJ 08854, USA. Electronic address: keuhrich@rutgers.edu.
authors.forename: Kathryn E
authors.initials: KE
authors.lastname: Uhrich
mesh_terms: D015060:1,2-Dipalmitoylphosphatidylcholine / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D002460:Cell Line; D003102:Colloids; D008081:Liposomes; D008264:Macrophages / Q000166:cytology / Q000378:metabolism*; D051379:Mice; D010587:Phagocytosis / Q000187:drug effects*; D011092:Polyethylene Glycols / Q000737:chemistry / Q000494:pharmacology
chemical_list: D003102:Colloids; D008081:Liposomes; D015060:1,2-Dipalmitoylphosphatidylcholine; D011092:Polyethylene Glycols
keywords: Aggregation; Amphiphilic macromolecule; Liposome stabilization; Phagocytosis