Poly(amino acid)s: promising enzymatically degradable stealth coatings for liposomes

Int J Pharm. 2007 Mar 1;331(2):186-9. doi: 10.1016/j.ijpharm.2006.11.018. Epub 2006 Nov 11.

Abstract

Poly(amino acid)s (PAAs) were evaluated as coating polymers for long-circulating liposomes. The pharmacokinetics of PAA-coated liposomes were assessed in rats. Prolonged circulation times were obtained, comparable to those reported for poly(ethylene glycol) (PEG)-liposomes. Besides, the enzymatic degradability of PAAs was studied. PAAs - in free as well as liposome-associated form - are degradable by proteases, which is beneficial for reducing the risks of accumulation in vivo. Furthermore, complement activation by PAA-liposomes was evaluated in vitro and in vivo. Like other liposome types, they appear to activate the complement system. However, a role of endotoxin contamination of the PAA-liposome formulations used cannot be excluded in our complement activation studies.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Coated Materials, Biocompatible / chemistry*
  • Coated Materials, Biocompatible / metabolism
  • Coated Materials, Biocompatible / pharmacokinetics
  • Complement Activation / drug effects
  • Drug Carriers / chemistry*
  • Drug Carriers / metabolism
  • Drug Carriers / pharmacokinetics
  • Injections, Intravenous
  • Liposomes / chemistry*
  • Liposomes / metabolism
  • Liposomes / pharmacokinetics
  • Male
  • Nylons / chemistry
  • Nylons / metabolism
  • Nylons / pharmacokinetics*
  • Peptide Hydrolases / metabolism
  • Pharmacokinetics
  • Rats
  • Rats, Wistar

Substances

  • Coated Materials, Biocompatible
  • Drug Carriers
  • Liposomes
  • Nylons
  • Peptide Hydrolases