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Non-stealth (poly(lactic Acid/albumin)) And Stealth (poly(lactic Acid-polyethylene Glycol)) Nanoparticles As Injectable Drug Carriers

T. Verrecchia, G. Spenlehauer, D. Bazile, A. Murry-Brelier, Y. Archimbaud, M. Veillard
Published 1995 · Chemistry

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Abstract Stealth liposomes and, today, stealth nanoparticles, constitute a new generation of parenteral therapeutic systems. PLA/ abumin nanoparticles are of particular interest because they constitute fully biodegradable and well tolerated colloidal suspensions. Solvent evaporation and microfluidisation did not damage the albumin molecules; therefore, PLA/albumin nanoparticles are no more immunogenic than native albumin in solution. However, rapid albumin exchanges on the nanoparticle surface probably does not prevent C3-complement binding and phagocytosis by the liver Kupffer cells. Because of their possible intracellular accumulation and toxicity, PLA/albumin nanoparticles are presumably limited to subcutaneous or intramuscular administration. Poly( d,l -lactide)-poly (ethylene glycol) (PLA-PEG) is a new biodegradable hydrophobic dibloc copolymer. The oriented PEG layer, coating the nanoparticle surface, dramatically increases the plasma half-life of the colloidal carrier (‘stealth nanoparticles’ ). In this way, the PLAPEG nanoparticle half-life is about 6 h instead of a few minutes as for PLA/ albumin or PLA/poloxamer 188-coated nanoparticles. The plasma clearance of a water-insoluble hydrophobic drug encapsulated in stealth nanoparticles and administered intravenously, decreases very significantly in comparison with non-stealth nanoparticles. PLAPEG nanoparticles can be considered as a sustained release parenteral (intravenous) dosage form.
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