Solid Lipid Nanoparticles: Phagocytic Uptake, in vitro Cytotoxicity and in vitro Biodegradation1 st Communication Rainer H. Müller and Carsten Olbrich Freie Universität Berlin, Institut für Pharmazie I (WE1), Pharmazeutische Technologie, Biopharmazie und Biotechnologie, Berlin (Germany) Dedicated to Prof. Gottfried Heinisch, Institut für Pharmazeutische Chemie, Leopold Franzens Universität Innsbruck (Austria), on the occasion of his 60th birthday Solid lipid nanoparticles (SLN) are an alternative delivery system for pharmaceutical and cosmetic ingredients to emulsions, liposomes and polymeric nanoparticles. Possible applications are the topical, peroral and the parenteral route. For the parenteral but also the peroral route information is required about the phagocytic uptake of the SLN by macrophages and the subsequent possible cytotoxicity or tolerability on the cellular level. Knowledge about the degradation velocity of SLN is essential for explaining the tolerability/non-tolerability by the cells and controlled adjustment of drug release by bulk erosion of the particle matrix. In the 1st communication of this review in vitro studies are presented showing the phagocytic uptake of differently composed lipid particles. It is demonstrated how controlled surface modification can reduce the uptake by macrophages - opening the perspectives to deliver drugs to sites other than the cells of the mononuclear phagocytic system (MPS). The 2nd communication focusses on cytotoxicity, especially in comparison to nanoparticles made from FDA-approved polymers, and shows in vitro data how biodegradation is affected by lipids and Surfactants used for SLN production - opening the perspective to control particle degradation and drug release -by optimised choice of the particle stabiliser. Key words Solid lipid nanoparticles, in vitro biodegradation, in vitro cytotoxicity, phagocytic uptake |
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pharmind 1999, Nr. 5, Seite 462
