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J Control Release. 2007 May 14;119(1):69-76. Epub 2007 Feb 1.

Optimum conditions for efficient phagocytosis of rifampicin-loaded PLGA microspheres by alveolar macrophages.

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Faculty of Pharmaceutical Sciences, Tokyo University of Science, 2641 Yamazaki Noda, Chiba 278-8510, Japan.


We examined the phagocytic activities of alveolar macrophages (NR8383 cells) toward poly(lactic-co-glycolic) acid (PLGA) microspheres (MS) loaded with the anti-tuberculosis agent rifampicin (RFP), the sizes of which were between 1 microm and 10 microm. We found that 1) the phagocytosis was dependent greatly on the particle size and the number of particles added; 2) macrophages phagocytosed considerably the PLGA microspheres loaded with RFP, the diameter of which was between 1 microm and 6 microm, but took up few 10-microm particles; 3) the population of the macrophages that phagocytosed 1-microm or 3-microm particles was larger than that of those phagocytosed 6- or 10-microm particles; 4) a considerable population of macrophages were not able to phagocytose even the 1- and 3-microm particles; 5) the most efficient deliveries of RFP into each macrophage cell and a large population of macrophages were achieved by the phagocytosis of 3-microm particles; and 6) phagocytosis did not affect macrophage viability in 4 h after the start of phagocytosis.

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