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论文类型：期刊论文

发表时间：2009-05-01

发表刊物：JOURNAL OF DRUG TARGETING

收录刊物：PubMed、SCIE

卷号：17

期号：4

页面范围：286-293

ISSN号：1061-186X

关键字：PLGA microspheres; lung targeting; yuanhuacine; fluorescent spiropyran labeled; anticancer

摘要：The present study was intended to develop poly(D,L-lactide-co-glycolide) (PLGA; 50:50, 0.15 dL/g) microspheres (MS) loaded with yuanhuacine (YHC) for passive targeting in lung as well as providing a simple evaluation method for the targeting efficiency of MS. A kind of photochromic spiropyran dye was applied to label MS to clearly demonstrate the in vivo distribution characteristics through intravenous injection into mice and rabbits. Sections of 10-mu m thickness from different organs were cut using a microtome, and fluorescent microscopy was used to determine the biodistribution of the MS. The average particle size of MS was 9.0 mu m, and the glass transition temperature was 37-40 degrees C. In vitro, the cumulative release achieved 50.8% in 24 h. Histological sections from different organs indicated that the amount of MS in lung achieved maximum in 6 h, as about 8 times as in liver and 70 times higher than the average concentration of other organs. In vivo, MS were gradually swelled and drug concentration remained just 10% in 12 h, which would not result in long time embolization in the lung. This evaluation method supplies a simple and visualized channel in focus for the targeting efficiency of PLGA MS.