A potential approach for decreasing the burst effect of protein from PLGA microspheres
A potential approach for decreasing the burst effect of protein from PLGA microspheres
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DOI：
10.1002/jps.10414
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发表时间：
2003-08-01
影响因子：
3.8
通讯作者：
Langer, R
中科院分区：
文献类型：
--
作者：
Fu, K;Harrell, R;Langer, R
从生物可降解微球控制递送治疗剂的中心问题是注射后药物释放的立即爆发。这种爆发经常在通过双乳液（w/o/w）技术制成的微球系统中观察到，并且可以通过改善药物在整个聚合物基质中的分布来防止。为此，将蛋白质和聚合物（聚丙交酯-共-乙交酯或PLGA）溶解在相同的溶剂系统中，并通过自发乳化从该溶液产生微米尺寸的微球。通过使蛋白质与带电表面活性剂离子配对以增加在单相溶剂系统中的溶解度来实现改善的蛋白质负载。体外和体内结果均显示突释大大减少：与复乳法制备的微球相比，突释减少了10倍以上。(C)2003 Wiley-Liss，Inc.和美国药剂师协会
A central issue in controlled delivery of therapeutics from biodegradable microspheres is the immediate burst of drug release upon injection. This burst is often observed with microsphere systems made by the double emulsion (w/o/w) technique, and may be prevented by improving the drug distribution throughout the polymer matrix. To this end, protein and polymer (poly-lactide-co-glycolide or PLGA) were dissolved within the same solvent system, and micron-sized microspheres were created from this solution by spontaneous emulsification. Improved protein loading was achieved by ion-pairing the protein with charged surfactants to increase solubility in the single-phase solvent system. Both in vitro and in vivo results showed a much diminished burst: compared to microspheres made by double emulsion, it was reduced over 10-fold. (C) 2003 Wiley-Liss, Inc. and the American Pharmacists Association.