Novel drug release profiles from micellar solutions of PLA-PEO-PLA triblock copolymers
Novel drug release profiles from micellar solutions of PLA-PEO-PLA triblock copolymers
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DOI：
10.1016/j.jconrel.2005.12.024
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发表时间：
2006-05-01
影响因子：
10.8
通讯作者：
Bhatia, SR
中科院分区：
文献类型：
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作者：
Agrawal, SK;Sanabria-DeLong, N;Bhatia, SR
从聚丙交酯-聚氧乙烯-聚丙交酯三嵌段共聚物胶束溶液中，我们实现了两种疏水药物舒林酸和四环胺的近零级缓释行为，时间长达10-20天。考察了聚乳酸嵌段长度和结晶度对药物释放曲线的影响。研究了一系列PEO相对分子质量恒定为8900Da，聚乳酸相对分子质量在4100-650ODa范围内变化的聚合物。与无定形聚乳酸嵌段的聚合物相比，晶状聚乳酸嵌段的药物释放要快得多。药物的释放率也很大程度上取决于解放军封闭剂的长度。舒林酸的缓释时间长达20天，丁卡因的缓释时间长达10天。相比之下，这些药物在没有聚合物载体的情况下在4-6小时内释放。这一结果，连同提出的药物释放机制，表明聚合物-药物相互作用显著影响药物释放情况，导致药物缓慢和持续释放。(C)2006爱思唯尔B.V.保留所有权利。
We have achieved nearly zero order sustained release behavior for periods up to 10-20 days for two hydrophobic drugs, sulindac and tetracame, from 5 wt.% micellar solutions of poly(lactide)-poly(ethylene oxide)-poly(lactide) (PLA-PEO-PLA) triblock copolymer. The effect of PLA block length and crystallinity on the drug release profiles was studied. A series of polymers with constant PEO molecular weight of 8900Da and PLA molecular weight varying in the range of 4100-650ODa were examined. Drug release was found to be much faster for polymers with crystalline PLA blocks as compared to those with amorphous PLA blocks. The drug release rate also depends significantly on the length of the PLA block. Sustained release of sulindac was observed up to 20 days, and for tetracaine up to 10 days. By comparison, release of these drugs without polymeric carriers occurs over 4-6h. This result, along with a proposed mechanism for drug release, suggests that polymer-drug interactions significantly impact release profiles, causing slow and sustained release of the drug. (c) 2006 Elsevier B.V. All rights reserved.