Highly loaded, sustained-release microparticles of curcumin for chemoprevention.
Highly loaded, sustained-release microparticles of curcumin for chemoprevention.
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DOI：
10.1002/jps.22475
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发表时间：
2011-07
影响因子：
3.8
通讯作者：
Panyam, Jayanth
中科院分区：
文献类型：
--
作者：
Shahani, Komal;Panyam, Jayanth
关键词：
姜黄素是一种膳食多酚，具有预防和治疗多种疾病的潜力。由于许多这些疾病的慢性性质，姜黄素的缓释剂型可能具有重要的临床价值。然而，姜黄素的极端亲脂性和不稳定性是其制剂开发中的重大挑战。本研究的目的是制造一种可注射的微粒制剂，可以在1个月的时间内维持姜黄素的释放，并确定其在小鼠模型中的化学预防活性。使用聚（D，L-丙交酯-共-乙交酯）聚合物制造微粒。常规的制备微粒的乳化溶剂蒸发方法导致姜黄素在微粒外部结晶并且包封差（~ 1%，w/w负载）。使用真空快速去除溶剂显著增加了药物包封（~ 38%，w/w负载; 76%包封率）。微粒在体外持续释放姜黄素超过4周，并且药物释放速率可以通过改变聚合物分子量和/或组成来调节。一个单一的皮下剂量的微粒维持姜黄素肝脏浓度近一个月的小鼠。肝谷胱甘肽-S-转移酶和环氧合酶-2的活动，化学预防的生物标志物，改变后与姜黄素微粒治疗。这些研究结果表明，姜黄素缓释微粒可能是一种新的和有效的癌症化学预防方法。
Curcumin, a dietary polyphenol, has preventive and therapeutic potential against several diseases. Because of the chronic nature of many of these diseases, sustained-release dosage forms of curcumin could be of significant clinical value. However, extreme lipophilicity and instability of curcumin are significant challenges in its formulation development. The objectives of this study were to fabricate an injectable microparticle formulation that can sustain curcumin release over a 1-month period and to determine its chemopreventive activity in a mouse model. Microparticles were fabricated using poly(D, L-lactide-co-glycolide) polymer. Conventional emulsion solvent evaporation method of preparing microparticles resulted in crystallization of curcumin outside of microparticles and poor entrapment (~1%, w/w loading). Rapid solvent removal using vacuum dramatically increased drug entrapment (~38%, w/w loading; 76% encapsulation efficiency). Microparticles sustained curcumin release over 4 weeks in vitro, and drug release rate could be modulated by varying the polymer molecular weight and/or composition. A single subcutaneous dose of microparticles sustained curcumin liver concentration for nearly a month in mice. Hepatic glutathione-s-transferase and cyclooxygenase-2 activities, biomarkers for chemoprevention, were altered following treatment with curcumin microparticles. The results of these studies suggest that sustained-release microparticles of curcumin could be a novel and effective approach for cancer chemoprevention.
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