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首页> 外文期刊>Journal of pharmaceutical sciences. >Modulating beta-lapachone release from polymer millirods through cyclodextrin complexation.
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Modulating beta-lapachone release from polymer millirods through cyclodextrin complexation.

机译：通过环糊精络合调节聚合物毫摩尔中β-拉帕酮的释放。

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Beta-lapachone (beta-lap) is a novel anticancer agent that kills tumors overexpressing the NADPH: quinone oxidoreductase enzyme. However, poor aqueous solubility and low bioavailability hinder its therapeutic applications. Herein we describe the development of poly(D,L-lactide-co-glycolide) (PLGA) polymer millirods for local delivery of beta-lap. The objective was to investigate the use of beta-lap inclusion complexes with cyclodextrins (CDs) to control beta-lap release kinetics from PLGA millirods. Differential scanning calorimetry was performed to measure drug/polymer interactions, complexation efficiency with different CDs, and complex/polymer interactions. beta-Lap was found to have a solid-state solubility of 13% in PLGA. beta-Lap dissolution in PLGA matrix lowered the glass transition temperature of PLGA from 44 to 31 degrees C, and led to a slow release of beta-lap (8.8+/-1.2% release after 22 days). For beta-lap and CD interactions, increasing complexation efficiency was observed in the order of alpha-CD, gamma-CD, and beta-CD. beta-Lap complexation with hydroxypropyl-beta-cyclodextrin (HPbeta-CD) prevented drug dissolution in PLGA, and led to fast release (79.6+/-2.1% after 2 days). Sustained drug release was achieved when beta-lap was complexed with alpha-CD or gamma-CD. These data demonstrate the ability to tailor beta-lap release kinetics via CD complexation, providing exciting opportunities for the use of beta-lap-millirods for intratumoral drug delivery. Association
机译：Beta-lapachone（beta-lap）是一种新型抗癌药，可以杀死过度表达NADPH的肿瘤：醌氧化还原酶。但是，水溶性差和生物利用度低阻碍了其治疗应用。在这里，我们描述了聚（D，L-丙交酯-共-乙交酯）（PLGA）聚合物毫摩尔的开发，用于局部递送β-lap。目的是研究将β-lap包合物与环糊精（CDs）结合使用，以控制PLGA Millirods的β-lap释放动力学。进行差示扫描量热法以测量药物/聚合物相互作用，与不同CD的络合效率以及络合物/聚合物相互作用。发现β-Lap在PLGA中的固态溶解度为13％。 β-Lap在PLGA基质中的溶解将PLGA的玻璃化转变温度从44降低到31摄氏度，并导致β-lap的缓慢释放（22天后释放8.8 +/- 1.2％）。对于β-lap和CD相互作用，观察到络合效率以α-CD，γ-CD和β-CD的顺序增加。 β-Lap与羟丙基-β-环糊精（HPbeta-CD）络合可防止药物在PLGA中溶解，并导致快速释放（2天后为79.6 +/- 2.1％）。当β-lap与α-CD或γ-CD复合时，药物释放得以持续。这些数据证明了通过CD络合调节β-lap释放动力学的能力，为使用β-lap-millirods进行肿瘤内药物递送提供了令人兴奋的机会。协会

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