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胶束导向的聚吡咯颗粒化学聚合用于电触发释放地塞米松碱和地塞米松磷酸酯。

Micelle directed chemical polymerization of polypyrrole particles for the electrically triggered release of dexamethasone base and dexamethasone phosphate.

机构信息

School of Pharmacy, Faculty of Medical and Health Sciences, University of Auckland, Auckland, New Zealand.

Buchanan Ocular Therapeutics Unit, Department of Ophthalmology, New Zealand National Eye Centre, University of Auckland, Auckland, New Zealand.

出版信息

Int J Pharm. 2018 May 30;543(1-2):38-45. doi: 10.1016/j.ijpharm.2018.03.039. Epub 2018 Mar 23.

Abstract

Conducting polymers such as polypyrrole (PPy) can be used as electrically responsive drug delivery systems typically prepared by electrochemical polymerisation, however, the amount of drug that can be delivered is typically low. To increase drug delivery capacity and prepare larger amounts of polymer, PPy nanoparticles were produced by chemical polymerisation over drug-loaded micelles. Two forms of dexamethasone were included to increase total drug loading and to explore the mechanisms of loading and release. The particles produced were approximately 50 nm in size and their conductivity and reversible redox activity were demonstrated. Loading of the hydrophobic dexamethasone base was more efficient than for the more hydrophilic phosphate salt. After pressing the particles into the desired form, electrically-responsive drug release was achieved with a pulsed potential signal being the most effective way to trigger release. Notably, the anionic phosphate salt of the drug was more sensitive to electrically stimulated release than the uncharged base of dexamethasone, highlighting the role of electrostatic forces in driving drug release. This system has potential to be loaded with different drugs widening the scope of application of these smart particles to treat a range of disease states.

摘要

导电聚合物如聚吡咯(PPy)可用作电响应药物输送系统,通常通过电化学聚合来制备,但是输送的药物量通常较低。为了增加药物输送能力并制备更多数量的聚合物,通过载药胶束上的化学聚合制备了 PPy 纳米颗粒。加入了两种形式的地塞米松以增加总药物负载并探索负载和释放的机制。所制备的颗粒大小约为 50nm,其电导率和可逆氧化还原活性得到了证明。疏水性地塞米松碱的负载比亲水性磷酸盐盐更有效。将颗粒压制成所需形状后,通过施加脉冲电势信号实现了电响应药物释放,这是触发释放的最有效方法。值得注意的是,药物的阴离子磷酸盐盐比地塞米松的无电荷碱更敏感于电刺激释放,这突出了静电在驱动药物释放中的作用。该系统具有负载不同药物的潜力,从而拓宽了这些智能颗粒在治疗多种疾病状态方面的应用范围。

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