Drug release characteristics of unimolecular polymeric micelles

Drug release characteristics of unimolecular polymeric micelles
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DOI:
10.1016/s0168-3659(00)00247-9
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发表时间:
2000-08-10
影响因子:
10.8
通讯作者:
Uhrich, K
Uhrich, K
中科院分区:
医学1区
文献类型:
--
作者:
Liu, HB;Farrell, S;Uhrich, K

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可生物降解的单分子聚合物胶束具有几个吸引药物输送应用的特征:热力学稳定性、包裹和增溶疏水客体分子的能力、生物降解性以及防止RE快速清除的尺寸和表面特征。在这里,我们研究了这些单分子聚合物胶束在较长时间内释放药物的可能性。利多卡因被用作体外研究的模型药物,使用水平扩散池和纤维素膜阻止聚合物从来源传输到接收器隔室。在汇条件下,游离利多卡因从来源到接收者的传输是零级的,在8小时内完成。最初包裹在聚合物中的利多卡因的传输在前14小时是零级的,在24小时内检测到96%的利多卡因。(C)2000爱思唯尔科学公司版权所有。
Biodegradable, unimolecular polymeric micelles possess several features that are attractive for drug delivery applications: Thermodynamic stability, ability to encapsulate and solubilize a hydrophobic guest molecule, biodegradability, as well as size and surface characteristics that prevent rapid clearance by the RES. Here we investigate the potential of these unimolecular polymeric micelles to release a drug for an extended time. Lidocaine was used as a model drug for in vitro studies using a horizontal diffusion cell and cellulose membrane that prevented polymer transport from the source to the receiver compartment. The transport of free lidocaine from source to receiver under sink conditions was zero-order and complete within 8 h. The transport of lidocaine initially encapsulated in polymer was zero-order for the first 14 h, and 96% of the lidocaine was detected within 24 h. (C) 2000 Elsevier Science B.V. All rights reserved.