可生物降解的自组装 PEG-PCL-PEG 胶束用于递送疏水性厚朴酚:I. 制备与表征。
Biodegradable self-assembled PEG-PCL-PEG micelles for hydrophobic honokiol delivery: I. Preparation and characterization.
机构信息
State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, and School of Life Sciences, Sichuan University, Chengdu, 610041, People's Republic of China.
出版信息
Nanotechnology. 2010 May 28;21(21):215103. doi: 10.1088/0957-4484/21/21/215103. Epub 2010 Apr 30.
This study aims to develop self-assembled poly(ethylene glycol)-poly(epsilon-caprolactone)-poly(ethylene glycol) (PEG-PCL-PEG, PECE) micelles to encapsulate hydrophobic honokiol (HK) in order to overcome its poor water solubility and to meet the requirement of intravenous administration. Honokiol loaded micelles (HK-micelles) were prepared by self-assembly of PECE copolymer in aqueous solution, triggered by its amphiphilic characteristic assisted by ultrasonication without any organic solvents, surfactants and vigorous stirring. The particle size of the prepared HK-micelles measured by Malvern laser particle size analyzer were 58 nm, which is small enough to be a candidate for an intravenous drug delivery system. Furthermore, the HK-micelles could be lyophilized into powder without any adjuvant, and the re-dissolved HK-micelles are stable and homogeneous with particle size about 61 nm. Furthermore, the in vitro release profile showed a significant difference between the rapid release of free HK and the much slower and sustained release of HK-micelles. Moreover, the cytotoxicity results of blank micelles and HK-micelles showed that the PECE micelle was a safe carrier and the encapsulated HK retained its potent antitumor effect. In short, the HK-micelles were successfully prepared by an improved method and might be promising carriers for intravenous delivery of HK in cancer chemotherapy, being effective, stable, safe (organic solvent and surfactant free), and easy to produce and scale up.
本研究旨在制备自组装的聚乙二醇-聚己内酯-聚乙二醇(PEG-PCL-PEG,PECE)胶束,以包封疏水性厚朴酚(HK),从而克服其水溶性差的问题,并满足静脉给药的要求。通过其两亲特性在超声辅助下自组装在水溶液中制备负载有厚朴酚的胶束(HK-胶束),无需有机溶剂、表面活性剂和剧烈搅拌。通过马尔文激光粒度分析仪测量的所制备的 HK-胶束的粒径为 58nm,小到足以成为静脉给药系统的候选物。此外,HK-胶束可以在没有任何赋形剂的情况下冻干成粉末,并且重新溶解的 HK-胶束是稳定且均匀的,粒径约为 61nm。此外,体外释放曲线表明游离 HK 的快速释放与 HK-胶束的缓慢和持续释放之间存在显著差异。此外,空白胶束和 HK-胶束的细胞毒性结果表明,PECE 胶束是一种安全的载体,包封的 HK 保留了其有效的抗肿瘤作用。总之,通过改进的方法成功制备了 HK-胶束,可能成为癌症化疗中 HK 静脉给药的有前途的载体,具有高效、稳定、安全(无有机溶剂和表面活性剂)、易于生产和放大的特点。