Wang Su He, Shi Xiangyang, Chen Xisui, Baker James R
Michigan Nanotechnology Institute for Medicine and Biological Sciences, University of Michigan, Ann Arbor, MI48109, USA.
Macromol Biosci. 2009 May 13;9(5):429-36. doi: 10.1002/mabi.200800381.
Development of a novel formulation of anticancer drugs to improve their water-solubility and bioavailability remains a great challenge. Herein, the potential anticancer agent 2-methoxyestradiol (2-ME) was selected as a model drug and was encapsulated within polyelectrolyte (PE) multilayers by layer-by-layer deposition of oppositely charged PEs onto the drug microcrystal surfaces. Cell viability and morphology observation of two cell lines reveal that the PE multilayer-encapsulated 2-ME microcrystals markedly decrease the cell viability, displaying similar inhibitory effect to that of the conventional formulation of 2-ME dissolved in ethanol. The current approach to encapsulate hydrophobic drug microparticles may be useful for formulating different drugs for a variety of biological applications.
开发新型抗癌药物制剂以提高其水溶性和生物利用度仍然是一项巨大挑战。在此,选择潜在的抗癌剂2-甲氧基雌二醇(2-ME)作为模型药物,并通过将带相反电荷的聚电解质(PE)逐层沉积在药物微晶表面上,将其封装在聚电解质(PE)多层膜中。对两种细胞系的细胞活力和形态观察表明,PE多层膜包裹的2-ME微晶显著降低细胞活力,显示出与溶解在乙醇中的2-ME传统制剂相似的抑制作用。目前这种封装疏水性药物微粒的方法可能有助于配制用于各种生物应用的不同药物。