Amphiphilic Block Copolymers: A Novel Substance for Bitter-Masking in Aqueous Solutions
Amphiphilic Block Copolymers: A Novel Substance for Bitter-Masking in Aqueous Solutions
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两亲性嵌段共聚物：一种用于水溶液中苦味掩蔽的新型物质
DOI：
10.1021/acs.molpharmaceut.9b01296
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发表时间：
2020-05-04
影响因子：
4.9
通讯作者：
Zhang, Ding-Kun
中科院分区：
文献类型：
--
作者：
Li, Pan;Tian, Yin;Zhang, Ding-Kun
抑制液体制剂的苦味是一项具有挑战性的任务，特别是对于儿童。苦味分子在液体中高度分散，导致对苦味受体的强烈和即时刺激。目前，除了添加甜味剂，还没有有效的方法来纠正这个问题，导致口感不满意。基于公认的苦味形成机理--三点接触理论，首次提出了两亲嵌段共聚物（ABCs）抑制苦味的新思路和应用。我们发现ABC可以广泛抑制四种典型苦味物质的苦味。其机理是ABC自组装形成缔合胶体，其吸引苦味组分并减少其在溶液中以分子形式的分布。苦味成分自动嵌入ABCs疏水链的螺旋疏水空腔中，苦味成分与ABCs的特殊相互作用分散了苦味基团的正静电势。该组合不影响苦味药物的药代动力学参数和药效学。这些发现突出了ABC抑制苦味的新应用，并阐明了潜在的抑制机制。
It is a challenging task to suppress the bitterness of liquid preparations, especially for children. Bitter molecules are highly dispersible in liquids, leading to a strong and instant stimulation of the bitter receptors. At present, there is no effective way to correct this issue except for adding sweeteners, resulting in an unsatisfying taste. Based on the three-point contact theory, which is a universally accepted mechanism of bitterness formation, a new idea and application of amphiphilic block copolymers (ABCs) for bitterness suppression was proposed for the first time. We found that ABCs could widely inhibit the bitterness of four typical bitter substances. The mechanism is that ABCs self-assemble to form association colloids, which attract bitter components and reduce their distribution in the molecular form in solution. The bitter components were demonstrated to automatically embed in the spiral hydrophobic cavity of the hydrophobic chain of the ABCs, and their special interaction dispersed the positive electrostatic potential of bitter groups. The combination did not affect the pharmacokinetic parameters and pharmacodynamics of bitter drugs. These findings highlight the novel application of ABCs for the inhibition of bitterness and illuminate the underlying inhibition mechanisms.