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辅酶Q10的口服递送和线粒体靶向策略。

Strategies for oral delivery and mitochondrial targeting of CoQ10.

作者信息

Zaki Noha M

机构信息

a Toronto Health Economics and Technology Assessment (THETA) Collaborative Leslie Dan Faculty of Pharmacy, University of Toronto , Toronto , Ontario , Canada.

出版信息

Drug Deliv. 2016 Jul;23(6):1868-81. doi: 10.3109/10717544.2014.993747. Epub 2014 Dec 29.

Abstract

Coenzyme Q10 (CoQ10), also known as ubiquinone or ubidecarenone, is a powerful, endogenously produced, intracellularly existing lipophilic antioxidant. It combats reactive oxygen species (ROS) known to be responsible for a variety of human pathological conditions. Its target site is the inner mitochondrial membrane (IMM) of each cell. In case of deficiency and/or aging, CoQ10 oral supplementation is warranted. However, CoQ10 has low oral bioavailability due to its lipophilic nature, large molecular weight, regional differences in its gastrointestinal permeability and involvement of multitransporters. Intracellular delivery and mitochondrial target ability issues pose additional hurdles. To maximize CoQ10 delivery to its biopharmaceutical target, numerous approaches have been undertaken. The review summaries the current research on CoQ10 bioavailability and highlights the headways to obtain a satisfactory intracellular and targeted mitochondrial delivery. Unresolved questions and research gaps were identified to bring this promising natural product to the forefront of therapeutic agents for treatment of different pathologies.

摘要

辅酶Q10(CoQ10),也称为泛醌或癸烯醌,是一种强大的、内源性产生的、存在于细胞内的亲脂性抗氧化剂。它能对抗已知会导致多种人类病理状况的活性氧(ROS)。其作用靶点是每个细胞的线粒体内膜(IMM)。在缺乏和/或衰老的情况下,有必要口服补充CoQ10。然而,由于CoQ10的亲脂性、大分子质量、胃肠道通透性的区域差异以及多种转运体的参与,其口服生物利用度较低。细胞内递送和线粒体靶向能力问题带来了额外的障碍。为了使CoQ10最大程度地递送至其生物制药靶点,人们采取了多种方法。本综述总结了目前关于CoQ10生物利用度的研究,并强调了在实现令人满意的细胞内和靶向线粒体递送方面取得的进展。识别出未解决的问题和研究空白,以便将这种有前景的天然产物推向治疗不同病症的治疗药物前沿。

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