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利用药物传递系统将药物递送至细胞内细胞器:研究趋势与靶向效率分析。

Delivery of drugs to intracellular organelles using drug delivery systems: Analysis of research trends and targeting efficiencies.

机构信息

Department of Clinical Biochemistry and Pharmacology, The Faculty of Health Sciences, Ben-Gurion University of the Negev, Beer Sheva, Israel.

Department of Clinical Biochemistry and Pharmacology, The Faculty of Health Sciences, Ben-Gurion University of the Negev, Beer Sheva, Israel.

出版信息

Int J Pharm. 2015 Dec 30;496(2):268-74. doi: 10.1016/j.ijpharm.2015.10.053. Epub 2015 Oct 26.

DOI:10.1016/j.ijpharm.2015.10.053
PMID:26516100
Abstract

Targeting of drug delivery systems (DDSs) to specific intracellular organelles (i.e., subcellular targeting) has been investigated in numerous publications, but targeting efficiency of these systems is seldom reported. We searched scientific publications in the subcellular DDS targeting field and analyzed targeting efficiency and major formulation parameters that affect it. We identified 77 scientific publications that matched the search criteria. In the majority of these studies nanoparticle-based DDSs were applied, while liposomes, quantum dots and conjugates were used less frequently. The nucleus was the most common intracellular target, followed by mitochondrion, endoplasmic reticulum and Golgi apparatus. In 65% of the publications, DDSs surface was decorated with specific targeting residues, but the efficiency of this surface decoration was not analyzed in predominant majority of the studies. Moreover, only 23% of the analyzed publications contained quantitative data on DDSs subcellular targeting efficiency, while the majority of publications reported qualitative results only. From the analysis of publications in the subcellular targeting field, it appears that insufficient efforts are devoted to quantitative analysis of the major formulation parameters and of the DDSs' intracellular fate. Based on these findings, we provide recommendations for future studies in the field of organelle-specific drug delivery and targeting.

摘要

药物递送系统(DDSs)靶向特定的细胞内细胞器(即亚细胞靶向)已在众多出版物中进行了研究,但这些系统的靶向效率很少有报道。我们搜索了亚细胞 DDS 靶向领域的科学出版物,并分析了靶向效率和影响靶向效率的主要制剂参数。我们确定了 77 篇符合搜索标准的科学出版物。在这些研究中,大多数研究应用了基于纳米粒子的 DDSs,而脂质体、量子点和偶联物的应用则较少。细胞核是最常见的细胞内靶标,其次是线粒体、内质网和高尔基体。在 65%的出版物中,DDSs 的表面用特定的靶向残基进行了修饰,但在大多数研究中,并没有对这种表面修饰的效率进行分析。此外,只有 23%的分析性出版物包含 DDS 亚细胞靶向效率的定量数据,而大多数出版物仅报告定性结果。从亚细胞靶向领域的文献分析来看,对于主要制剂参数和 DDS 细胞内命运的定量分析投入的精力不足。基于这些发现,我们为细胞器特异性药物递送和靶向领域的未来研究提供了建议。

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