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介孔硅纳米颗粒用于口服药物传递的评价- MSNs 药物载体的现状和展望。

Evaluation of mesoporous silica nanoparticles for oral drug delivery - current status and perspective of MSNs drug carriers.

机构信息

Department of Inorganic Chemistry - Functional Materials, Faculty of Chemistry, University of Vienna, Währinger Str. 42, 1090 Vienna, Austria.

出版信息

Nanoscale. 2017 Oct 19;9(40):15252-15277. doi: 10.1039/c7nr05762h.

Abstract

The oral pathway is considered as the most common method for drug administration, although many drugs, especially the highly pH- and/or enzymatic biodegradable peptide drugs, are very difficult to formulate and achieve a good intestinal absorption. Efficient systematic absorption of an active substance, delivered via oral ingestion, is only achievable if the drug (1) is substantially present as a solution in the gastrointestinal tract, (2) is able to penetrate through the intestinal mucus, (3) overcomes the different gastrointestinal barriers, and (4) provides an effective therapeutic dose. Therefore, optimization of oral bioavailability of poorly-soluble drugs still remains a significant challenge for the pharmaceutical industry. Even though numerous conventional drug carriers have successfully solved some of the issues related to oral delivery of poorly-soluble drugs, only few of them met commercialization requirements. These drawbacks have led the scientific world to reconsider its approaches toward targeted drug delivery systems and researchers started looking for alternative vectorized carriers. In this area, nanoparticle-based materials have several significant advantages over free and non-formulated drugs. For example, nanosized porous silica carriers allow for more sustained and controlled drug release or improved oral bioavailability. Thus, in the present review, we will highlight the most important features of nanostructured silica drug carriers, such as particle size, particle shape, surface roughness or surface functionalization, and underline the key advantages of these nanosupports. In particular, this article will discuss recent progress and challenges in the area of mesoporous silica nanocarriers used for oral drug delivery. Additional emphasis will be set on the biological and chemical features of the gastrointestinal tract as well as currently tested nanoformulations and strategies to avoid drug degradation in the gastrointestinal environment.

摘要

口服途径被认为是给药的最常见方法,尽管许多药物,尤其是高度 pH 值和/或酶可生物降解的肽类药物,非常难以制剂化并实现良好的肠道吸收。通过口服摄入的活性物质的有效系统吸收,只有在药物(1)在胃肠道中基本上以溶液形式存在,(2)能够穿透肠粘液,(3)克服不同的胃肠道屏障,并且(4)提供有效的治疗剂量时才可行。因此,优化难溶性药物的口服生物利用度仍然是制药行业面临的重大挑战。尽管许多传统药物载体已成功解决了一些与难溶性药物口服递送相关的问题,但只有少数符合商业化要求。这些缺点促使科学界重新考虑其靶向药物递送系统的方法,研究人员开始寻找替代载体化载体。在这一领域,纳米颗粒基材料在靶向药物递送系统中具有几个显著的优势。例如,纳米多孔硅载体允许更持续和受控的药物释放或改善口服生物利用度。因此,在本综述中,我们将重点介绍纳米结构硅药物载体的一些重要特征,例如粒径、颗粒形状、表面粗糙度或表面功能化,并强调这些纳米载体的关键优势。特别是,本文将讨论用于口服药物递送的介孔硅纳米载体的最新进展和挑战。此外,还将重点介绍胃肠道的生物学和化学特征,以及目前测试的纳米制剂和在胃肠道环境中避免药物降解的策略。

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