粒度对药物在人体各部位生物利用度的影响

Zi Hong Mok
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引用次数: 0

摘要

药物递送的有效性涉及多种机制。药物颗粒大小是挑战之一,因为颗粒需要从外部环境输送到血液循环或组织间液中,并通过细胞膜被细胞内化。小颗粒可能更容易被内化,但不易保留,因为它们会被快速清除。大颗粒不容易穿过生物屏障,但其大小分布更容易控制。由于给药途径多种多样,这些微粒的大小范围也需要考虑到所涉及的解剖、生物和动态屏障。本综述希望能让人们深入了解为通过人体各种给药途径(如穿过胃肠道上皮、肺部、皮肤、血脑屏障、肾脏和肝脏、眼、鼻、耳、癌症肿瘤基质以及肌肉)给药而设计的颗粒尺寸范围。虽然成功的药物递送也取决于递送系统的材料特性以及生物/纳米界面的相关特性,但本综述的重点是粒度对提高体内各器官生物利用度的重要性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
The effect of particle size on drug bioavailability in various parts of the body

Multiple mechanisms are involved in driving the efficacy of drug delivery. Drug particle size is one of the challenges as particles need to be delivered from the external environment, into the circulation or interstitial fluid and transiting the cell membranes for cellular internalisation. Small particles are presumably easier to be internalised, yet they are not easy to retain as they are subject to fast clearance. Big particles do not cross biological barriers as easily, but their size distribution is easier to be controlled. Because of the various routes of administration, the size range of these particles will also need to be catered for the anatomical, biological, and dynamic barriers involved. This review hopes to provide an insight into the range of particle size that has been engineered for drug delivery via various routes of administration of the body, such as to cross the epithelium of gastrointestinal tract, lungs, skin, blood-brain barrier, kidney and liver, the eye, nose, and ear, the cancer tumour matrix and into the muscles. While successful drug delivery also depends on the material properties of the delivery systems and the bio/nano interface related properties, this review focuses on the importance of particle size for enhancing bioavailability at the various organs of the body.

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