Agrahari Vibhuti, Agrahari Vivek, Mitra Ashim K
Division of Pharmaceutical Sciences, School of Pharmacy, University of Missouri-Kansas City, HSB 5258, 2464 Charlotte St, Kansas City, MO 64108, USA.
Ther Deliv. 2016;7(4):257-78. doi: 10.4155/tde-2015-0012.
Macromolecules (proteins/peptides) have the potential for the development of new therapeutics. Due to their specific mechanism of action, macromolecules can be administered at relatively low doses compared with small-molecule drugs. Unfortunately, the therapeutic potential and clinical application of macromolecules is hampered by various obstacles including their large size, short in vivo half-life, phagocytic clearance, poor membrane permeability and structural instability. These challenges have encouraged researchers to develop novel strategies for effective delivery of macromolecules. In this review, various routes of macromolecule administration (invasive/noninvasive) are discussed. The advantages/limitations of novel delivery systems and the potential role of nanotechnology for the delivery of macromolecules are elaborated. In addition, fabrication approaches to make nanoformulations in different shapes and sizes are also summarized.
大分子（蛋白质/肽）具有开发新型疗法的潜力。由于其特定的作用机制，与小分子药物相比，大分子可以以相对较低的剂量给药。不幸的是，大分子的治疗潜力和临床应用受到各种障碍的阻碍，包括其体积大、体内半衰期短、吞噬清除、膜通透性差和结构不稳定。这些挑战促使研究人员开发有效的大分子递送新策略。在这篇综述中，讨论了大分子给药的各种途径（侵入性/非侵入性）。阐述了新型递送系统的优点/局限性以及纳米技术在大分子递送中的潜在作用。此外，还总结了制备不同形状和尺寸纳米制剂的方法。
