Chemical Process Engineering Research Institute, Centre for Research and Technology Hellas, P.O. Box 60361, 57001 Thessaloniki, Greece.
J Control Release. 2012 Aug 10;161(3):781-94. doi: 10.1016/j.jconrel.2012.05.040. Epub 2012 May 29.
This review highlights the recent developments in the area of nanocarrier-based mucosal delivery of therapeutic biomolecules and antigens. Macromolecular drugs have the unique power to tackle challenging diseases but their structure, physicochemical properties, stability, pharmacodynamics, and pharmacokinetics place stringent demands on the way they are delivered into the body (e.g., inability to cross mucosal surfaces and biological membranes). Carrier-based drug delivery systems can diminish the toxicity of therapeutic biomolecules, improve their bioavailability and make possible their administration via less-invasive routes (e.g., oral, nasal, pulmonary, etc.). Thus, the development of functionalized nanocarriers and nanoparticle-based microcarriers for the delivery of macromolecular drugs is considered an important scientific challenge and at the same time a business breakthrough for the biopharmaceutical industry. In order to be translated to the clinic the nanocarriers need to be biocompatible, biodegradable, stable in biological media, non-toxic and non-immunogenic, to exhibit mucoadhesive properties, to cross mucosal barriers and to protect their sensitive payload and deliver it to its target site in a controlled manner, thus increasing significantly its bioavailability and efficacy.
本综述重点介绍了基于纳米载体的治疗性生物分子和抗原黏膜递药领域的最新进展。大分子药物具有攻克挑战性疾病的独特能力，但它们的结构、物理化学性质、稳定性、药效学和药代动力学对其进入体内的输送方式提出了严格的要求（例如，无法穿过黏膜表面和生物膜）。基于载体的药物输送系统可以降低治疗性生物分子的毒性，提高其生物利用度，并使它们能够通过侵袭性较小的途径（例如口服、鼻内、肺部等）给药。因此，开发用于输送大分子药物的功能化纳米载体和基于纳米颗粒的微粒载体被认为是一个重要的科学挑战，同时也是生物制药行业的商业突破。为了将纳米载体转化为临床应用，它们需要具有生物相容性、可生物降解性、在生物介质中稳定、无毒性和免疫原性，表现出黏膜黏附特性，能够穿越黏膜屏障，并以可控的方式保护其敏感的有效载荷并将其递送至靶部位，从而显著提高其生物利用度和疗效。
