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用于生物制剂鼻内递送的先进制剂。

Advanced formulations for intranasal delivery of biologics.

机构信息

Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck, Innrain 80/82, Innsbruck, Austria.

Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck, Innrain 80/82, Innsbruck, Austria.

出版信息

Int J Pharm. 2018 Dec 20;553(1-2):8-20. doi: 10.1016/j.ijpharm.2018.10.029. Epub 2018 Oct 11.

Abstract

INTRODUCTION

The global biologics market has been ever increasing over the last decades and is predicted to top Euro 350 by 2020. Facing this scenario, the parenteral route of biologics administration as hitherto standard route is inconvenient for the future. Among the alternatives, the intranasal delivery of therapeutic biologicals seems to be most promising but researchers are still facing challenges as indicated by the scarce number of successfully marketed peptide drugs.

AREAS COVERED

This review article is a compilation of current research focusing on achievements in the field of auxiliary agents for biologics delivery. First, the key benefits of the nose as most promising alternative route of drug administration are highlighted. Then, the potential of the different auxiliary agents in preclinical research is in detail discussed. Moreover, the most used permeation enhancing agents, mucolytic agents, mucoadhesive agents, in situ gelling agents and enzyme inhibiting agents in the formulation of nasal drug delivery systems are described. Thus, the overall purpose of this review is to highlight recent achievements in nasal delivery of biologics and to encourage researchers to work in the direction of needle-free nasal administration of biologics.

EXPERT OPINION

The nasal epithelium is a promising route for biologics administration, which is reflected in a number of well-established products on the market treating chronic diseases as well as a large number of clinical trials currently in progress. The nasal route of drug administration might be a chance to improve therapy of biologics however break-through advances, especially for very complex molecules, such as antibodies, are still needed.

摘要

简介

在过去的几十年里,全球生物制品市场一直在不断增长,预计到 2020 年将超过 3500 亿欧元。面对这种情况,生物制品的注射给药途径作为目前的标准途径,在未来将变得不方便。在替代途径中,鼻内给药似乎是最有前途的,但正如成功上市的肽类药物数量稀少所表明的那样,研究人员仍然面临挑战。

涵盖领域

本文综述了目前专注于生物制品给药辅助剂研究领域的最新研究成果。首先,强调了鼻腔作为最有前途的替代药物给药途径的关键优势。然后,详细讨论了不同辅助剂在临床前研究中的潜力。此外,还描述了在鼻内给药系统的制剂中最常用的渗透增强剂、黏液溶解剂、黏膜黏附剂、原位凝胶形成剂和酶抑制剂。因此,本文的总体目的是强调生物制品鼻内给药的最新进展,并鼓励研究人员朝着无针鼻内给予生物制品的方向努力。

专家意见

鼻上皮是生物制品给药的一个很有前途的途径,这反映在市场上有许多成熟的治疗慢性疾病的产品,以及目前正在进行的大量临床试验。药物的鼻腔给药途径可能是改善生物制品治疗效果的一个机会,但是,特别是对于非常复杂的分子,如抗体,仍需要突破性进展。

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