Overview of intranasally delivered peptides: key considerations for pharmaceutical development
Overview of intranasally delivered peptides: key considerations for pharmaceutical development
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DOI：
10.1080/17425247.2018.1517742
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发表时间：
2018-01-01
影响因子：
6.6
通讯作者：
Yang, Zhen
中科院分区：
文献类型：
--
作者：
Al Bakri, Wisam;Donovan, Maureen D.;Yang, Zhen
与其他侵入性全身递送途径相比，鼻内递送肽具有独特的优势。然而，如何评估多肽的鼻腔给药潜力以及鼻制剂开发的关键考虑因素仍然缺乏明确的认识。涵盖领域：进行了鼻内递送肽的回顾性分析。这项工作的目标是1)建立一个关于经鼻途径给药肽的关键物理化学和药代动力学特性的数据库，2)评估适用于IN肽递送系统的配方属性，以及3)提供IN肽递送的关键考虑因素。专家意见/评论：广泛的数据挖掘显示，分子量高达6000Da的肽已被经鼻给药。一些多肽的高溶解度突出了在有限体积内提供足够多肽的可能性，可用于鼻腔喷雾剂。渗透增强剂和黏合剂在改善肽的生物利用度方面显示出了希望。其他制剂的考虑，如制剂的类型，pH值，渗透压，以及药物沉积，在这里进行了审查。基于这一回顾性分析，提出了鼻用肽制剂的关键考虑因素，以指导药物的发现和开发。
Introduction: Intranasal (IN) delivery for peptides provides unique advantages compared to other invasive systemic delivery routes. However, there still lacks a clear understanding on how to evaluate the potential of the peptides for nasal delivery and key considerations for the nasal formulation development.Areas covered: A retrospective analysis of intranasally delivered peptides was conducted. The goals of this undertaking were 1) to build a database of the key physicochemical and pharmacokinetic properties of peptides delivered by the nasal route, 2) to evaluate formulation attributes applied to IN peptide delivery systems, and 3) to provide key considerations for IN delivery of peptides.Expert Opinion/Commentary: Extensive data mining showed that peptides with molecular weights up to 6000Da have been delivered intranasally. The high solubility of some peptides highlighted the possibility of delivering sufficient amounts of peptide in the limited volume available for nasal sprays. Permeation enhancers and mucoadhesives have shown promise in improving the IN bioavailability of peptides. Other formulation considerations, such as the type of formulation, pH, osmolality, as well as drug deposition, are reviewed herein. Based on this retrospective analysis, key considerations for nasal peptides formulations were proposed to guide drug discovery and development for IN delivery of peptides.