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I-Corps: Monodisperse Polyethylene Glycol Synthesis Technologies

I-Corps：单分散聚乙二醇合成技术

基本信息

批准号：
1754235
负责人：
Shiyue Fang
金额：
$ 5万
依托单位：
Michigan Technological University
依托单位国家：
美国
项目类别：
Standard Grant
财政年份：
2017
资助国家：
美国
起止时间：
2017-11-01 至 2019-04-30
项目状态：
已结题

来源：
https://www.nsf.gov/awardsearch/showAward?AWD_ID=1754235&HistoricalAwards=false
关键词：
Corps Monodisperse Polyethylene Glycol Synthesis

项目摘要

The broader impact/commercial potential of this I-Corps project includes the commercial availability of affordable monodisperse short and long polyethylene glycols (PEGs). Areas that will benefit from their commercialization include organic synthesis, bioconjugation, nanotechnology, pharmaceutical chemistry and more. Currently, monodisperse short PEGs can be prohibitively expensive. Many scientists have to devote significant time to synthesize them or have to use less ideal alternative materials. More seriously, there is no technology to synthesize monodisperse long PEGs and scientists in the pharmaceutical industry often use impure PEGs for drug PEGylation (i.e. tagging with PEG). Commercialization of affordable monodisperse PEGs and their derivatives may transform the ways researchers and manufacturers conduct their projects.This I-Corps project explores the market potential of novel technologies that can be used to synthesize polyethylene glycols (PEG) and derivatives in monodisperse form and with much lower costs. Short PEGs are widely used as linkers in areas including organic synthesis, and pharmaceutical chemistry. Long PEGs are used for PEGylating pharmaceuticals to increase water solubility and bio-stability, and to reduce undesirable immune responses and dosing frequency. Currently monodisperse short PEGs can be synthesized via stepwise organic synthesis. However, the process requires chromatography to purify intermediates and product, which consumes large volumes of solvents and silica gel. The waste to product ratio can be over 1000 to 1. For long PEGs, they are made by random polymerization, and there is no technology to make them monodisperse. Therefore, impure PEGs are often used for drug PEGylation. To overcome the challenges in monodisperse PEG production, novel technologies based on solid phase stepwise synthesis will be developed.

该I-Corps项目更广泛的影响/商业潜力包括可负担得起的单分散短和长聚乙二醇（PEG）的商业可用性。将从其商业化中受益的领域包括有机合成，生物共轭，纳米技术，药物化学等。目前，单分散短PEG可能过于昂贵。许多科学家不得不投入大量时间来合成它们，或者不得不使用不太理想的替代材料。更严重的是，没有合成单分散长PEG的技术，制药工业中的科学家经常使用不纯的PEG进行药物PEG化（即用PEG标记）。经济实惠的单分散聚乙二醇及其衍生物的商业化可能会改变研究人员和制造商开展项目的方式。I-Corps项目探索了可用于以低得多的成本合成单分散形式的聚乙二醇（PEG）及其衍生物的新技术的市场潜力。短聚乙二醇广泛用作有机合成和药物化学等领域的连接剂。长PEG用于PEG化药物以增加水溶性和生物稳定性，并减少不期望的免疫应答和给药频率。目前，单分散短PEG可以通过逐步有机合成来合成。然而，该方法需要色谱法来纯化中间体和产物，这消耗了大量的溶剂和硅胶。废物与产品的比例可以超过1000比1。对于长PEG，它们是通过无规聚合制备的，并且没有使它们单分散的技术。因此，不纯的PEG通常用于药物PEG化。为了克服单分散PEG生产中的挑战，将开发基于固相逐步合成的新技术。