可生物降解的两亲性肽水凝胶作为阿片肽的延长释放系统。
Biodegradable Amphipathic Peptide Hydrogels as Extended-Release System for Opioid Peptides.
机构信息
Research Group of Organic Chemistry , Vrije Universiteit Brussel , Pleinlaan 2 , Brussels B-1050 , Belgium.
Department of Pharmaceutical Chemistry, Institute of Pharmacy and Center for Molecular Biosciences (CMBI) , University of Innsbruck , Innrain 80-82 , 6020 Innsbruck , Austria.
出版信息
J Med Chem. 2018 Nov 8;61(21):9784-9789. doi: 10.1021/acs.jmedchem.8b01282. Epub 2018 Oct 26.
Chronic pain is currently treated with opioids that offer unsatisfactory long-term analgesia and produce serious side effects. There is a clear need for alternative therapies. Herein, peptide-based hydrogels are used as extended-release drug delivery carriers. Two different formulations were developed: the drug is coformulated within the hydrogel; the drug is an integral part of the hydrogelator. Both strategies afford a prolonged and significant antinociception up to 72 h after subcutaneous administration in mice.
慢性疼痛目前采用阿片类药物治疗，但长期镇痛效果不理想，并产生严重的副作用。显然需要替代疗法。在此，我们使用基于肽的水凝胶作为长效药物递送载体。开发了两种不同的制剂：药物共混在水凝胶中；药物是水凝胶形成剂的组成部分。这两种策略都能在小鼠皮下给药后长达 72 小时提供持续且显著的镇痛作用。
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