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Peptide delivery with poly(ethylene glycol) diacrylate microneedles through swelling effect

机译:聚乙二醇二丙烯酸酯微针通过溶胀作用输送肽

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摘要

Transdermal delivery of therapeutic biomolecules (including peptides) can avoid enzymatic digestion that occurs in the oral route. (Polyethylene glycol) diacrylate (PEGDA)‐based microneedles, with good biocompatibility, are easily fabricated through photo‐polymerization with a precisely controlled structure. It has successfully been used for the transdermal delivery of small molecule drugs such as 5‐fluorouracil. However, the delivery of peptide‐based therapeutics using this platform is seldom reported. This is because of the potential damage to the peptide during the photo‐polymerization process of PEGDA. Herein, we introduce a method to load PEGDA microneedles with peptides without compromising peptide potency. Using gap junction inhibitor (Gap 26) as an example, the peptide was loaded into PEGDA microneedles through the swelling effect of PEGDA in the aqueous solution. The peptide‐loaded microneedles were applied to a keloid scar model and exhibited inhibition expression of collagen I, a predominant marker of keloid scar, demonstrating its potential therapeutic effects.
机译:治疗性生物分子(包括肽)的透皮递送可避免口服途径发生酶消化。 (聚乙二醇)二丙烯酸酯(PEGDA)基的微针具有良好的生物相容性,可通过具有精确控制结构的光聚合反应轻松制造。它已成功用于小分子药物(例如5-氟尿嘧啶)的透皮递送。但是,很少有报道使用该平台提供基于肽的治疗剂。这是因为在PEGDA的光聚合过程中可能会对肽造成损害。在这里,我们介绍了一种在不影响肽效价的情况下用肽加载PEGDA微针的方法。以间隙连接抑制剂(Gap 26)为例,通过PEGDA在水溶液中的溶胀作用将肽加载到PEGDA微针中。将载有肽的微针应用于瘢痕loid疤痕模型,并显示胶原I(瘢痕loid疤痕的主要标志物)的抑制表达,证明了其潜在的治疗效果。

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