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

Abstract

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.

Recent Advances in Photo-Crosslinkable Hydrogels for Biomedical Applications

“…UV-crosslinked PEGDA hydrogel was made into pharmaceutical tablets using 3D inkjet printing to control the release of ropinorole hydrochloride, a drug used for the treatment of Parkinson's disease [38]. It has also been made into microneedles using a micromolding approach to deliver gap junction inhibitor (Gap 26) for repair of keloid scars via the transdermal route [40] (Figure 2A). In addition, PEGDA hydrogel can be used as an implant to control a sustained release of stromal cell-derived factor 1/glycoprotein VI, which promotes migration and engraftment of bone marrow-derived stem cells at the ischemic region of cardiovascular tissues for angiogenesis and cardiac regeneration [35].…”

“… (A) Microneedle-based drug delivery for treatment of skin disease; adapted with permission from [40]. (B) Bone regeneration; adapted with permission from [41].…”

4D Printing of a Bioinspired Microneedle Array with Backward‐Facing Barbs for Enhanced Tissue Adhesion

“…The bare polymeric base sample, i.e., the flat and square polymeric substrate without MNs, was used as control to take RhoB loaded in/released from the base of the MN array into account. Notice that the barbs in MNs were designed to provide a more robust tissue interlock during prolonged insertion in skin, so that the loading/release mechanism of barbed MNs is analogous to other barbless polymeric MNs reported in the literature …”

Polymeric Microneedle Arrays: Versatile Tools for an Innovative Approach to Drug Administration

“…Coated (33) Dissolving (34), (35), (37), (43) Swelling (35) Hollow (36) In vivo (mouse) In vitro [33,[35][36][37]43] [ 34] Nausea and vomiting Swelling In vivo [38] Obesity Dissolving In vivo (mouse) [40,41] Keloid scar Swelling Ex vivo [42] Vitamin K deficiency Dissolving In vitro [44] have been loaded into MNs and effectively administered both in vitro and in vivo. [42][43][44] The spectrum of substances proven to be compatible with MN technology is wide.…”