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Study summary · research use only

Efficient transdermal delivery of functional protein cargoes by a hydrophobic peptide MTD 1067

Study · Scientific reports · 2022 · DOI 10.1038/s41598-022-14463-9 · PMID 35760980

Plain-language summary

Paraphrased from the published abstract below — not a verdict on whether anything works.

This study evaluated the hydrophobic cell-penetrating peptide macromolecule transduction domain 1067 (MTD 1067) for transdermal delivery of protein cargoes, including growth hormone-releasing hexapeptide-6 (GHRP-6), a truncated des(1-3)IGF-I, and platelet-derived growth factor BB (PDGF-BB), using skin tissue and confocal microscopy (species not specified). The abstract reports MTD 1067-conjugated cargoes (MTD-GHRP-6 synthesized chemically; MTD-des(1-3)IGF-I and MTD-PDGF-BB as recombinant proteins) showed biological activities identical to or improved compared with the original cargoes, and were detected in the dermis at 4.4-, 18.8-, and 32.9-times higher levels, respectively, than a control group without MTD, without observed cytotoxicity.

Abstract

The skin has a protective barrier against the external environment, making the transdermal delivery of active macromolecules very difficult. Cell-penetrating peptides (CPPs) have been accepted as useful delivery tools owing to their high transduction efficiency and low cytotoxicity. In this study, we evaluated the hydrophobic peptide, macromolecule transduction domain 1067 (MTD 1067) as a CPP for the transdermal delivery of protein cargoes of various sizes, including growth hormone-releasing hexapeptide-6 (GHRP-6), a truncated form of insulin-like growth factor-I (des(1-3)IGF-I), and platelet-derived growth factor BB (PDGF-BB). The MTD 1067-conjugated GHRP-6 (MTD-GHRP-6) was chemically synthesized, whereas the MTD 1067-conjugated des(1-3)IGF-I and PDGF-BB proteins (MTD-des(1-3)IGF-I and MTD-PDGF-BB) were generated as recombinant proteins. All the MTD 1067-conjugated cargoes exhibited biological activities identical or improved when compared to those of the original cargoes. The analysis of confocal microscopy images showed that MTD-GHRP-6, MTD-des(1-3)IGF-I, and MTD-PDGF-BB were detected at 4.4-, 18.8-, and 32.9-times higher levels in the dermis, respectively, compared to the control group without MTD. Furthermore, the MTD 1067-conjugated cargoes did not show cytotoxicity. Altogether, our data demonstrate the potential of MTD 1067 conjugation in developing functional macromolecules for cosmetics and drugs with enhanced transdermal permeability.

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