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      Enhanced delivery of hydrophilic peptides in vitro by transdermal microneedle pretreatment.

      Acta Pharmaceutica Sinica. B
      Elsevier BV
      Transdermal, Peptide, Convective solvent flow, Microneedle

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          Abstract

          The aims of this study were to investigate the utility of solid microneedle arrays (150 µm in length) in enhancing transdermal delivery of peptides and to examine the relationship between peptide permeation rates and D2O flux. Four model peptides were used (Gly-Gln-Pro-Arg [tetrapeptide-3, 456.6 Da], Val-Gly-Val-Ala-Pro-Gly [hexapeptide, 498.6 Da], AC-Glu-Glu-Met-Gln-Arg-Arg-NH2 [acetyl hexapeptide-3, 889 Da] and Cys-Tyr-Ile-Gln-Asn-Cys-Pro-Leu-Gly-NH2 [oxytocin, 1007.2 Da]). The influence of microneedle pretreatment on skin permeation was evaluated using porcine ear skin with Franze diffusion cell. Peptide permeation across the skin was significantly enhanced by microneedle pretreatment, and permeation rates were dependent on peptide molecular weights. A positive correlation between D2O flux and acetyl hexapeptide-3 clearances suggests that convective solvent flow contributes to the enhanced transdermal peptide delivery. It is concluded that solid microneedle arrays are effective devices to enhance skin delivery of peptides.

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          Author and article information

          Journal
          26579370
          4590292
          10.1016/j.apsb.2013.12.011

          Transdermal,Peptide,Convective solvent flow,Microneedle
          Transdermal, Peptide, Convective solvent flow, Microneedle

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