Enhanced delivery of hydrophilic peptides in vitro by transdermal microneedle pretreatment

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.

Modelling drug flux through microporated skin

“…To assess the validity of the new model, it was used to predict published experimental results [16][17][18][19][20][21] for a variety of drugs permeating across mammalian skin that had been fully porated either using microneedles or by laser ablation; the measured values were also compared to estimates from the intuitive model and the results are presented in Tables 1 and 2. For laser-porated skin, the pore diameter was reported; in the case of microneedle poration, the pore radius (r p ) was calculated from geometric considerations:…”

Peptide Hydrolysates from Astragalus membranaceus Bunge Inhibit the Expression of Matrix Metalloproteinases in Human Dermal Fibroblasts

“…The skin permeation of peptides increases as their molecular weight decreases [21]. In this experiment, we investigated the mass of AMPs separated on portion 5 of 40% polyacrylamide gel and found that it was < 1500 Da (Fig.…”

Controlled Drug Delivery Using Microdevices

“…Zhang et al . studied the use of solid microneedle arrays (SMNA) (150 μm in length) in transdermal peptide delivery and examined the relationship between peptide permeation rates and D 2 O flux [74]. The influence of MN pre-treatment on skin permeation was evaluated using porcine ear skin with Franze diffusion cell.…”