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

Zhang S, Qiu Y, Gao Y - Acta Pharm Sin B (2014)

Bottom Line: 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]).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.

View Article: PubMed Central - PubMed

Affiliation: Lab of Organic Optoelectronic Functional Materials and Molecular Engineering, Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Beijing 100190, China.

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.

No MeSH data available.


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Relationship between the permeation rate of five model peptides and their corresponding molecular weight.
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f0025: Relationship between the permeation rate of five model peptides and their corresponding molecular weight.

Mentions: Fig. 4 shows the cumulative amount of these peptides after application of the microneedles during 24 h. Besides the dipeptides studied here, transport for l-carnitine (161.2 Da) was also studied. The permeation rates of l-carnitine, tetrapeptide-3, hexapeptide, acetyl hexapeptide-3 and oxytocin were 1.95±0.21, 0.90±0.09, 0.84±0.11, 0.42±0.14, 0.16±0.05 μmoL/cm·h, respectively. Fig. 5 shows an inverse relationship between permeability and molecular weight of the peptides.


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

Zhang S, Qiu Y, Gao Y - Acta Pharm Sin B (2014)

Relationship between the permeation rate of five model peptides and their corresponding molecular weight.
© Copyright Policy - CC BY-NC-ND
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4590292&req=5

f0025: Relationship between the permeation rate of five model peptides and their corresponding molecular weight.
Mentions: Fig. 4 shows the cumulative amount of these peptides after application of the microneedles during 24 h. Besides the dipeptides studied here, transport for l-carnitine (161.2 Da) was also studied. The permeation rates of l-carnitine, tetrapeptide-3, hexapeptide, acetyl hexapeptide-3 and oxytocin were 1.95±0.21, 0.90±0.09, 0.84±0.11, 0.42±0.14, 0.16±0.05 μmoL/cm·h, respectively. Fig. 5 shows an inverse relationship between permeability and molecular weight of the peptides.

Bottom Line: 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]).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.

View Article: PubMed Central - PubMed

Affiliation: Lab of Organic Optoelectronic Functional Materials and Molecular Engineering, Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Beijing 100190, China.

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.

No MeSH data available.


Related in: MedlinePlus