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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 D2O flux and permeation clearance of acetyl hexapeptide-3.
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f0030: Relationship between D2O flux and permeation clearance of acetyl hexapeptide-3.

Mentions: The enhancing effects of ultrasound and iontophoresis on skin permeation of hydrophilic compound can be explained by inducing convective solvent flow13. In the present study, we analyzed how the transport of the hydrophilic compound acetyl hexapeptide-3 was improved by microneedles based on the relationship between hydrophilic solute and vehicle (D2O) transport. To assess the skin permeability of D2O and acetyl hexapeptide-3, the time course of D2O flux and permeation clearance of acetyl hexapeptide-3 under various osmotic concentrations were determined (Fig. 6). A good correlation was observed between the acetyl hexapeptide-3 clearance and the D2O flux (r=0.96, slope of the regression line: 0.23±0.037). The results suggest that convection generated by microneedles plays an important role in skin permeability of hydrophilic drugs.


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

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

Relationship between D2O flux and permeation clearance of acetyl hexapeptide-3.
© Copyright Policy - CC BY-NC-ND
Related In: Results  -  Collection

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

f0030: Relationship between D2O flux and permeation clearance of acetyl hexapeptide-3.
Mentions: The enhancing effects of ultrasound and iontophoresis on skin permeation of hydrophilic compound can be explained by inducing convective solvent flow13. In the present study, we analyzed how the transport of the hydrophilic compound acetyl hexapeptide-3 was improved by microneedles based on the relationship between hydrophilic solute and vehicle (D2O) transport. To assess the skin permeability of D2O and acetyl hexapeptide-3, the time course of D2O flux and permeation clearance of acetyl hexapeptide-3 under various osmotic concentrations were determined (Fig. 6). A good correlation was observed between the acetyl hexapeptide-3 clearance and the D2O flux (r=0.96, slope of the regression line: 0.23±0.037). The results suggest that convection generated by microneedles plays an important role in skin permeability of hydrophilic drugs.

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