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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.


Related in: MedlinePlus

The microneedle array and the autoapplicator employed in this study. (A) Microneedle array; (B) autoapplicator.
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f0005: The microneedle array and the autoapplicator employed in this study. (A) Microneedle array; (B) autoapplicator.

Mentions: Microneedle arrays and applicator were developed by our group and made by Nasheng Microelectronics (Suzhou) Co. Ltd., China. Arrays of solid microneedle (Fig. 1A) were fabricated by dry and wet etching from silicon wafers. Each microneedle array has 121 needles of 150 μm-length in an area of 4 mm×4 mm. The array was fixed onto a supporting column (5 mm in diameter) of applicator (Fig. 1B), which provided insertion force of nearly 2 N. Microneedle arrays were inserted into the skin with a constant vibration frequency for 20 s.


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

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

The microneedle array and the autoapplicator employed in this study. (A) Microneedle array; (B) autoapplicator.
© Copyright Policy - CC BY-NC-ND
Related In: Results  -  Collection

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

f0005: The microneedle array and the autoapplicator employed in this study. (A) Microneedle array; (B) autoapplicator.
Mentions: Microneedle arrays and applicator were developed by our group and made by Nasheng Microelectronics (Suzhou) Co. Ltd., China. Arrays of solid microneedle (Fig. 1A) were fabricated by dry and wet etching from silicon wafers. Each microneedle array has 121 needles of 150 μm-length in an area of 4 mm×4 mm. The array was fixed onto a supporting column (5 mm in diameter) of applicator (Fig. 1B), which provided insertion force of nearly 2 N. Microneedle arrays were inserted into the skin with a constant vibration frequency for 20 s.

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