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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

Calcein fluorescence across the porcine ear skin at Z=0, 20, 40, 60, 80 and 100 μm following microneedle pretreatment. Z direction is defined as perpendicular distance to the skin surface from the dermis. Fluorescence-emission signal of calcein is represented by green color.
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f0010: Calcein fluorescence across the porcine ear skin at Z=0, 20, 40, 60, 80 and 100 μm following microneedle pretreatment. Z direction is defined as perpendicular distance to the skin surface from the dermis. Fluorescence-emission signal of calcein is represented by green color.

Mentions: In order to directly verify the formation of microconduits in the skin, microneedles with 150 μm length were used with an insertion system designed to pierce the skin at a constant speed. Fig. 2 shows the distribution of calcien fluorescence at skin depths of 0, 20, 40, 60, 80 and 100 μm after microneedle pretreatment. Confocal images confirmed the formation of microconduits by microneedle pretreatment. Calcein fluorescence was confined to microconduits, while dots correspond to sites of microconduits from the array. Calcein could diffuse into deeper skin layers. At Z=80 μm, the fluorescence of calcein around microconduits are still visible, but at Z=100 μm, there is trace amount of calcein fluorescence and microconduits is disappeared.


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

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

Calcein fluorescence across the porcine ear skin at Z=0, 20, 40, 60, 80 and 100 μm following microneedle pretreatment. Z direction is defined as perpendicular distance to the skin surface from the dermis. Fluorescence-emission signal of calcein is represented by green color.
© Copyright Policy - CC BY-NC-ND
Related In: Results  -  Collection

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

f0010: Calcein fluorescence across the porcine ear skin at Z=0, 20, 40, 60, 80 and 100 μm following microneedle pretreatment. Z direction is defined as perpendicular distance to the skin surface from the dermis. Fluorescence-emission signal of calcein is represented by green color.
Mentions: In order to directly verify the formation of microconduits in the skin, microneedles with 150 μm length were used with an insertion system designed to pierce the skin at a constant speed. Fig. 2 shows the distribution of calcien fluorescence at skin depths of 0, 20, 40, 60, 80 and 100 μm after microneedle pretreatment. Confocal images confirmed the formation of microconduits by microneedle pretreatment. Calcein fluorescence was confined to microconduits, while dots correspond to sites of microconduits from the array. Calcein could diffuse into deeper skin layers. At Z=80 μm, the fluorescence of calcein around microconduits are still visible, but at Z=100 μm, there is trace amount of calcein fluorescence and microconduits is disappeared.

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