Transdermal Iontophoretic Delivery of Lysine-Proline-Valine (KPV) Peptide Across Microporated Human Skin.
Lysine-proline-valine (KPV) is a C-terminal peptide fragment of α-melanocyte stimulating hormone with potent anti-inflammatory properties. Present study investigates various transdermal enhancement strategies such as iontophoresis (ITP), microneedles (MN), and their combination (ITP + MN) on KPV delivery across dermatomed human skin. KPV attains a positive charge at pH less than 7.0, thus anodal ITP was used. The influence of current strength, KPV concentration, and duration of current application on the KPV delivery was investigated. At defined ITP parameters, the influence of MN on KPV delivery (ITP + MN) across skin was also determined. KPV permeation was less than detectable levels (limit of detection, 0.01 μg/mL) by simple passive diffusion. However, KPV permeation was increased to 4.4 μg/cm2/h by MN treatment. Furthermore, ITP and ITP + MN increased the permeation rate by 8 and 35 fold, respectively, as compared to MN alone. The skin retention levels of KPV by MN, ITP, and ITP + MN were increased by 5, 10, and 10 fold, respectively, as compared to passive diffusion. Confocal studies indicate that fluorescein isothiocyanate-labeled KPV migrated through the stratum corneum, along the microchannels and into the lower epidermal tissue because the fluorescence was observed beyond the depth of 100 μm.
Department of Drug Discovery and Development, Auburn University, Auburn, Alabama 36849.
Kasturi
K
Pawar
Department of Pharmaceutical and Biomedical Sciences, College of Pharmacy, California Health Sciences University, Clovis, California 93612.
Chandra S
CS
Kolli
Department of Materials Science and Engineering, Tuskegee University, Tuskegee, Alabama 36088.
Vijaya K
VK
Rangari
Department of Drug Discovery and Development, Auburn University, Auburn, Alabama 36849. Electronic address: rjbabu68@gmail.com.
R Jayachandra
RJ
Babu
D000279:Administration, Cutaneous; D004058:Diffusion; D016503:Drug Delivery Systems / Q000379:methods; D006801:Humans; D007478:Iontophoresis / Q000379:methods*; D009842:Oligopeptides / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption
D009842:Oligopeptides
iontophoresis; passive diffusion/transport; peptide delivery; percutaneous; skin; transdermal