title: Transdermal delivery of a approximately 13 kDa protein--an in vivo comparison of physical enhancement methods.
abstract: The availability of several enhancement techniques has made it possible to study delivery of macromolecules through skin. This study was conducted to evaluate the transdermal delivery of a ~13 kDa protein using iontophoresis, sonophoresis, and microneedles alone or in combination. In vivo delivery experiments were carried out using hairless rats with daniplestim (DP) as the model protein (molecular weight: 12.760 kDa; isoelectric point, 6.2). Delivery enhancement abilities of the above techniques were evaluated at two different drug concentrations in the patch: 2 mg/mL and 5 mg/mL. At a drug loading concentration of 2 mg/mL maximum delivery was seen with the combination of microneedles and iontophoresis. At 5 mg/mL, sonophoresis alone gave a C(max) of 8.22 +/- 5.9 ng/mL and a combination of sonophoresis and iontophoresis gave a C(max) of 4.9 +/- 1.8 ng/mL. The results of this study suggest that combination of microneedles and iontophoresis was the most effective approach in delivering a 13 kDa protein through the skin.
authors.affiliation: Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, Mercer University, Atlanta, GA 30341, USA.
authors.forename: Sahitya
authors.initials: S
authors.lastname: Katikaneni
authors.forename: Guohua
authors.initials: G
authors.lastname: Li
authors.forename: Advait
authors.initials: A
authors.lastname: Badkar
authors.forename: Ajay K
authors.initials: AK
authors.lastname: Banga
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D019540:Area Under Curve; D004305:Dose-Response Relationship, Drug; D004337:Drug Carriers / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D016503:Drug Delivery Systems; D018274:Electroporation / Q000379:methods; D007377:Interleukin-3 / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000097:blood / Q000493:pharmacokinetics / Q000494:pharmacology; D007478:Iontophoresis; D008297:Male; D010446:Peptide Fragments / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics* / Q000494:pharmacology; D010539:Permeability; D051381:Rats; D054772:Rats, Hairless; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption
chemical_list: D004337:Drug Carriers; D007377:Interleukin-3; D010446:Peptide Fragments; C093340:daniplestim