Poloxamer gel as vehicle for transdermal iontophoretic delivery of arginine vasopressin: evaluation of in vivo performance in rats.
The present study describes the formulation and evaluation for pharmacokinetic and pharmacodynamic activity of arginine vasopressin (AVP), a nanopeptide with antidiuretic activity on being delivered by transdermal iontophoresis. Poloxamer 407 was used to form stable gels that did not reduce the release of AVP. The release rate from the gel followed Higuchi kinetics indicating that the dominant mechanism of release is diffusion. Iontophoresis alone and in combination with chemical enhancers was used to augment the transdermal permeation of AVP. The results of both pharmacokinetic and pharmacodynamic studies emphasize the dimension of 'rapid onset' achieved by iontophoresis. The correlation between pharmacokinetic data and pharmacodynamic activity was only qualitative. Histopathological studies revealed that skin toxicity caused by either iontophoresis or chemical enhancers when used alone could be reduced by using a combination of both the techniques in tandem.
Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Sector-67, S.A.S. Nagar, 160 062, Punjab, India. panchagnula@yahoo.com
Vinod
V
Nair
Ramesh
R
Panchagnula
D000279:Administration, Cutaneous; D000704:Analysis of Variance; D000818:Animals; D001127:Arginine Vasopressin / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D003511:Cyclohexanols / Q000493:pharmacokinetics; D000077591:Eucalyptol; D005782:Gels; D007478:Iontophoresis / Q000379:methods*; D008051:Lipid Bilayers / Q000493:pharmacokinetics; D039821:Monoterpenes / Q000493:pharmacokinetics; D019301:Oleic Acid / Q000493:pharmacokinetics; D014677:Pharmaceutical Vehicles; D020442:Poloxamer / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012867:Skin / Q000187:drug effects / Q000503:physiopathology; D017550:Spectroscopy, Fourier Transform Infrared
D003511:Cyclohexanols; D005782:Gels; D008051:Lipid Bilayers; D039821:Monoterpenes; D014677:Pharmaceutical Vehicles; D020442:Poloxamer; D001127:Arginine Vasopressin; D019301:Oleic Acid; D000077591:Eucalyptol