Transmucosal delivery of oxytocin to rabbits using a mucoadhesive buccal patch

Pharmaceutical Development and Technology
C LiT P Johnston

Abstract

A biocompatible, mucoadhesive buccal patch was evaluated in rabbits for transmucosal delivery of peptides. Oxytocin (OT) was incorporated into custom coformulations of Carbopol 974P and silicone polymer and the resulting plasma OT concentration versus time profiles determined following patch application. For comparative purposes, the mean values determined for the elimination half-life (t1/2), volume of distribution (Vd), and the total body clearance (CL) following intravenous injection of OT were 2.9 +/- 0.2 min, 85.3 +/- 6.7 ml, and 20.4 +/- 2.03 ml/min, respectively. Following application of oxytocin-loaded mucoadhesive patches, plasma OT concentrations remained 20- to 28-fold greater from 0.5 to 3.0 hr than control animals administered placebo patches. The steady-state plasma OT concentration (Css) following application of the buccal patches was 80.6 +/- 15.9 pg/ml. The lag-time associated with attainment of the Css was 0.45 +/- 0.18 hr. Steady-state flux (Jss) of oxytocin in vivo was 139 +/- 36.8 ng/hr/cm2. Based on the amount of OT remaining in the patches following removal, the average dose of OT released in vivo was 0.27 +/- 0.024 mg with a bioavailability of 0.1%. No significant alterations in mucosal histology were ob...Continue Reading

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Citations

Aug 6, 1999·Pharmaceutical Development and Technology·H H AlurT P Johnston
Mar 1, 2014·Drug Development and Industrial Pharmacy·Flavia Laffleur
Mar 13, 2014·Drug Development and Industrial Pharmacy·Javier O Morales, Jason T McConville
Aug 23, 2008·Drug Development and Industrial Pharmacy·G S AsaneY Madhusudan Rao
Jan 7, 1999·Drug Development and Industrial Pharmacy·C LiT P Johnston
May 27, 2009·Drug Development and Industrial Pharmacy·Marie WahlgrenStefan Ulvenlund
Jul 10, 2008·Drug Development and Industrial Pharmacy·Munish Kumar DhimanKrutika K Sawant
Sep 5, 2002·Journal of Pharmaceutical Sciences·Steven JayRussell J Mumper
Jan 3, 2012·Colloids and Surfaces. B, Biointerfaces·David Ivarsson, Marie Wahlgren
May 1, 2010·Pharmaceutical Development and Technology·Maimoona G Chinwala, Senshang Lin
Apr 5, 2001·Clinical Pharmacokinetics·J Woodley
Jan 4, 2017·Expert Opinion on Drug Delivery·Sandra Lindert, Jörg Breitkreutz
Mar 1, 2015·Interdisciplinary Toxicology·Harold I Zeliger, Boguslaw Lipinski
Jan 11, 2005·The Journal of Pharmacy and Pharmacology·Katarina Edsman, Helene Hägerström
Jan 4, 2012·Carbohydrate Polymers·Angela AbruzzoBarbara Luppi

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