Transbuccal peptide delivery: stability and in vitro permeation studies on endomorphin-1

Journal of Controlled Release : Official Journal of the Controlled Release Society
A P BirdA H Shojaei

Abstract

The purpose of this study was to investigate the feasibility of buccal delivery of a model peptide, endomorphin-1 (ENI), using stability and in vitro permeation studies. ENI is a recently isolated mu-opiate receptor agonist with high selectivity and specificity for this receptor subtype. Stability studies were conducted in various buffers and the drug was shown to be stable in both acidic and basic buffer systems. In the presence of full thickness porcine buccal epithelium, ENI was unstable with only 23.4+/-15.7% intact drug present after 6 h. The region responsible for this degradation was found to coincide with the major barrier region of the buccal epithelium as delineated through stability experiments in the presence of partial thickness buccal epithelium. Various peptidase inhibitors were used to isolate the enzyme(s) responsible for this degradation. Diprotin-A, a potent inhibitor of dipeptidyl peptidase IV, provided significant inhibition of the degradation of ENI in the presence of buccal epithelium. In vitro permeation studies revealed that the permeability coefficient of ENI across porcine buccal epithelium was 5.67+/-4.74x10(-7) cm/s. The enzymatic degradation of ENI was found not to be rate limiting to the drug's pe...Continue Reading

Citations

Apr 22, 2010·AAPS PharmSciTech·Saadia A TayelDina Louis
Feb 20, 2015·Advanced Healthcare Materials·Gopakumar GopalakrishnanPatrick Couvreur
Jun 1, 2014·International Journal of Pharmaceutics·Mohammed SattarMajella E Lane
Aug 30, 2014·Pharmaceutical Research·Thiago CaonJoseph A Nicolazzo
Aug 2, 2003·Critical Reviews in Clinical Laboratory Sciences·Anne-Marie LambeirIngrid De Meester

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