Systemic absorption of L- and D-phenylalanine across the rat nasal mucosa

Abstract

Nasal absorption of L-phenylalanine (L-Phe) and D-phenylalanine (D-Phe) have been investigated in rats using an in vivo absorption technique. L-Phe was effectively absorbed into systemic circulation with peak plasma level at 45 min after nasal administration. The absolute nasal bioavailability was calculated to be 96.3% when 5 mg/kg dose was given to fasted rats. The absolute bioavailability declined to 66.8% when 12.5 mg/kg of L-Phe was given intranasally while the time to reach peak concentration remained at 45 min. The results substantiated previous in situ data that, despite its high polarity, L-Phe was transported across the rat nasal mucosa into blood stream by the large neutral amino acid (LNAA) carrier. The carrier showed partial saturation at higher doses. On the other hand, when 5 mg/kg of D-Phe was given intranasally, slow and incomplete absorption was observed resulting in a peak time of 60 min and an absolute bioavailability of only 35.2%, suggesting specificity of the carrier for natural L-amino acids.