Lectin poly(lactide) microsphere conjugates specifically designed for oral
administration were prepared and their activity and specificity in presence
of mucus were characterized. The presence of hydroxyl or amino groups suit
able for covalent coupling of lectins by the glutaraldehyde method at the s
urface of the microspheres have been ensured by preparing the particles in
presence either of poly(vinyl alcohol) (PVA) or bovine serum albumin (BSA).
Tomato and asparagus pea lectins could be covalently attached to these par
ticles (1.0-1.3 mg/m(2) of particles). The conjugates demonstrated a 4-10 f
old increase in their interactions with mucus compared to control particles
. Moreover, the sugar specificity of the lectins was maintained. (C) 2001 E
lsevier Science B.V. All rights reserved.