U. Schroeder et al., NANOPARTICLE TECHNOLOGY FOR DELIVERY OF DRUGS ACROSS THE BLOOD-BRAIN-BARRIER, Journal of pharmaceutical sciences, 87(11), 1998, pp. 1305-1307
The Leu-enkephalin dalargin and the Met-enkephalin kyotorphin normally
do not cross the blood-brain barrier (BBB) when given systemically. T
o transport these neuropeptides across the BBB they were adsorbed onto
the surface of poly(butylcyanoacrylate) nanoparticles (NPs) and the N
Ps were coated with polysorbate 80. Central analgesia was measured by
the hot plate test in mice. The antidepressant amitriptyline, which no
rmally penetrates the BBB, was used to examine the versatility of the
NP method. The concentration, of amitriptyline in serum and brain of m
ice was determined by a gas; chromatographic method. Furthermore, NPs
were fabricated with different stabilizers. After the adsorption of th
e peptides on polysorbate 85-stabilized NPs, analgesia was noted after
intravenous application when NPs were not coated. The amitriptyline l
evel was significantly enhanced in brain when the substance was adsorb
ed onto the NP and coated or when the particles were stabilized with p
olysorbate 85.