Delivery of loperamide across the blood-brain barrier with polysorbate 80-coated polybutylcyanoacrylate nanoparticles.
OBJECTIVE
The possibility of using polysorbate 80-coated nanoparticles for the delivery of the water insoluble opioid agonist loperamide across the blood-brain barrier was investigated. The analgesic effect after i.v. injection of the preparations was used to indicate drug transport through this barrier.


METHODS
Loperamide was incorporated into PBCA nanoparticles. Drug-containing nanoparticles were coated with polysorbate 80 and injected intravenously into mice. Analgesia was then measured by the tail-flick test.


RESULTS
Intravenous injection of the particulate formulation resulted in a long and significant analgesic effect. A polysorbate 80 loperamide solution induced a much less pronounced and very short analgesia. Uncoated nanoparticles loaded with loperamide were unable to produce analgesia.


CONCLUSIONS
Polysorbate 80-coated PBCA nanoparticles loaded with loperamide enabled the transport of loperamide to the brain.
Alyautdin
R N
RN
Department of Pharmacology, Sechenov Medical Academy, Moscow, Russia.
Petrov
V E
VE
Langer
K
K
Berthold
A
A
Kharkevich
D A
DA
Kreuter
J
J
D000700:Analgesics / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology; D000818:Animals; D001812:Blood-Brain Barrier; D004337:Drug Carriers; D004659:Enbucrilate; D008139:Loperamide / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D008297:Male; D051379:Mice; D008863:Microspheres; D010147:Pain Measurement; D010316:Particle Size; D011136:Polysorbates
D000700:Analgesics; D004337:Drug Carriers; D011136:Polysorbates; D008139:Loperamide; D004659:Enbucrilate